The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Article Title | Organization | Depostion |
|---|
| 19746963 |
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
Purdue University |
12/19/09 |
| 19848404 |
Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase. |
Wyeth Research |
12/19/09 |
| 18835174 |
Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists. |
Astellas Pharma Inc. |
12/19/09 |
| 19321349 |
Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists. |
Astellas Pharma Inc. |
12/19/09 |
| 19695884 |
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides. |
Vernalis (R&D) Ltd |
12/17/09 |
| 19201197 |
Carbonic anhydrase inhibitors. The nematode alpha-carbonic anhydrase of Caenorhabditis elegans CAH-4b is highly inhibited by 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides. |
Istanbul University |
12/17/09 |
| 19700331 |
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists. |
Ono Pharmaceutical Co., Ltd |
12/17/09 |
| 19645433 |
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription. |
St. Jude Research Hospital |
12/17/09 |
| 19736928 |
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). |
AstraZeneca |
12/17/09 |
| 19700330 |
Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity. |
Virginia Commonwealth University |
12/17/09 |
| 19884015 |
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: exploration of 5-6 fused rings as alternative S1 moieties. |
Daiichi Sankyo Co, Ltd |
12/16/09 |
| 10482466 |
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist. |
Otsuka Pharmaceutical Co., Ltd |
12/15/09 |
| 19900813 |
Optimization of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetamide derivatives as arginine vasopressin V2 receptor agonists and discussion of their binding modes. |
Astellas Pharma Inc. |
12/15/09 |
| 19827834 |
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. |
Vertex |
12/15/09 |
| 18434170 |
Synthesis of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives as inhibitors of human liver glycogen phosphorylase a. |
Astellas Pharma Inc. |
12/15/09 |
| 19645448 |
ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines |
Wyeth Research |
12/14/09 |
| 19877603 |
Identification and Biological Evaluation of a Series of 1H-Benzo[de]isoquinoline-1,3(2H)-diones as Hepatitis C Virus NS5B Polymerase Inhibitors (double dagger). |
IRBM-MRL Rome |
12/14/09 |
| 19877692 |
Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: quinone oxidoreductase-1 (NQO1). |
University of Manchester |
12/13/09 |
| 18952447 |
Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors. |
Astellas Pharma Inc. |
12/10/09 |
| 19539481 |
Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
Istanbul University |
12/09/09 |
| 19900814 |
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: exploration of 6-6 fused rings as alternative S1 moieties. |
Daiichi Sankyo Co, Ltd |
12/08/09 |
| 17433696 |
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists. |
AstraZeneca |
12/08/09 |
| 19443226 |
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives. |
Griffith University |
12/07/09 |
| 19896847 |
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. |
Bristol-Myers Squibb Company |
12/06/09 |
| 19764794 |
Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. |
Amgen |
12/06/09 |
| 19162487 |
Biarylether amide quinolines as liver X receptor agonists. |
Wyeth Research |
11/29/09 |
| 19811924 |
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury. |
Dainippon Sumitomo Pharma Co |
11/26/09 |
| 19097791 |
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor. |
Pfizer |
11/25/09 |
| 19836248 |
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3. |
Wyeth Research |
11/25/09 |
| 19884013 |
5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity. |
Wyeth Research |
11/25/09 |
| 19836247 |
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles. |
Wyeth Research |
11/25/09 |
| 19853462 |
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists. |
Wyeth Research |
11/24/09 |
| 19880322 |
N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53. |
NIH |
11/24/09 |
| 19842661 |
Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases. |
Abbott Laboratories |
11/23/09 |
| 17638903 |
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. |
University Hospital Basel |
11/23/09 |
| 19117760 |
Structure-based virtual screening for novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase and their experimental evaluation. |
Northern Kentucky University |
11/11/09 |
| 19450983 |
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
Universite degli Studi di Firenze |
11/10/09 |
| 19699645 |
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase. |
Northern Kentucky University |
11/10/09 |
| 19781947 |
Glucose-based spiro-isoxazolines: a new family of potent glycogen phosphorylase inhibitors. |
Universite de Lyon |
11/10/09 |
| 17184135 |
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site. |
Rutgers University |
11/10/09 |
| 19758807 |
Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts. |
Universitat de Barcelona |
11/10/09 |
| 19758809 |
Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. |
Shanghai Institutes for Biological Sciences |
11/09/09 |
| 18394907 |
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies. |
Pfizer |
11/09/09 |
| 17616632 |
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. |
NIH |
11/09/09 |
| 19748274 |
Tetraiodobenzimidazoles are potent inhibitors of protein kinase CK2. |
University of Padova |
11/09/09 |
| 19773165 |
Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements. |
Johnson & Johnson Pharmaceutical |
11/08/09 |
| 19729306 |
Structure-based design of novel human Pin1 inhibitors (I). |
Pfizer |
11/08/09 |
| 19827831 |
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. |
Novartis |
11/07/09 |
| 19791799 |
RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information. |
Gilead Sciences Inc. |
11/07/09 |
| 18831589 |
Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity. |
National Cancer Institute |
11/07/09 |
| 19748785 |
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors. |
Duquesne University |
11/06/09 |
| 19781950 |
Discovery and structure-activity relationship analysis of Staphylococcus aureus sortase A inhibitors. |
University of California at Los Angeles |
10/27/09 |
| 19572550 |
Flaviviral protease inhibitors identified by fragment-based library docking into a structure generated by molecular dynamics. |
University of Zurich |
10/27/09 |
| 19783444 |
Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists. |
Pfizer |
10/27/09 |
| 19767211 |
Synthesis and structure-activity relationships of dehydroaltenusin derivatives as selective DNA polymerase alpha inhibitors. |
Kyoto Prefectural University |
10/27/09 |
| 19682971 |
A fluorescence quenching assay to discriminate between specific and nonspecific inhibitors of dengue virus protease. |
Novartis Institute for Tropical Diseases |
10/26/09 |
| 19773173 |
Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II. |
Universita degli Studi di Firenze |
10/26/09 |
| 19610616 |
Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone. |
Vernalis (R&D) Ltd |
10/26/09 |
| 15582469 |
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases. |
University of Alabama at Birmingham |
10/26/09 |
| 19572549 |
Identification of inhibitors of checkpoint kinase 1 through template screening. |
The Institute of Cancer Research |
10/25/09 |
| 19731956 |
Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
CNR |
10/22/09 |
| 19620011 |
Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy. |
Universita degli Studi di Milano |
10/14/09 |
| 19555120 |
Botryllamides: Natural Product Inhibitors of ABCG2. |
SAIC-Frederick |
10/13/09 |
| 19413326 |
Discovery of antibacterial biotin carboxylase inhibitors by virtual screening and fragment-based approaches. |
Pfizer |
10/13/09 |
| 18089721 |
New inhibitors of ABCG2 identified by high-throughput screening. |
SAIC-Frederick |
10/13/09 |
| 19520086 |
Think twice: understanding the high potency of bis(phenyl)methane inhibitors of thrombin. |
Philipps-University Marburg |
10/13/09 |
| 18760609 |
Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors. |
Philipps-University Marburg |
10/12/09 |
| 19492850 |
Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists. |
Genentech |
10/12/09 |
| 19628388 |
Benzo[c][2,7]naphthyridines as inhibitors of PDK-1. |
Wyeth Research |
10/12/09 |
| 18511278 |
Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). |
Amgen Inc. |
10/12/09 |
| 18485702 |
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. |
Bristol-Myers Squibb Company |
10/12/09 |
| 19433357 |
Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors. |
The Scripps Research Institute |
10/12/09 |
| 19692239 |
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
10/11/09 |
| 19515558 |
Dipeptidyl nitrile inhibitors of Cathepsin L. |
AstraZeneca |
10/09/09 |
| 18316192 |
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
Chemical Genomics Centre of the Max Planck Society |
09/30/09 |
| 19719239 |
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents. |
Duquesne University |
09/29/09 |
| 19309082 |
Discovering potent inhibitors against the beta-hydroxyacyl-acyl carrier protein dehydratase (FabZ) of Helicobacter pylori: structure-based design, synthesis, bioassay, and crystal structure determination. |
Shanghai Institute of Materia Medica |
09/29/09 |
| 16807364 |
Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs. |
Queen's University |
09/29/09 |
| 19631219 |
Structural-thermodynamic relationships of interactions in the N-terminal ATP-binding domain of Hsp90. |
University College London |
09/29/09 |
| 19402633 |
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. |
Genentech |
09/28/09 |
| 19320487 |
A structure-based approach to ligand discovery for 2C-methyl-D-erythritol-2,4-cyclodiphosphate synthase: a target for antimicrobial therapy. |
University of Dundee |
09/28/09 |
| 19462975 |
Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
Chemical Genomics Centre of the Max Planck Society |
09/28/09 |
| 19256508 |
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. |
Vernalis (R&D) Ltd. |
09/28/09 |
| 19663388 |
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds. |
Universitat de Barcelona |
09/28/09 |
| 10964567 |
Structural basis for isotype selectivity of the human retinoic acid nuclear receptor. |
CNRS |
09/28/09 |
| 19338303 |
Structural insight into the inhibition of human kynurenine aminotransferase I/glutamine transaminase K. |
Virginia Tech |
09/28/09 |
| 19555126 |
Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. |
Burnham Institute for Medical Research |
09/27/09 |
| 19473017 |
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
Purdue University |
09/27/09 |
| 19527033 |
One scaffold, three binding modes: novel and selective pteridine reductase 1 inhibitors derived from fragment hits discovered by virtual screening. |
University of Dundee |
09/27/09 |
| 19678708 |
Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase. |
Almirall Research Center |
09/14/09 |
| 19630403 |
Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia (dagger) dagger Coordinates of the PDE10A crystal structures have been depo |
Pfizer |
09/14/09 |
| 19603809 |
Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. |
Nerviano Medical Sciences Srl |
09/14/09 |
| 19525117 |
Identification of PDE4B Over 4D subtype-selective inhibitors revealing an unprecedented binding mode. |
GSK |
09/14/09 |
| 19645480 |
Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease. |
Purdue University |
09/14/09 |
| 19268600 |
Synthesis and evaluation of imidazole-dioxolane compounds as selective heme oxygenase inhibitors: effect of substituents at the 4-position of the dioxolane ring. |
Queen's University |
09/14/09 |
| 19409795 |
Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores. |
BioCryst Pharmaceuticals |
09/13/09 |
| 19200745 |
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta. |
Takeda Pharmaceutical Company Ltd. |
09/13/09 |
| 19179081 |
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents. |
Yale University |
09/13/09 |
| 19246009 |
Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase. |
Duke University Medical Center |
09/13/09 |
| 18589438 |
Structure of the BH3 domains from the p53-inducible BH3-only proteins Noxa and Puma in complex with Mcl-1. |
University of Otago |
09/13/09 |
| 15826183 |
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction. |
Yale University |
09/13/09 |
| 16028929 |
Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL. |
Yale University |
09/13/09 |
| 15293988 |
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells. |
Virginia Commonwealth University |
08/17/09 |
| 11148027 |
Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53. |
Max Planck Institute |
08/17/09 |
| 15715460 |
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells. |
Johnson & Johnson Pharmaceutical |
08/17/09 |
| 16630722 |
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists. |
Johnson & Johnson Pharmaceutical |
08/17/09 |
| 16600594 |
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design. |
Johnson & Johnson Pharmaceutical |
08/17/09 |
| 19457663 |
Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking. |
H. Lee Moffitt Cancer Center |
08/17/09 |
| 16647257 |
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity. |
Johnson & Johnson Pharmaceutical |
08/17/09 |
| 17961830 |
Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta. |
University of Virginia at Charlottesville |
08/16/09 |
| 16789731 |
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy. |
University of Michigan |
08/16/09 |
| 19438227 |
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors. |
Pfizer |
08/16/09 |
| 15246006 |
Fluorescence polarization assay and inhibitor design for MDM2/p53 interaction. |
Schering-Plough Research Institute |
08/16/09 |
| 17034127 |
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. |
University of Newcastle upon Tyne |
08/16/09 |
| 19492852 |
Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase. |
Friedrich Alexander University Erlangen |
08/16/09 |
| 16759082 |
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction. |
University of Michigan |
08/16/09 |
| 18662878 |
4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase. |
Anadys Pharmaceuticals |
08/06/09 |
| 19422229 |
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13. |
Novartis |
08/06/09 |
| 18722768 |
Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase. |
Anadys Pharmaceuticals |
08/06/09 |
| 18487044 |
Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase. |
Anadys Pharmaceuticals |
08/06/09 |
| 18554907 |
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase. |
Anadys Pharmaceuticals |
08/06/09 |
| 19054673 |
5,6-Dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase. |
Anadys Pharmaceuticals |
08/05/09 |
| 18621523 |
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. |
GSK |
08/05/09 |
| 19328688 |
Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist. |
Roche R&D Center(China) Ltd |
08/05/09 |
| 18242088 |
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine. |
Anadys Pharmaceuticals |
08/05/09 |
| 18945615 |
Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity. |
Novartis |
08/04/09 |
| 18391212 |
Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation. |
Merck Research Laboratories |
07/26/09 |
| 19195886 |
Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors. |
Novartis |
07/07/09 |
| 18291646 |
Synthesis and SAR studies of indole-based MK2 inhibitors. |
Boehringer Ingelheim Pharmaceuticals Inc. |
07/06/09 |
| 19256502 |
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
Human BioMolecular Research Institute |
07/05/09 |
| 19457661 |
Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists. |
Banyu Pharmaceutical Co. |
07/05/09 |
| 19323560 |
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF). |
The Institute of Cancer Research |
07/05/09 |
| 17480064 |
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). |
Pfizer |
07/05/09 |
| 19477642 |
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent. |
GSK |
07/05/09 |
| 19406640 |
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics. |
GSK |
07/05/09 |
| 19428244 |
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics. |
GSK |
07/05/09 |
| 19464885 |
Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE. |
Wyeth Research |
07/05/09 |
| 19326941 |
Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6. |
Washington University |
07/05/09 |
| 17576063 |
The discovery of carboline analogs as potent MAPKAP-K2 inhibitors. |
Boehringer Ingelheim Pharmaceuticals Inc. |
07/05/09 |
| 19394217 |
2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists. |
Banyu Pharmaceutical Co. |
07/04/09 |
| 19447610 |
Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists. |
Banyu Pharmaceutical Co. |
07/04/09 |
| 19464886 |
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors. |
National Human Genome Research Institute |
07/04/09 |
| 18243697 |
Identification of a potent new chemotype for the selective inhibition of PDE4. |
NIH |
07/04/09 |
| 19398200 |
Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity. |
Banyu Pharmaceutical Co. |
07/02/09 |
| 19345579 |
Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles. |
Wyeth Research |
07/02/09 |
| 19457666 |
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines. |
Vitae Pharmaceuticals |
07/01/09 |
| 19450980 |
Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold. |
Merck-Serono |
07/01/09 |
| 19464171 |
Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma. |
Amgen |
07/01/09 |
| 19473839 |
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
Pfizer |
07/01/09 |
| 19464884 |
Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. |
Wyeth Research |
07/01/09 |
| 18254726 |
Kinetic, thermodynamic and X-ray structural insights into the interaction of melatonin and analogues with quinone reductase 2. |
University of Illinois at Chicago |
06/10/09 |
| 19338333 |
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. |
Kochi Medical School |
06/09/09 |
| 19271755 |
Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase. |
Burnham Institute for Medical Research |
06/09/09 |
| 19374444 |
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
CSIC |
06/09/09 |
| 19361210 |
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. |
Bristol-Myers Squibb Company |
06/08/09 |
| 19378991 |
Chalcones: a valid scaffold for monoamine oxidases inhibitors. |
Universita degli Studi di Roma La Sapienza |
06/08/09 |
| 19371038 |
Compounds binding to the S2-S3 pockets of thrombin. |
University of Kalmar |
06/08/09 |
| 19348415 |
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta). |
GSK |
06/08/09 |
| 19354253 |
Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase. |
Vanderbilt University |
06/08/09 |
| 19351168 |
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation. |
Bristol-Myers Squibb Company |
06/08/09 |
| 19309081 |
Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine. |
Wyeth Research |
06/08/09 |
| 19419203 |
Structure-based discovery of triphenylmethane derivatives as inhibitors of hepatitis C virus helicase. |
National Taiwan University |
06/08/09 |
| 19361209 |
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. |
Bristol-Myers Squibb Company |
06/08/09 |
| 19237285 |
Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation. |
CNRS |
06/07/09 |
| 19334715 |
Design, synthesis, and biological evaluation of new 5-HT4 receptor agonists: application as amyloid cascade modulators and potential therapeutic utility in Alzheimer's disease. |
CNRS |
06/07/09 |
| 18582436 |
ERRgamma tethers strongly bisphenol A and 4-alpha-cumylphenol in an induced-fit manner. |
Kyushu University |
06/07/09 |
| 19317450 |
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. |
Harvard Medical School |
06/07/09 |
| 17825569 |
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
Polish Academy of Science |
06/07/09 |
| 19317447 |
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
Kochi Medical School |
06/05/09 |
| 19265439 |
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities. |
Purdue University |
06/04/09 |
| 19296678 |
Crystal structures of constitutive nitric oxide synthases in complex with de novo designed inhibitors. |
University of California at Irvine |
06/03/09 |
| 19374401 |
Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models. |
Kalypsys Inc. |
06/03/09 |
| 19267475 |
Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins. |
Universita degli Studi di Roma La Sapienza |
06/03/09 |
| 19361197 |
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes. |
Universita del Piemonte Orientale |
06/01/09 |
| 19385613 |
Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties. |
Novo Nordisk A/S |
06/01/09 |
| 19338356 |
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
ACADIA Pharmaceuticals AB |
06/01/09 |
| 19351113 |
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
Pfizer |
05/25/09 |
| 19419202 |
Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity. |
University of St Andrews |
05/25/09 |
| 19351152 |
Structure-based design, synthesis, and characterization of inhibitors of human and Plasmodium falciparum dihydroorotate dehydrogenases. |
University of Leeds |
05/25/09 |
| 18178084 |
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase. |
Bristol-Myers Squibb Company |
05/10/09 |
| 18556202 |
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors. |
Wyeth Research |
05/10/09 |
| 16899369 |
Synthesis of bicyclic molecular scaffolds (BTAa): an investigation towards new selective MMP-12 inhibitors. |
University of Florence |
05/10/09 |
| 18799592 |
Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist. |
Bristol-Myers Squibb Company |
05/09/09 |
| 16275079 |
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors. |
Merck Research Laboratories |
05/08/09 |
| 19329331 |
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs. |
Absolute Science, Inc. |
05/08/09 |
| 19012391 |
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
Wyeth Research |
05/08/09 |
| 18221310 |
Rhodanine derivatives as selective protease inhibitors against bacterial toxins. |
Burnham Institute for Medical Research |
05/08/09 |
| 16931011 |
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2. |
GNF |
05/07/09 |
| 19053776 |
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
Consiglio Nazionale delle Ricerche |
05/07/09 |
| 17157019 |
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists. |
LG Life Sciences |
05/07/09 |
| 19296651 |
Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice. |
University of Washington at Seattle |
05/07/09 |
| 17403688 |
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands. |
Consiglio Nazionale delle Ricerche |
05/07/09 |
| 19168353 |
Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists. |
Johnson & Johnson Pharmaceutical |
05/06/09 |
| 18722772 |
Discovery of a novel class of PPARdelta partial agonists. |
GSK |
05/06/09 |
| 17243659 |
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents. |
GSK |
05/06/09 |
| 17608467 |
Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta. |
Johnson & Johnson Pharmaceutical |
05/06/09 |
| 18374567 |
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. |
Scripps Florida |
05/06/09 |
| 19345582 |
1-Sulfonylindazoles as potent and selective 5-HT6 ligands. |
Wyeth Research |
05/05/09 |
| 19346128 |
Synthesis and SAR of tolylamine 5-HT6 antagonists. |
Pfizer |
05/05/09 |
| 19159286 |
Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR). |
Exelixis Inc. |
05/02/09 |
| 19267461 |
Novel tricyclic inhibitors of IkappaB kinase. |
Bristol-Myers Squibb Company |
05/02/09 |
| 19217284 |
1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position. |
GSK |
04/21/09 |
| 19237286 |
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. |
GSK |
04/21/09 |
| 19226143 |
Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors. |
Universita di Pisa |
04/21/09 |
| 19209891 |
New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C(8) Substitution in Structural Analogues of S-Adenosylmethionine (dagger). |
Cornell University |
04/21/09 |
| 19243944 |
Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors. |
Japan Tobacco Inc. |
04/21/09 |
| 19028424 |
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
GSK |
04/21/09 |
| 19278250 |
A selective matrix metalloprotease 12 inhibitor for potential treatment of chronic obstructive pulmonary disease (COPD): discovery of (S)-2-(8-(methoxycarbonylamino)dibenzo[b,d]furan-3-sulfonamido)-3-methylbutanoic acid (MMP408). |
Wyeth Research |
04/20/09 |
| 19296695 |
Development of a novel virtual screening cascade protocol to identify potential trypanothione reductase inhibitors. |
University of Alberta |
04/20/09 |
| 19217779 |
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors. |
Amgen |
04/20/09 |
| 19256503 |
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode. |
Boehringer Ingelheim Pharmaceuticals Inc. |
04/20/09 |
| 19208477 |
Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors. |
GSK |
04/20/09 |
| 19097784 |
Discovery of thiophene inhibitors of polo-like kinase. |
GSK |
04/19/09 |
| 19217781 |
The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore. |
GSK |
04/19/09 |
| 18763755 |
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor acti |
Bristol-Myers Squibb Company |
04/06/09 |
| 19173605 |
Extra Binding Region Induced by Non-Zinc Chelating Inhibitors into the S(1)' Subsite of Matrix Metalloproteinase 8 (MMP-8) (dagger). |
Universita degli Studi |
04/06/09 |
| 19228017 |
Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold. |
Genentech, Inc. |
04/06/09 |
| 19193011 |
Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger). |
Johnson & Johnson Pharmaceutical |
04/06/09 |
| 19260677 |
Structure-activity relationships of orotidine-5'-monophosphate decarboxylase inhibitors as anticancer agents. |
Toronto General Research Institute |
04/06/09 |
| 19170530 |
Thioamide Hydroxypyrothiones Supersede Amide Hydroxypyrothiones in Potency against Anthrax Lethal Factor. |
Howard Hughes Medical Institute |
04/06/09 |
| 18287036 |
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases. |
GSK |
04/05/09 |
| 19217287 |
Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases. |
Abbott Laboratories |
04/05/09 |
| 19143533 |
Discovery and Structure-Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists. |
Bristol-Myers Squibb Company |
04/05/09 |
| 19260711 |
Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily. |
Bristol-Myers Squibb Company |
04/05/09 |
| 19256504 |
Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. |
AstraZeneca |
04/05/09 |
| 19245211 |
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol. |
Intervet Innovation GmbH |
04/05/09 |
| 19243938 |
Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors. |
University of Michigan at Ann Arbor |
04/04/09 |
| 19231176 |
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator. |
F. Hoffmann-La Roche Ltd |
04/04/09 |
| 19217782 |
Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production. |
Abbott Laboratories |
04/04/09 |
| 19041240 |
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. |
Wyeth Research |
04/04/09 |
| 18501599 |
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. |
Wyeth Research |
04/04/09 |
| 19056263 |
Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. |
GSK |
03/25/09 |
| 19131248 |
N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). |
MethylGene Inc. |
03/25/09 |
| 19071018 |
Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. |
GSK |
03/25/09 |
| 19007201 |
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
Roche Palo Alto LLC |
03/24/09 |
| 19128971 |
Discovery of 2-(alpha-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS. |
Cytopia Research Pty Ltd |
03/24/09 |
| 16288880 |
Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling. |
Fujisawa Pharmaceutical Co. Ltd |
03/24/09 |
| 18713665 |
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors. |
Deltagen Research Laboratories |
03/24/09 |
| 19138518 |
Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases. |
Boehringer Ingelheim (Canada) Ltd. |
03/24/09 |
| 19175319 |
Novel Indazole Non-Nucleoside Reverse Transcriptase Inhibitors Using Molecular Hybridization Based on Crystallographic Overlays (dagger). |
Pfizer |
03/24/09 |
| 19170521 |
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations. |
Universita di Siena |
03/24/09 |
| 19138846 |
Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy. |
GSK |
03/23/09 |
| 18579376 |
Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase. |
KuDOS Pharmaceuticals Ltd |
03/23/09 |
| 19138845 |
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization. |
Merck Research Laboratories |
03/23/09 |
| 19167883 |
Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines. |
Gilead Sciences Inc. |
03/23/09 |
| 18201066 |
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships. |
Nerviano Medical Sciences Srl |
03/10/09 |
| 17416521 |
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
Tanabe Research Laboratories USA |
03/10/09 |
| 19143565 |
Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases. |
Institute of Chemistry in Estonia |
03/10/09 |
| 18800822 |
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. |
KuDOS Pharmaceuticals Ltd. |
03/09/09 |
| 16997559 |
5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase. |
GSK |
03/09/09 |
| 16078828 |
Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone. |
Inotek Pharmaceuticals Corporation |
03/09/09 |
| 18809672 |
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. |
University of Konstanz |
03/09/09 |
| 19071019 |
Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors. |
Roche |
03/09/09 |
| 17502144 |
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. |
GSK |
03/09/09 |
| 17587573 |
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
Tanabe Research Laboratories USA |
03/08/09 |
| 19102698 |
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
Pfizer |
03/08/09 |
| 19115845 |
First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. |
Nerviano Medical Sciences Srl |
03/08/09 |
| 19093884 |
Non-peptide macrocyclic histone deacetylase inhibitors. |
Georgia Institute of Technology |
03/07/09 |
| 19128055 |
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue. |
Universite de Lyon |
03/06/09 |
| 18683917 |
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
Abbott Laboratories |
03/06/09 |
| 19143569 |
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer. |
Abbott Laboratories |
02/24/09 |
| 19167885 |
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. |
GSK |
02/24/09 |
| 18541433 |
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer. |
Abbott Laboratories |
02/23/09 |
| 19102654 |
Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease. |
Schering-Plough Research Institute |
02/23/09 |
| 19041249 |
Discovery and structure-activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists. |
Nippon Shinyaku Co. |
02/23/09 |
| 19143567 |
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. |
Astex |
02/23/09 |
| 19168351 |
Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings. |
Schering-Plough Research Institute |
02/23/09 |
| 19119014 |
Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
Universita degli Studi di Firenze |
02/22/09 |
| 19128966 |
Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions. |
Universita degli Studi di Firenze |
02/22/09 |
| 19193158 |
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
University of Tampere |
02/22/09 |
| 19147350 |
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2. |
Schering-Plough Research Institute |
02/22/09 |
| 19154150 |
Design, synthesis, and evaluation of oxygen-containing macrocyclic peptidomimetics as inhibitors of HCV NS3 protease. |
Schering-Plough Research Institute |
02/20/09 |
| 19022670 |
Potent inhibitors of HCV-NS3 protease derived from boronic acids. |
Schering-Plough Research Institute |
02/20/09 |
| 14766749 |
Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors. |
Vertex |
02/11/09 |
| 18930400 |
2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket. |
Boehringer Ingelheim Pharmaceuticals Inc. |
02/10/09 |
| 17218638 |
Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase. |
Loma Linda University |
02/10/09 |
| 18234496 |
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Company |
02/09/09 |
| 19111460 |
Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design. |
Boehringer Ingelheim Pharmaceuticals Inc. |
02/09/09 |
| 18242982 |
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents. |
Bristol-Myers Squibb Company |
02/09/09 |
| 16866524 |
The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. |
The Scripps Research Institute |
02/09/09 |
| 18171615 |
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells. |
GSK |
02/08/09 |
| 17459705 |
Novel inhibitors of fatty acid amide hydrolase. |
Bristol-Myers Squibb Company |
02/08/09 |
| 17949010 |
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
Pfizer |
02/08/09 |
| 19072118 |
Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors. |
Abbott Laboratories |
02/08/09 |
| 18290603 |
Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase. |
Vertex |
02/07/09 |
| 17251021 |
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. |
Valeant Pharmaceuticals Research and Development |
02/07/09 |
| 18790640 |
Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling. |
Abbott Laboratories |
02/07/09 |
| 19072652 |
Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. |
Medical University of South Carolina |
02/07/09 |
| 18042731 |
Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids. |
The Johns Hopkins University |
01/30/09 |
| 19072053 |
Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors. |
University of Southern California |
01/27/09 |
| 18054488 |
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones. |
Vertex Pharmaceuticals |
01/26/09 |
| 18282708 |
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents. |
Bristol-Myers Squibb Company |
01/26/09 |
| 19010686 |
Structure-activity relationship studies of 5-benzylaminoimidazo[1,2-c]pyrimidine-8-carboxamide derivatives as potent, highly selective ZAP-70 kinase inhibitors. |
Kissei Pharmaceutical Company |
01/26/09 |
| 19054672 |
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors. |
Schering-Plough Research Institute |
01/25/09 |
| 17289381 |
Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides. |
Vertex Pharmaceuticals |
01/25/09 |
| 19007108 |
Synthetic and Crystallographic Studies of a New Inhibitor Series Targeting Bacillus anthracis Dihydrofolate Reductase. |
University of Connecticut |
01/25/09 |
| 18457381 |
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability. |
GSK |
01/24/09 |
| 18005335 |
Selectivity-determining residues in Plk1. |
Pfizer |
01/24/09 |
| 18620382 |
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. |
GSK |
01/23/09 |
| 19036583 |
Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement. |
Merck Research Laboratories |
01/23/09 |
| 19007109 |
Novel Naphthalene-N-sulfonyl-d-glutamic Acid Derivatives as Inhibitors of MurD, a Key Peptidoglycan Biosynthesis Enzyme. |
Lek Pharmaceuticals d.d. |
01/23/09 |
| 18817367 |
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. |
Abbott Laboratories |
01/23/09 |
| 18321037 |
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation. |
Amgen |
01/07/09 |
| 18998662 |
Design, Structure-Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors. |
Bristol-Myers Squibb Company |
01/05/09 |
| 19007202 |
Development of Novel G-Protein-Coupled Receptor 54 Agonists with Resistance to Degradation by Matrix Metalloproteinase. |
Kyoto University |
01/05/09 |
| 18678489 |
Discovery of a potent and selective aurora kinase inhibitor. |
Sunesis Pharmaceuticals |
01/05/09 |
| 17373783 |
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. |
AstraZeneca |
01/05/09 |
| 18620380 |
Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid. |
Monash University |
01/05/09 |
| 18973287 |
Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different. |
University of Wisconsin at Madison |
01/05/09 |
| 19006379 |
Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors. |
University of Ferrara |
01/05/09 |
| 18805694 |
Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators. |
The Ohio State University |
01/04/09 |
| 18947224 |
Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease. |
Neurocrine Bioscience |
01/04/09 |
| 18811133 |
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands. |
Abbott Laboratories |
01/04/09 |
| 18983139 |
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia. |
Abbott Laboratories |
01/04/09 |
| 19012392 |
Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases. |
Shanghai Institute of Organic Chemistry |
01/03/09 |
| 18954041 |
Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP). |
University of Michigan |
01/03/09 |
| 18851976 |
Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles. |
University of Milano |
01/03/09 |
| 18294849 |
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity. |
AstraZeneca |
01/01/09 |
| 18942827 |
Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors. |
Novartis |
12/19/08 |
| 18621524 |
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. |
GSK |
12/19/08 |
| 17636914 |
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB. |
University of California at Berkeley |
12/18/08 |
| 18922779 |
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. |
Burnham Institute for Medical Research |
12/18/08 |
| 18973288 |
Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis |
Wyeth Research |
12/18/08 |
| 15911271 |
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides. |
Pfizer |
12/18/08 |
| 18942826 |
Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases. |
University of Oxford |
12/18/08 |
| 17349580 |
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. |
Harvard Medical School |
12/18/08 |
| 18579385 |
Carbonic anhydrase inhibitors: Inhibition of mammalian isoforms I?XIV with a series of substituted phenols including paracetamol and salicylic acid. |
Universita degli Studi di Firenze |
12/17/08 |
| 18983140 |
Discovery of Boronic Acids as Novel and Potent Inhibitors of Fatty Acid Amide Hydrolase. |
University of Oxford |
12/17/08 |
| 18956862 |
Fragment-Based Design of Small Molecule X-Linked Inhibitor of Apoptosis Protein Inhibitors. |
Burnham Institute for Medical Research |
12/17/08 |
| 17600705 |
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics. |
GSK |
12/17/08 |
| 18844338 |
Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach. |
Johnson & Johnson Pharmaceutical |
12/16/08 |
| 18227510 |
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. |
Harvard Medical School |
12/15/08 |
| 17981461 |
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR. |
GSK |
12/08/08 |
| 18006306 |
Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode. |
GSK |
12/06/08 |
| 18374572 |
Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
Universita degli Studi di Firenze |
12/06/08 |
| 17197177 |
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors. |
Bristol-Myers Squibb Company |
12/06/08 |
| 18790643 |
A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis. |
University of Wisconsin-Milwaukee |
12/05/08 |
| 18819811 |
Carbonic anhydrase inhibitors: synthesis and inhibition studies against mammalian isoforms I-XV with a series of 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides. |
Istanbul University |
12/05/08 |
| 18855374 |
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). |
Saarland University |
12/05/08 |
| 17723305 |
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides. |
Incyte Corporation |
12/05/08 |
| 17846131 |
Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray crystallography. |
University of California at San Francisco |
12/05/08 |
| 18834108 |
Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from cryptosporidium. |
University of Connecticut at Storrs |
12/05/08 |
| 18571418 |
Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors. |
University of Canterbury |
12/05/08 |
| 18812261 |
The molecular interactions of buspirone analogues with the serotonin transporter. |
National Medicines Institute |
12/05/08 |
| 17540562 |
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors. |
Bristol-Myers Squibb Company |
12/04/08 |
| 18640037 |
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
Universita degli Studi di Firenze |
12/03/08 |
| 18287029 |
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. |
Plexxikon |
11/24/08 |
| 18307303 |
Discovery of selective aminothiazole aurora kinase inhibitors. |
Novartis |
11/24/08 |
| 18672868 |
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
Saarland University |
11/24/08 |
| 18585390 |
The molecular structure of epoxide hydrolase B from Mycobacterium tuberculosis and its complex with a urea-based inhibitor. |
University of Alberta |
11/24/08 |
| 15655528 |
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. |
University of Nottingham |
11/24/08 |
| 18783200 |
Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors. |
Wyeth Research |
11/23/08 |
| 18473434 |
Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold. |
Cancer Research UK Centre for Cancer Therapeutics |
11/23/08 |
| 18676143 |
Potent and selective pyrazole-based inhibitors of B-Raf kinase. |
Array BioPharma |
11/23/08 |
| 18793847 |
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors. |
Sunesis Pharmaceuticals |
11/22/08 |
| 18834107 |
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. |
The Scripps Research Institute |
11/22/08 |
| 18842034 |
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. |
GSK |
11/22/08 |
| 18925736 |
Structure-activity relationship studies of phenanthridine-based Bcl-XL inhibitors. |
A*STAR |
11/22/08 |
| 18921992 |
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications. |
Pfizer |
11/21/08 |
| 18855373 |
Structure-based virtual screening and biological evaluation of Mycobacterium tuberculosis adenosine 5'-phosphosulfate reductase inhibitors. |
The Scripps Research Institute |
11/21/08 |
| 18783202 |
Identification of BRAF inhibitors through in silico screening. |
University of Pennsylvania |
11/11/08 |
| 17567585 |
X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. |
Jacobus Pharmaceutical Company |
11/11/08 |
| 18440229 |
2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors. |
IRBM/Merck |
11/10/08 |
| 18778048 |
Discovery of novel nitrobenzothiazole inhibitors for Mycobacterium tuberculosis ATP phosphoribosyl transferase (HisG) through virtual screening. |
Yale University |
11/10/08 |
| 18800762 |
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation. |
National Taiwan University |
11/10/08 |
| 18434142 |
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines. |
AstraZeneca |
11/10/08 |
| 18783211 |
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands. |
Monash University |
11/10/08 |
| 17884497 |
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors. |
GlaxoSmithKline |
11/10/08 |
| 18378451 |
Design and campaign synthesis of pyridine-based histone deacetylase inhibitors. |
AstraZeneca |
11/09/08 |
| 18811140 |
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase. |
Merck Research Laboratories |
11/09/08 |
| 18378449 |
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors. |
AstraZeneca |
11/08/08 |
| 18763751 |
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. |
Merck Research Laboratories |
11/08/08 |
| 18783203 |
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies. |
Purdue University |
11/08/08 |
| 18370373 |
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo. |
IRBM/Merck |
10/28/08 |
| 18759424 |
Adamantyl-substituted retinoid-derived molecules that interact with the orphan nuclear receptor small heterodimer partner: effects of replacing the 1-adamantyl or hydroxyl group on inhibition of cancer cell growth, induction of cancer cell apoptosis, and inhibition of SRC homology 2 domain-containi |
Burnham Institute for Medical Research |
10/28/08 |
| 17685602 |
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction. |
TargeGen Inc. |
10/28/08 |
| 18754655 |
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain. |
Novartis |
10/28/08 |
| 18308563 |
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
IRBM/Merck |
10/28/08 |
| 17095227 |
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma. |
Pfizer |
10/27/08 |
| 17655330 |
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity. |
Abbott Laboratories |
10/27/08 |
| 17172449 |
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. |
TargeGen Inc. |
10/27/08 |
| 17049248 |
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors. |
Astellas Pharma Inc. |
10/27/08 |
| 17040210 |
BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. |
University of Dundee |
10/26/08 |
| 17601739 |
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. |
Astellas Pharma Inc. |
10/26/08 |
| 18754654 |
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
Piramed Pharma |
10/26/08 |
| 18800763 |
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. |
GlaxoSmithKline |
10/25/08 |
| 17098432 |
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). |
Paradigm Pharmaceuticals |
10/14/08 |
| 16951187 |
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. |
Amgen |
10/13/08 |
| 18343106 |
Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase. |
Texas A&M University |
10/13/08 |
| 18717581 |
Design, synthesis, and evaluation of novel organophosphorus inhibitors of bacterial ureases. |
Wroclaw University of Technology |
10/13/08 |
| 16632359 |
Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists. |
Pfizer |
10/13/08 |
| 18318466 |
Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors. |
Bryn Mawr College |
10/13/08 |
| 17620441 |
Novel antagonists of the thioesterase domain of human fatty acid synthase. |
Burnham Institute for Medical Research |
10/13/08 |
| 18729351 |
Potent cationic inhibitors of West Nile virus NS2B/NS3 protease with serum stability, cell permeability and antiviral activity. |
University of Queensland |
10/13/08 |
| 18456494 |
Synthesis and structure based optimization of novel Akt inhibitors. |
Pfizer |
10/13/08 |
| 18790636 |
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors. |
Sunesis Pharmaceuticals |
10/12/08 |
| 18714982 |
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
Cephalon |
10/12/08 |
| 18249537 |
Development of pyridopyrimidines as potent Akt1/2 inhibitors. |
Merck Research Laboratories |
10/11/08 |
| 18294842 |
Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors. |
Merck Research Laboratories |
10/11/08 |
| 18763753 |
Design, synthesis, and biological evaluation of potent c-Met inhibitors. |
Amgen |
10/10/08 |
| 16420054 |
Structure-activity study of brassinin derivatives as indoleamine 2,3-dioxygenase inhibitors. |
Bryn Mawr College |
10/10/08 |
| 18702480 |
2-Thiazolylimino/heteroarylimino-5-arylidene-4-thiazolidinones as new agents with SHP-2 inhibitory action. |
Aristotle University |
09/30/08 |
| 18630890 |
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability. |
Genentech |
09/30/08 |
| 18637666 |
Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. |
UniVersity of Belgrade |
09/30/08 |
| 18710209 |
Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid. |
Eberhard-Karls-University Tuebingen |
09/30/08 |
| 18686942 |
Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase. |
The Scripps Research Institute |
09/29/08 |
| 16731764 |
CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. |
Celera Genomics |
09/29/08 |
| 12725862 |
Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. |
University of North Carolina at Chapel Hill |
09/29/08 |
| 18570366 |
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor. |
MethylGene Inc. |
09/29/08 |
| 18646745 |
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases. |
AstraZeneca |
09/29/08 |
| 18656911 |
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design. |
Astex |
09/29/08 |
| 18665584 |
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase. |
Bryn Mawr College |
09/29/08 |
| 18680359 |
Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. |
Moffitt Cancer Center |
09/28/08 |
| 18690678 |
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships. |
Vertex |
09/28/08 |
| 18710210 |
Synthesis of novel beta-lactone inhibitors of fatty acid synthase. |
The Burnham Institute for Medical Research |
09/28/08 |
| 18540668 |
Thermodynamic and structure guided design of statin based inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase. |
Pfizer |
09/17/08 |
| 18426196 |
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. |
Amgen |
09/16/08 |
| 18434145 |
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
MethylGene Inc. |
09/16/08 |
| 18553959 |
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). |
Amgen |
09/16/08 |
| 18690676 |
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. |
Bristol-Myers Squibb Company |
09/16/08 |
| 18494463 |
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
University of Illinois at Chicago |
09/15/08 |
| 17095214 |
Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors. |
AstraZeneca |
09/15/08 |
| 18522386 |
Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum. |
University of Texas Southwestern Medical Center at Dallas |
09/15/08 |
| 18590272 |
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity. |
University of Bath |
09/14/08 |
| 17580845 |
Dual aromatase-steroid sulfatase inhibitors. |
University of Bath |
09/14/08 |
| 18588282 |
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
Johnson & Johnson Pharmaceutical |
09/14/08 |
| 18578471 |
Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors. |
AstraZeneca |
09/14/08 |
| 18394906 |
Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase. |
Berlex Biosciences |
09/14/08 |
| 16458511 |
Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series. |
Bristol-Myers Squibb Company |
08/04/08 |
| 16439123 |
Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP. |
Merck Research Laboratories |
08/04/08 |
| 18636690 |
Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids. |
University of Tennessee Health Science Center |
08/04/08 |
| 17498954 |
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors. |
Kalypsys, Inc. |
08/04/08 |
| 15634023 |
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. |
Institut Claudius Regaud |
08/04/08 |
| 17804234 |
5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2). |
Wyeth Research |
08/03/08 |
| 16275085 |
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors. |
Wyeth Research |
08/03/08 |
| 17239589 |
Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists. |
Pharmacopeia Drug Discovery Inc. |
08/02/08 |
| 16844380 |
Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors. |
ENSCMu |
08/02/08 |
| 16603356 |
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP. |
Merck Research Laboratories |
08/01/08 |
| 17766111 |
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP. |
Merck Research Laboratories |
08/01/08 |
| 16821772 |
Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. |
Curacyte Chemistry GmbH |
07/30/08 |
| 18343126 |
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development. |
University of Tokyo |
07/26/08 |
| 17994679 |
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. |
Merck Research Laboratories |
07/26/08 |
| 18266314 |
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5. |
Institut de Biologie Structurale |
07/26/08 |
| 18522384 |
Chemically induced dimerization of human nonpancreatic secretory phospholipase A2 by bis-indole derivatives. |
Peking University |
07/25/08 |
| 17993277 |
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines. |
Universite Paris 7-Denis Diderot |
07/25/08 |
| 17850059 |
N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase. |
Montana State University |
07/25/08 |
| 17636949 |
Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors. |
University of Tennessee Health Science Center |
07/25/08 |
| 18459730 |
Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. |
University of Namur |
07/24/08 |
| 15743201 |
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents. |
Quorex Pharmaceuticals Inc. |
07/24/08 |
| 17466326 |
Crystal structures of multidrug binding protein TtgR in complex with antibiotics and plant antimicrobials. |
Imperial College London |
07/23/08 |
| 18247549 |
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes. |
Schering-Plough Research Institute |
07/23/08 |
| 16407274 |
Effector-repressor interactions, binding of a single effector molecule to the operator-bound TtgR homodimer mediates derepression. |
Consejo Superior de Investigaciones Cientificas |
07/23/08 |
| 14718605 |
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. |
Wyeth Research |
07/23/08 |
| 17606376 |
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket. |
Wyeth Research |
07/23/08 |
| 17296300 |
Amphipathic benzoic acid derivatives: synthesis and binding in the hydrophobic tunnel of the zinc deacetylase LpxC. |
University of San Francisco |
07/12/08 |
| 17293454 |
An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists. |
The Scripps Research Institute |
07/12/08 |
| 16451085 |
Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands. |
Pfizer |
07/12/08 |
| 17951059 |
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors. |
The Scripps Research Institute |
07/12/08 |
| 12139467 |
Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. |
Guilford Pharmaceuticals, Inc. |
07/12/08 |
| 17417831 |
A refined pharmacophore identifies potent 4-amino-7-chloroquinoline-based inhibitors of the botulinum neurotoxin serotype A metalloprotease. |
National Cancer Institute at Frederick |
07/11/08 |
| 17636950 |
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors. |
University of Mississippi |
07/11/08 |
| 18507367 |
Flavonoids for controlling starch digestion: structural requirements for inhibiting human alpha-amylase. |
Nestle Research Center |
07/11/08 |
| 15117937 |
Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity. |
University of Bristol |
07/11/08 |
| 16597152 |
Identification of a potent botulinum neurotoxin a protease inhibitor using in situ lead identification chemistry. |
The Scripps Research Institute |
07/11/08 |
| 17761421 |
Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening. |
Waseda University |
07/11/08 |
| 17116397 |
Substrate specificity analysis and inhibitor design of homoisocitrate dehydrogenase. |
Tokyo Institute of Technology |
07/11/08 |
| 18086528 |
Thiahomoisocitrate: a highly potent inhibitor of homoisocitrate dehydrogenase involved in the alpha-aminoadipate pathway. |
Tokyo Institute of Technology |
07/11/08 |
| 16844375 |
Binding mode of new (thio)hydantoin inhibitors of fatty acid amide hydrolase: comparison with two original compounds, OL-92 and JP104. |
FUNDP |
07/08/08 |
| 18565342 |
Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors. |
Gilead Sciences Inc. |
07/08/08 |
| 18343121 |
Structure-based virtual screening against SARS-3CL(pro) to identify novel non-peptidic hits. |
University of Mississippi |
07/08/08 |
| 17559203 |
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
The Scripps Research Institute |
06/30/08 |
| 14709046 |
A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization. |
Fujisawa Pharmaceutical Co., Ltd. |
06/29/08 |
| 15598563 |
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate. |
Mitsubishi Pharma Corporation |
06/29/08 |
| 10639181 |
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors. |
Vanderbilt University School of Medicine |
06/29/08 |
| 15947036 |
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. |
Vrije Universiteit Amsterdam |
06/29/08 |
| 15901723 |
NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors. |
India Central Drug Research Institute |
06/29/08 |
| 17557328 |
NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor. |
India Central Drug Research Institute |
06/29/08 |
| 18517260 |
Naturally Occurring Pentacyclic Triterpenes as Inhibitors of Glycogen Phosphorylase: Synthesis, Structure-Activity Relationships, and X-ray Crystallographic Studies. |
China Pharmaceutical University |
06/29/08 |
| 18027904 |
New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. |
University of Rome La Sapienza |
06/29/08 |
| 12643924 |
Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors. |
Fujisawa Pharmaceutical Co., Ltd. |
06/29/08 |
| 18507366 |
Synthesis and Biological Evaluation of d-Amino Acid Oxidase Inhibitors. |
MGI Pharma |
06/29/08 |
| 17052908 |
Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum. |
University of Cape Town |
06/29/08 |
| 17941623 |
Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. |
St. Jude Research Hospital |
06/28/08 |
| 15139750 |
Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors. |
Fujisawa Pharmaceutical Co., Ltd. |
06/20/08 |
| 15239652 |
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors. |
Fujisawa Pharmaceutical Co., Ltd. |
06/20/08 |
| 17154493 |
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species. |
IRBM-MRL |
06/15/08 |
| 18217703 |
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors. |
IRBM-MRL |
06/15/08 |
| 17824681 |
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones. |
IRBM-MRL |
06/15/08 |
| 15828829 |
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. |
University of Mississippi |
06/15/08 |
| 17378546 |
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. |
St. Jude Research Hospital |
06/15/08 |
| 16316253 |
Strong solute-solute dispersive interactions in a protein-ligand complex. |
University of Leeds |
06/15/08 |
| 15355974 |
Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening. |
The Scripps Research Institute |
06/14/08 |
| 15725032 |
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry. |
University of North Carolina at Chapel Hill |
06/14/08 |
| 17393456 |
Identification of novel fragment compounds targeted against the pY pocket of v-Src SH2 by computational and NMR screening and thermodynamic evaluation. |
University College London |
06/14/08 |
| 18042718 |
Protein protein interaction inhibition (2P2I) combining high throughput and virtual screening: Application to the HIV-1 Nef protein. |
CNRS |
06/14/08 |
| 17324932 |
Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase. |
The Scripps Research Institute |
06/14/08 |
| 16935302 |
Thermodynamic penalty arising from burial of a ligand polar group within a hydrophobic pocket of a protein receptor. |
University of Leeds |
06/14/08 |
| 18433114 |
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists. |
VU University Amsterdam |
06/13/08 |
| 14722321 |
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. |
Johnson & Johnson Pharmaceutical |
06/13/08 |
| 16990005 |
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands. |
Johnson & Johnson Pharmaceutical |
06/13/08 |
| 17656360 |
Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides. |
Michigan State University |
06/13/08 |
| 16821792 |
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase. |
Friedrich Alexander University Erlangen |
05/31/08 |
| 15857113 |
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma. |
GSK |
05/31/08 |
| 16307879 |
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma. |
GSK |
05/31/08 |
| 16509583 |
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases. |
University of Alberta |
05/31/08 |
| 18419108 |
2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice. |
Biovitrum AB |
05/30/08 |
| 17240142 |
Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor. |
GSK |
05/30/08 |
| 18412327 |
Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors. |
University of Notre Dame |
05/30/08 |
| 17500511 |
Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists. |
Johnson & Johnson Pharmaceutical |
05/30/08 |
| 17556356 |
Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism. |
Novartis |
05/29/08 |
| 17154495 |
Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1. |
University of Southampton |
05/29/08 |
| 17602602 |
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes. |
Research Triangle Institute |
05/29/08 |
| 18311898 |
Computer-aided discovery of anti-inflammatory thiazolidinones with dual cyclooxygenase/lipoxygenase inhibition. |
Aristotle University |
05/28/08 |
| 17656086 |
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment. |
Bristol-Myers Squibb Company |
05/28/08 |
| 15713402 |
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase. |
Bristol-Myers Squibb Company |
05/28/08 |
| 18412317 |
(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A Rationally Designed Orally Efficacious 3-Hydroxy-3-methylglutaryl Coenzyme-A Reductase Inhibitor with Reduced Myotoxicity Potential. |
Bristol-Myers Squibb Company |
05/10/08 |
| 18393401 |
Design and Synthesis of 2- and 3-Substituted-3-phenylpropyl Analogs of 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: Role of Amino, Fluoro, Hydroxyl, Methoxyl, Methyl, Methylene, and Oxo Substituents on Affinity f |
National Taiwan University |
05/10/08 |
| 16190743 |
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3. |
Merck Research Laboratories |
05/10/08 |
| 17092714 |
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties. |
Merck Research Laboratories |
05/10/08 |
| 18416543 |
Aza-peptidyl Michael Acceptors. A New Class of Potent and Selective Inhibitors of Asparaginyl Endopeptidases (Legumains) from Evolutionarily Diverse Pathogens. |
Georgia Institute of Technology |
05/09/08 |
| 18251493 |
Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases. |
Industrial Research Limited |
05/09/08 |
| 18173229 |
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. |
University of California at San Francisco |
05/09/08 |
| 17228885 |
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation. |
Universita di Pisa |
05/09/08 |
| 17676727 |
Targeting plague virulence factors: a combined machine learning method and multiple conformational virtual screening for the discovery of Yersinia protein kinase A inhibitors. |
The Rockefeller University |
05/09/08 |
| 17228867 |
Optimization of monocarboxylate transporter 1 blockers through analysis and modulation of atropisomer interconversion properties. |
AstraZeneca |
05/08/08 |
| 16455256 |
Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds. |
AstraZeneca |
05/08/08 |
| 14718923 |
Structural basis for dipeptide amide isoform-selective inhibition of neuronal nitric oxide synthase. |
University of California at Irvine |
05/08/08 |
| 18393489 |
Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine a. |
University of British Columbia |
05/08/08 |
| 17985858 |
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1. |
Georgetown University Medical Center |
04/30/08 |
| 17973363 |
Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
04/30/08 |
| 17614291 |
Hydroxyethylene isosteres of selective neuronal nitric oxide synthase inhibitors. |
Northwestern University |
04/30/08 |
| 18173230 |
Inhibition of adenosine deaminase by analogues of adenosine and inosine, incorporating a common heterocyclic base, 4(7)-amino-6(5)H-imidazo[4,5-d]pyridazin-7(4)one. |
University of Maryland Baltimore County |
04/30/08 |
| 15916444 |
Inhibition of herpes simplex virus thymidine kinases by 2-phenylamino-6-oxopurines and related compounds: structure-activity relationships and antiherpetic activity in vivo. |
GLSynthesis Inc. |
04/30/08 |
| 17715908 |
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles. |
Wyeth Research |
04/30/08 |
| 17425297 |
Structure-based design and synthesis of N(omega)-nitro-L-arginine-containing peptidomimetics as selective inhibitors of neuronal nitric oxide synthase. Displacement of the heme structural water. |
Northwestern University |
04/30/08 |
| 18232652 |
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists. |
Istituto Superiore di Sanita |
04/30/08 |
| 17292610 |
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist. |
University of Tokyo |
04/29/08 |
| 17477519 |
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors. |
University of Liverpool |
04/29/08 |
| 17274610 |
Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy. |
Bayer HealthCare Pharmaceuticals Corporation |
04/29/08 |
| 17920884 |
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation. |
Amgen |
04/29/08 |
| 18341273 |
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design. |
AstraZeneca |
04/20/08 |
| 17074800 |
Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound. |
Microbiotix |
04/19/08 |
| 18318467 |
Arginine binding motifs: design and synthesis of galactose-derived arginine tweezers as galectin-3 inhibitors. |
Lund University |
04/19/08 |
| 17215127 |
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism. |
University of North Carolina at Chapel Hill |
04/19/08 |
| 18318469 |
Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases. |
Merck Serono |
04/19/08 |
| 17685603 |
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5. |
University di Perugia |
04/19/08 |
| 12538898 |
Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species. |
GSK |
04/19/08 |
| 16242339 |
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors. |
Lund University |
04/19/08 |
| 11906289 |
Toward an optimal joint recognition of the S1' subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP). |
CNRS |
04/19/08 |
| 18324760 |
Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2. |
University of Athens |
04/18/08 |
| 18314943 |
Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-beta Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-beta Receptor Type I Inhibitor as Antitumor Agent. |
Lilly Research Laboratories |
04/18/08 |
| 17256834 |
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
Abbott Laboratories |
04/18/08 |
| 12358520 |
Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. |
Millennium Pharmaceuticals |
04/18/08 |
| 18269230 |
Derivatives of 4-Amino-6-hydroxy-2-mercaptopyrimidine as Novel, Potent, and Selective A3 Adenosine Receptor Antagonists. |
Universita di Napoli |
04/08/08 |
| 18189347 |
Structure-activity relationships of C6-uridine derivatives targeting plasmodia orotidine monophosphate decarboxylase. |
Toronto General Research Institute |
04/08/08 |
| 18307293 |
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships. |
Neuroscience |
04/07/08 |
| 18311908 |
Characterization of Type II Ligands in CYP2C9 and CYP3A4. |
AstraZeneca |
04/07/08 |
| 17948978 |
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist. |
Wyeth Research |
04/07/08 |
| 18311894 |
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity. |
Abbott Laboratories |
04/07/08 |
| 17649988 |
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. |
Universita degli Studi di Bari |
04/07/08 |
| 18293908 |
Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. |
Sapienza Universitàadi Roma |
04/07/08 |
| 18307292 |
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 1. Structure-Activity Relationships and Optimization of Heterocyclic Substituents. |
Neuroscience |
04/06/08 |
| 17927164 |
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors. |
University of Arizona at Tucson |
04/06/08 |
| 16686530 |
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
University of Arizona at Tucson |
04/06/08 |
| 17539621 |
Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis. |
Universita degli Studi |
04/06/08 |
| 18260617 |
3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases. |
Abbott Laboratories |
03/29/08 |
| 18266313 |
A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists. |
University of Arizona at Tucson |
03/29/08 |
| 17516639 |
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
University of Arizona at Tucson |
03/29/08 |
| 18269228 |
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. |
Wyeth Research |
03/29/08 |
| 18288792 |
2-Aryloxy-4-alkylaminopyridines: Discovery of Novel Corticotropin-Releasing Factor 1 Antagonists. |
Pfizer |
03/28/08 |
| 18020435 |
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. |
Vernalis (R&D) Ltd |
03/28/08 |
| 17709247 |
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors. |
Amgen |
03/28/08 |
| 17402721 |
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling. |
Bristol-Myers Squibb Company |
03/28/08 |
| 18260618 |
Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes. |
Bristol-Myers Squibb Company |
03/28/08 |
| 18278855 |
Exploring inhibitor binding at the s' subsites of cathepsin L. |
National Research Council Canada |
03/28/08 |
| 17697781 |
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. |
Amgen |
03/28/08 |
| 18260619 |
Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists. |
Pfizer |
03/28/08 |
| 18072727 |
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors. |
Duquesne University |
03/17/08 |
| 18197612 |
Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90. |
Wyeth Research |
03/17/08 |
| 17488003 |
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
Biogen Idec |
03/17/08 |
| 18215016 |
Design, Synthesis, Evaluation, and Crystallographic-Based Structural Studies of HIV-1 Protease Inhibitors with Reduced Response to the V82A Mutation. |
Universidad de Santiago de Compostela |
03/16/08 |
| 18072718 |
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors. |
Novartis Pharmaceuticals |
03/16/08 |
| 12825935 |
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands. |
Novartis Pharmaceuticals |
03/16/08 |
| 16420067 |
Orally active purine-based inhibitors of the heat shock protein 90. |
Conforma Therapeutics Corporation |
03/16/08 |
| 15658851 |
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands. |
Novartis Pharmaceuticals |
03/16/08 |
| 18072721 |
Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia. |
Pfizer |
03/16/08 |
| 11906280 |
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes. |
Novartis Pharmaceuticals |
03/16/08 |
| 18183944 |
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. |
Abbott Laboratories |
03/16/08 |
| 16913725 |
7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors. |
Conforma Therapeutics Corporation |
03/14/08 |
| 17583335 |
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists. |
Abbott Laboratories |
02/28/08 |
| 15689158 |
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties. |
Abbott Laboratories |
02/28/08 |
| 17585749 |
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides. |
Amgen |
02/28/08 |
| 17585750 |
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
Amgen |
02/28/08 |
| 17585751 |
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
Amgen |
02/28/08 |
| 16580202 |
Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. |
GSK |
02/24/08 |
| 15203132 |
Discovery of small molecule antagonists of TRPV1. |
GSK |
02/24/08 |
| 17660385 |
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. |
Abbott Laboratories |
02/23/08 |
| 17507218 |
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model. |
Abbott Laboratories |
02/22/08 |
| 16621571 |
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists. |
Abbott Laboratories |
02/22/08 |
| 17629487 |
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. |
Seoul National University |
02/11/08 |
| 18154266 |
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects. |
University of Central Florida College of Medicine |
02/11/08 |
| 17513110 |
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'. |
University of Michigan |
02/11/08 |
| 16107141 |
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
GlaxoSmithKline |
02/11/08 |
| 12639546 |
Identification of a high-affinity phosphopeptide inhibitor of Stat3. |
The University of Texas at Houston |
02/11/08 |
| 11985463 |
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
GlaxoSmithKline |
02/11/08 |
| 16220982 |
Investigation of the binding determinants of phosphopeptides targeted to the SRC homology 2 domain of the signal transducer and activator of transcription 3. Development of a high-affinity peptide inhibitor. |
The University of Texas at Houston |
02/11/08 |
| 11300870 |
Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha. |
Dartmouth College |
02/11/08 |
| 17463090 |
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. |
University of Central Florida College of Medicine |
02/11/08 |
| 18072720 |
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. |
Seoul National University |
02/11/08 |
| 17336521 |
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains. |
Yale University |
02/10/08 |
| 17665897 |
N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
GNF |
01/16/08 |
| 16250633 |
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats. |
Lilly Research Laboratories |
01/15/08 |
| 17804226 |
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies. |
Lilly Research Laboratories |
01/15/08 |
| 17391964 |
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators. |
Wyeth Research |
01/15/08 |
| 16302809 |
Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. |
Rheinische Friedrich-Wilhelms-Universitat Bonn |
01/15/08 |
| 17408953 |
Beta-substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core. |
Merck Frosst Centre for Therapeutic Research |
01/07/08 |
| 12904076 |
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K. |
Merck Frosst Centre for Therapeutic Research |
01/06/08 |
| 17485205 |
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold. |
Lilly Research Laboratories |
01/06/08 |
| 17614275 |
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification. |
Lilly Research Laboratories |
01/06/08 |
| 17662603 |
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring. |
Lilly Research Laboratories |
01/06/08 |
| 16480867 |
Dipeptide nitrile inhibitors of cathepsin K. |
Novartis Pharmaceuticals |
01/06/08 |
| 17963370 |
Discovery of 5-Substituted-6-chlorouracils as Efficient Inhibitors of Human Thymidine Phosphorylase. |
Gilead Sciences Inc. |
01/06/08 |
| 17256925 |
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. |
Novartis Pharmaceuticals |
01/05/08 |
| 17157021 |
Acyclic, orally bioavailable ketone-based cathepsin K inhibitors. |
GSK |
01/05/08 |
| 17034120 |
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. |
Lilly Research Laboratories |
01/05/08 |
| 11262083 |
Cyclic ketone inhibitors of the cysteine protease cathepsin K. |
GSK |
01/05/08 |
| 16509577 |
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors. |
GSK |
01/05/08 |
| 16610787 |
Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators. |
Bristol-Myers Squibb Company |
01/05/08 |
| 16451072 |
Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K. |
Merck Frosst Centre for Therapeutic Research |
01/04/08 |
| 16337119 |
Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase. |
Academy of Sciences of the Czech Republic |
01/04/08 |
| 17034119 |
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
Wyeth Research |
01/04/08 |
| 16302795 |
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
Merck Frosst Centre for Therapeutic Research |
01/04/08 |
| 17649976 |
Biochemical and biophysical characterization of inhibitor binding to caspase-3 reveals induced asymmetry. |
Wyeth Research |
12/19/07 |
| 15723556 |
Use of binding enthalpy to drive an allosteric transition. |
University of Maryland at College Park |
12/19/07 |
| 16412634 |
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl. |
GNF |
12/18/07 |
| 16876407 |
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors. |
GNF |
12/18/07 |
| 17469812 |
Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode. |
University of California at Berkeley |
12/18/07 |
| 16183279 |
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1. |
GNF |
12/18/07 |
| 16413777 |
Identification of a potent and selective non-basic cathepsin K inhibitor. |
Merck Frosst Centre for Therapeutic Research |
12/18/07 |
| 17034136 |
Identification of selective, nonpeptidic nitrile inhibitors of cathepsin s using the substrate activity screening method. |
University of California at Berkeley |
12/18/07 |
| 16876402 |
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers. |
GNF |
12/18/07 |
| 17382545 |
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S. |
GNF |
12/18/07 |
| 16446091 |
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3. |
GNF |
12/18/07 |
| 17590332 |
The identification of potent, selective, and bioavailable cathepsin S inhibitors. |
Merck Frosst Centre for Therapeutic Research |
12/18/07 |
| 16610800 |
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists. |
Abbott Laboratories |
12/10/07 |
| 17489582 |
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
University of Illinois at Chicago |
12/10/07 |
| 16854051 |
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists. |
Abbott Laboratories |
12/10/07 |
| 17426033 |
Glyoxylate and pyruvate are antagonistic effectors of the Escherichia coli IclR transcriptional regulator. |
Banting and Best Department of Medical Research |
12/10/07 |
| 17941625 |
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. |
MethylGene Inc |
12/10/07 |
| 17887776 |
Structural and thermodynamic consequences of 1-(4-chlorophenyl)imidazole binding to cytochrome P450 2B4. |
University of Texas Medical Branch |
12/10/07 |
| 17927165 |
Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations. |
CNRS |
12/10/07 |
| 17585753 |
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419). |
Bristol-Myers Squibb Company |
12/09/07 |
| 17765263 |
Nucleation of an allosteric response via ligand-induced loop folding. |
University of Maryland at College Park |
12/09/07 |
| 17228884 |
Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains. |
University of Illinois at Urbana |
12/09/07 |
| 17149865 |
Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta. |
Ghent University |
12/09/07 |
| 17948975 |
Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase. |
Pfizer |
12/09/07 |
| 17958343 |
Probing Binding Requirements of Type I and Type II Isoforms of Inosine Monophosphate Dehydrogenase with Adenine-Modified Nicotinamide Adenine Dinucleotide Analogues. |
University of Minnesota at Twin Citiies |
12/02/07 |
| 17941624 |
Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors. |
Wyeth Research |
11/25/07 |
| 17902635 |
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series. |
CNRS |
11/25/07 |
| 17915852 |
Structures of Human Monoamine Oxidase B Complexes with Selective Noncovalent Inhibitors: Safinamide and Coumarin Analogs. |
University of Pavia |
11/25/07 |
| 16078847 |
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. |
Abbott Laboratories |
11/24/07 |
| 16828557 |
Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. |
University of Tennessee Health Science Center |
11/24/07 |
| 15115388 |
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity. |
Merck Research Laboratories |
11/24/07 |
| 17467988 |
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments. |
Merck Research Laboratories |
11/24/07 |
| 17910428 |
Synthesis and monoamine oxidase inhibitory activity of new pyridazine-, pyrimidine- and 1,2,4-triazine-containing tricyclic derivatives. |
University of Bari |
11/24/07 |
| 17929798 |
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. |
Nagoya City University |
11/23/07 |
| 17948981 |
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin. |
University of California at Davis |
11/23/07 |
| 17915848 |
Small molecule inhibitors of integrin alpha2beta1. |
University of Pennsylvania |
11/23/07 |
| 17958342 |
The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor. |
University of Southampton |
11/23/07 |
| 16439135 |
Chlamydocin analogs bearing carbonyl group as possible ligand toward zinc atom in histone deacetylases. |
Kyushu Institute of Technology |
11/19/07 |
| 17914785 |
Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa. |
Bristol-Myers Squibb Company |
11/11/07 |
| 15857115 |
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. |
Karo Bio AB |
11/11/07 |
| 17154490 |
Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. |
Karo Bio AB |
11/11/07 |
| 15177471 |
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta. |
Bristol-Myers Squibb |
11/11/07 |
| 14521405 |
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants. |
Bristol-Myers Squibb Company |
11/10/07 |
| 8770901 |
Structure-function relationship of the inhibition of the 3,5,3'-triiodothyronine binding to the alpha1- and beta1-thyroid hormone receptor by amiodarone analogs. |
University of Amsterdam |
11/10/07 |
| 12699376 |
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
Karo Bio AB |
11/10/07 |
| 17254783 |
Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. |
Karo Bio AB |
11/10/07 |
| 17543524 |
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
Karo Bio AB |
11/10/07 |
| 17918822 |
Inhibitors of the Interaction of a Thyroid Hormone Receptor and Coactivators: Preliminary Structure-Activity Relationships. |
St. Jude Research Hospital |
11/09/07 |
| 9651155 |
Pharmacophores incorporating numerous excluded volumes defined by X-ray crystallographic structure in three-dimensional database searching: application to the thyroid hormone receptor. |
Karo Bio AB |
11/08/07 |
| 17174550 |
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues. |
Bristol-Myers Squibb Company |
11/08/07 |
| 16303304 |
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta. |
Karo Bio AB |
11/08/07 |
| 16451071 |
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1). |
Duquesne University |
11/05/07 |
| 16954316 |
Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays. |
National Center for Genetic Engineering and Biotechnology at Thailand |
11/05/07 |
| 12704428 |
Insights into antifolate resistance from malarial DHFR-TS structures. |
Mahidol University |
11/05/07 |
| 16279780 |
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolate reductase and thymidylate synthase and a |
Duquesne University |
11/05/07 |
| 17681466 |
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists. |
Boehringer Ingelheim Pharmaceuticals Inc. |
11/04/07 |
| 17004711 |
Antibacterial agent discovery using thymidylate synthase biolibrary screening. |
UNIMORE |
11/03/07 |
| 16204883 |
The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition. |
University of California at San Francisco |
11/01/07 |
| 16420057 |
(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist. |
Astellas Pharma Inc. |
10/28/07 |
| 9514878 |
Discovery of nonsteroidal androgens. |
University of Tennessee at Memphis |
10/28/07 |
| 10691684 |
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring. |
University of Tennessee at Memphis |
10/26/07 |
| 14761201 |
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators. |
University of Tennessee at Memphis |
10/26/07 |
| 16386422 |
Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands. |
Boehringer Ingelheim Pharmaceuticals Inc. |
10/25/07 |
| 17269758 |
Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis. |
Dartmouth College |
10/17/07 |
| 17827006 |
N(4)-Phenyl modifications of N(2)-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease. |
NIH |
10/17/07 |
| 17267219 |
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. |
Ligand Pharmaceuticals Inc. |
10/17/07 |
| 17705362 |
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma. |
Ligand Pharmaceuticals Inc. |
10/17/07 |
| 17034117 |
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator. |
Ligand Pharmaceuticals Inc. |
10/16/07 |
| 17257838 |
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones. |
Ligand Pharmaceuticals Inc. |
10/16/07 |
| 17764936 |
Pyrazole inhibitors of HMG-CoA reductase: An attempt to dramatically reduce synthetic complexity through minimal analog re-design. |
Pfizer |
10/16/07 |
| 17005826 |
Structure-activity relationships of Bacillus cereus and Bacillus anthracis dihydrofolate reductase: toward the identification of new potent drug leads. |
University of Connecticut at Storrs |
10/16/07 |
| 17887661 |
Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators. |
Ligand Pharmaceuticals Inc. |
10/16/07 |
| 17670938 |
Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease. |
NIH |
10/16/07 |
| 16919960 |
Alpha-1-C-octyl-1-deoxynojirimycin as a pharmacological chaperone for Gaucher disease. |
Hokuriku University |
10/08/07 |
| 17552508 |
Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates. |
Duquesne University |
10/08/07 |
| 17552509 |
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
10/08/07 |
| 17560788 |
Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase. |
Pfizer |
10/08/07 |
| 17201413 |
Isofagomine- and 2,5-anhydro-2,5-imino-D-glucitol-based glucocerebrosidase pharmacological chaperones for Gaucher disease intervention. |
The Scripps Research Institute |
10/08/07 |
| 17824679 |
Novel 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamide Transition State Peptidomimetics Are Potent and Orally Active Inhibitors of Human Renin. |
Novartis Pharmaceuticals |
10/08/07 |
| 17824680 |
Structural Modification of the P2' Position of 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The Discovery of Aliskiren, a Potent Nonpeptide Human Renin Inhibitor Active after Once Daily Dosing in Marmosets. |
Novartis Pharmaceuticals |
10/08/07 |
| 15974594 |
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain. |
Harvard Medical School |
10/07/07 |
| 17181141 |
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold. |
Bristol-Myers Squibb Company |
10/07/07 |
| 17439112 |
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. |
Ligand Pharmaceuticals Inc. |
10/07/07 |
| 12731874 |
Thermodynamic characterization of the binding of nucleotides to glycyl-tRNA synthetase. |
Medical College of Ohio |
10/01/07 |
| 17125251 |
A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region. |
University of Prince Edward Island |
09/30/07 |
| 17696333 |
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase. |
University of Tennessee at Knoxville |
09/30/07 |
| 15561838 |
Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim. |
Oklahoma State University at Stillwater |
09/30/07 |
| 15895686 |
Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase. |
CREFSIP |
09/30/07 |
| 14623005 |
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria. |
GSK |
09/30/07 |
| 782880 |
Influence of side-chain structure of aliphatic amino acids on binding to isoleucyl-tRNA synthetase from Escherichia coli MRE 600. |
Gesellschaft Fur Molekularbiolische Forschung mbH |
09/30/07 |
| 11520201 |
X-Ray crystal structures of Candida albicans dihydrofolate reductase: high resolution ternary complexes in which the dihydronicotinamide moiety of NADPH is displaced by an inhibitor. |
GSK |
09/30/07 |
| 11567092 |
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors. |
GSK |
09/29/07 |
| 15837314 |
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase. |
GSK |
09/29/07 |
| 15582453 |
Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs. |
CREFSIP |
09/29/07 |
| 17049867 |
Synthesis of beta-ketophosphonate analogs of glutamyl and glutaminyl adenylate, and selective inhibition of the corresponding bacterial aminoacyl-tRNA synthetases. |
CREFSIP |
09/29/07 |
| 17113558 |
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors. |
Pfizer |
09/19/07 |
| 17482464 |
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors. |
Pfizer |
09/19/07 |
| 15755665 |
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors. |
Pfizer |
09/19/07 |
| 16480874 |
Ketopiperazine-based renin inhibitors: optimization of the "C" ring. |
Pfizer |
09/19/07 |
| 17574423 |
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. |
Pfizer |
09/19/07 |
| 10903938 |
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin. |
Novartis Pharmaceuticals |
09/19/07 |
| 15582452 |
The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors. |
Pfizer |
09/19/07 |
| 14998322 |
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate. |
Morphochem AG |
09/18/07 |
| 17444623 |
Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization. |
Schering-Plough Research Institute |
09/18/07 |
| 17114291 |
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression. |
Johns Hopkins University |
09/18/07 |
| 17120228 |
Serendipitous discovery of novel bacterial methionine aminopeptidase inhibitors. |
The Procter & Gamble Pharmaceuticals |
09/18/07 |
| 17194595 |
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists. |
Daiichi Pharmaceutical |
09/18/07 |
| 16377201 |
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists. |
Daiichi Pharmaceutical |
09/18/07 |
| 12946343 |
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors. |
Morphochem AG |
09/18/07 |
| 17132624 |
Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors. |
Johnson & Johnson Pharmaceutical |
09/11/07 |
| 17696416 |
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors. |
Amgen |
09/11/07 |
| 17676829 |
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors. |
GSK |
09/11/07 |
| 15801825 |
Enantiospecificity of glutamate carboxypeptidase II inhibition. |
Guilford |
09/11/07 |
| 17132625 |
Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies. |
Johnson & Johnson Pharmaceutical |
09/11/07 |
| 16686531 |
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain. |
MGI Pharma |
09/11/07 |
| 17685503 |
2-Amino-3,4-dihydroquinazolines as Inhibitors of BACE-1 (beta-Site APP Cleaving Enzyme): Use of Structure Based Design to Convert a Micromolar Hit into a Nanomolar Lead. |
Johnson & Johnson Pharmaceutical |
09/10/07 |
| 17696512 |
Design and Synthesis of HIV-1 Protease Inhibitors Incorporating Oxazolidinones as P2/P2' Ligands in Pseudosymmetric Dipeptide Isosteres. |
University of Massachusetts Medical School |
09/10/07 |
| 16884310 |
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. |
Amgen |
09/10/07 |
| 17276681 |
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties. |
Amgen |
09/09/07 |
| 17636946 |
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. |
GSK |
09/01/07 |
| 17338508 |
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
GSK |
08/31/07 |
| 17567119 |
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II. |
NCI-FCRDC |
08/31/07 |
| 17663538 |
Synthesis, Biological Activity, and Crystal Structure of Potent Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase That Retain Activity against Mutant Forms of the Enzyme. |
NCI-FCRDC |
08/31/07 |
| 16134930 |
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo. |
GSK |
08/30/07 |
| 14996743 |
Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin. |
The University of Birmingham |
08/30/07 |
| 16632353 |
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. |
Abbott Laboratories |
08/30/07 |
| 16789740 |
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding. |
Abbott Laboratories |
08/30/07 |
| 14633714 |
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2. |
Abbott Laboratories |
08/30/07 |
| 17350258 |
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids. |
Abbott Laboratories |
08/29/07 |
| 12223444 |
A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity. |
CHUL |
08/18/07 |
| 11027132 |
Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa. |
Berlex |
08/18/07 |
| 11342132 |
Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors. |
Boehringer Ingelheim Pharma KG |
08/18/07 |
| 17166832 |
Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase. |
CHUL |
08/18/07 |
| 17227710 |
Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa. |
Berlex |
08/18/07 |
| 17350841 |
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV. |
Merck Research Laboratories |
08/17/07 |
| 12657282 |
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
Abbott Laboratories |
08/17/07 |
| 17168540 |
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs. |
Genentech |
08/17/07 |
| 17336535 |
Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP. |
Princeton University |
08/17/07 |
| 10417407 |
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin. |
Berlex |
08/16/07 |
| 17035017 |
2,6-Quinolinyl derivatives as potent VLA-4 antagonists. |
UCB |
08/09/07 |
| 16455247 |
Pyridone derivatives as potent and selective VLA-4 integrin antagonists. |
GlaxoSmithKline |
08/09/07 |
| 17570665 |
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping. |
Vernalis (R&D) Ltd |
08/08/07 |
| 16931004 |
Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists. |
GlaxoSmithKline |
08/08/07 |
| 16495061 |
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent. |
Johnson & Johnson Pharmaceutical |
08/08/07 |
| 12244092 |
Structural basis for Chk1 inhibition by UCN-01. |
GlaxoSmithKline |
08/08/07 |
| 17536795 |
Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors(1). |
Berlex Biosciences |
08/08/07 |
| 16750629 |
p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones. |
Merck Research Laboratories |
08/08/07 |
| 17531483 |
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. |
Berlex Biosciences |
08/02/07 |
| 17544272 |
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. |
Berlex Biosciences |
08/02/07 |
| 14962382 |
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1. |
University of Dundee |
08/02/07 |
| 15772071 |
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. |
Berlex Biosciences |
08/02/07 |
| 12892559 |
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition. |
University of Dundee |
08/02/07 |
| 16112583 |
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
08/01/07 |
| 16644221 |
Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers. |
Abbott Laboratories |
08/01/07 |
| 16603355 |
Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity. |
Abbott Laboratories |
08/01/07 |
| 17041919 |
Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells. |
University of California Davis |
08/01/07 |
| 16722660 |
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
08/01/07 |
| 17034121 |
Acylguanidines as small-molecule beta-secretase inhibitors. |
Wyeth Research |
07/25/07 |
| 16690314 |
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres. |
Merck Research Laboratories |
07/25/07 |
| 17112725 |
Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites. |
Merck Research Laboratories |
07/25/07 |
| 14695829 |
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase. |
Elan Pharmaceuticals |
07/25/07 |
| 17258463 |
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt. |
Abbott Laboratories |
07/25/07 |
| 17257835 |
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation. |
Merck Research Laboratories |
07/25/07 |
| 17034118 |
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model. |
Merck Research Laboratories |
07/25/07 |
| 16821787 |
Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays. |
Universite de la Mediterranee |
07/25/07 |
| 11520194 |
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase). |
University of Illinois at Chicago |
07/25/07 |
| 15466206 |
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. |
Bayer Pharmaceuticals Corporation |
07/18/07 |
| 14971907 |
Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
Universita degli Studi di Firenze |
07/18/07 |
| 16134934 |
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex. |
IGBMC |
07/18/07 |
| 16190759 |
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners. |
Pfizer |
07/17/07 |
| 16289938 |
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification. |
Vernalis (R&D) Ltd |
07/17/07 |
| 15734645 |
Structural basis for the highly selective inhibition of MMP-13. |
Aventis Pharma Deutschland GmbH |
07/17/07 |
| 17523610 |
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension. |
Abbott Laboratories |
07/17/07 |
| 16945533 |
p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design. |
Merck Research Laboratories |
07/17/07 |
| 17107793 |
Evaluating scoring functions for docking and designing beta-secretase inhibitors. |
Merck Research Laboratories |
07/10/07 |
| 16950396 |
Quantitative evaluation of each catalytic subsite of cathepsin B for inhibitory activity based on inhibitory activity-binding mode relationship of epoxysuccinyl inhibitors by X-ray crystal structure analyses of complexes. |
Osaka University of Pharmaceutical Sciences |
07/03/07 |
| 16190753 |
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase. |
Bristol-Myers Squibb Company |
07/02/07 |
| 12773033 |
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one. |
Pfizer |
07/02/07 |
| 15857120 |
Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. |
The Institute for Diabetes Discovery |
07/02/07 |
| 16337231 |
High-resolution crystal structure of aldose reductase complexed with the novel sulfonyl-pyridazinone inhibitor exhibiting an alternative active site anchoring group. |
University of Marburg |
07/02/07 |
| 16759861 |
Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development. |
Pfizer |
07/02/07 |
| 15588077 |
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1). |
Merck Research Laboratories |
07/02/07 |
| 17451234 |
Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery. |
Astex |
06/17/07 |
| 16620080 |
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors. |
Purdue University |
06/10/07 |
| 17432843 |
Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands. |
Purdue University |
06/10/07 |
| 17163639 |
High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis. |
SUNY Stony Brook |
06/10/07 |
| 16451048 |
Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1. |
Sunesis |
06/09/07 |
| 9468142 |
Design of potent selective zinc-mediated serine protease inhibitors. |
Arris |
06/09/07 |
| 17441705 |
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. |
Takeda Pharmaceutical Company Ltd. |
06/09/07 |
| 17418233 |
Evidence for a novel binding site conformer of aldose reductase in ligand-bound state. |
University of Marburg |
06/09/07 |
| 15044733 |
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain. |
University of Copenhagen |
06/09/07 |
| 17368668 |
Structural and thermodynamic study on aldose reductase: nitro-substituted inhibitors with strong enthalpic binding contribution. |
University of Marburg |
06/09/07 |
| 15582402 |
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase). |
University of Illinois at Chicago |
06/08/07 |
| 11196150 |
Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. |
Janssen Research Foundation |
06/04/07 |
| 10926521 |
Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design. |
Max-Planck-Institut fuer Biochemie |
06/04/07 |
| 17458947 |
De Novo Parallel Design, Synthesis and Evaluation of Inhibitors against the Reverse Transcriptase of Human Immunodeficiency Virus Type-1 and Drug-Resi |
Bar Ilan University |
06/04/07 |
| 15916422 |
Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
University of Washington at Seattle |
06/04/07 |
| 16406782 |
Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase. |
Cornell University |
06/03/07 |
| 17447747 |
Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines. |
Pfizer |
06/03/07 |
| 16236496 |
The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. |
University of Leeds |
06/03/07 |
| 17451235 |
Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design. |
Astex |
06/01/07 |
| 16246558 |
Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors. |
4SC AG |
05/31/07 |
| 16759099 |
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. |
Abbott Laboratories |
05/28/07 |
| 16263281 |
Conformationally biased P3 amide replacements of beta-secretase inhibitors. |
Merck Research Laboratories |
05/28/07 |
| 17107797 |
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. |
Abbott Laboratories |
05/28/07 |
| 17149856 |
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1). |
Merck Research Laboratories |
05/28/07 |
| 15566281 |
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases. |
Merck Research Laboratories |
05/28/07 |
| 16854060 |
Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE). |
Universite de Montreal at Succursale Centre-Ville |
05/28/07 |
| 16078837 |
Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics. |
Universite de Montreal at Succursale Centre-Ville |
05/28/07 |
| 12954329 |
The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity. |
Merck Research Laboratories |
05/28/07 |
| 15261268 |
Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents. |
Aventis Pharma Deutschland GmbH |
05/27/07 |
| 15261269 |
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand. |
Aventis Pharma Deutschland GmbH |
05/27/07 |
| 16527482 |
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors. |
Abbott Laboratories |
05/27/07 |
| 16854050 |
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors. |
Abbott Laboratories |
05/24/07 |
| 17315856 |
Application of fragment screening by X-ray crystallography to beta-secretase. |
Astex |
05/15/07 |
| 17337342 |
Affinity-based ranking of ligands for DPP-4 from mixtures. |
Merck Research Laboratories |
05/14/07 |
| 17315857 |
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase. |
Astex |
05/14/07 |
| 17300163 |
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase. |
Elan Pharmaceuticals |
05/14/07 |
| 16509574 |
Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase. |
Roche Palo Alto LLC |
05/14/07 |
| 17300186 |
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors. |
Vertex |
05/14/07 |
| 16249081 |
Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex. |
Lilly S.A. |
05/14/07 |
| 17256833 |
New pyrrole inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity. |
Universita di Roma La Sapienza |
05/14/07 |
| 17291750 |
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes. |
Merck Research Laboratories |
05/14/07 |
| 12749891 |
Potent, selective inhibitors of protein tyrosine phosphatase 1B. |
Abbott Laboratories |
05/14/07 |
| 17034137 |
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis. |
University of California at San Francisco |
05/14/07 |
| 14561090 |
Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase. |
Roche Palo Alto LLC |
05/11/07 |
| 17276063 |
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit. |
Abbott Laboratories |
05/08/07 |
| 16213716 |
3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone. |
Vernalis (R&D) Ltd |
05/07/07 |
| 15012994 |
Benzimidazolone p38 inhibitors. |
Pfizer |
05/07/07 |
| 14592490 |
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors. |
Merck Research Laboratories |
05/07/07 |
| 15147193 |
Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity. |
Merck Research Laboratories |
05/07/07 |
| 17239592 |
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site. |
Lilly Research Laboratories |
05/07/07 |
| 16480261 |
Dual binding mode of a novel series of DHODH inhibitors. |
4SC AG |
05/07/07 |
| 15795226 |
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. |
University of Texas Southwestern Medical Center |
05/07/07 |
| 16735511 |
Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development. |
University of North Carolina at Chapel Hill |
05/07/07 |
| 15974572 |
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. |
Vernalis (R&D) Ltd |
05/07/07 |
| 17352464 |
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors. |
Abbott Laboratories |
05/07/07 |
| 16134941 |
Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase. |
Pfizer |
05/07/07 |
| 17367123 |
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors. |
Abbott Laboratories |
05/04/07 |
| 15217611 |
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms. |
Vernalis (R&D) Ltd |
05/04/07 |
| 16202589 |
Structure-based discovery of a new class of Hsp90 inhibitors. |
Vernalis (R&D) Ltd |
05/04/07 |
| 12897767 |
Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity. |
Merck Research Laboratories |
05/01/07 |
| 9753691 |
Structural basis of inhibitor selectivity in MAP kinases. |
University of Texas Southwestern Medical Center at Dallas |
05/01/07 |
| 11090628 |
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. |
MRC |
05/01/07 |
| 17275837 |
A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera. |
Astex |
04/30/07 |
| 15664853 |
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. |
Merck Research Laboratories |
04/30/07 |
| 17343373 |
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
Griffith University |
04/30/07 |
| 15686884 |
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. |
Merck Research Laboratories |
04/30/07 |
| 16678413 |
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase. |
Abbott Laboratories |
04/30/07 |
| 16249095 |
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B. |
UK Centre for Cancer Therapeutics |
04/30/07 |
| 16413780 |
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
Abbott Laboratories |
04/30/07 |
| 15801821 |
Virtual docking approaches to protein kinase B inhibition. |
The Burnham Institute |
04/30/07 |
| 16403626 |
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
Abbott Laboratories |
04/26/07 |
| 17253679 |
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase. |
Amgen |
04/17/07 |
| 15996097 |
Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases. |
Merck Research Laboratories |
04/17/07 |
| 17253678 |
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. |
Amgen |
04/17/07 |
| 16413783 |
Factor VIIa inhibitors: gaining selectivity within the trypsin family. |
Celera |
04/17/07 |
| 11896401 |
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. |
Boehringer Ingelheim Pharmaceuticals Inc. |
04/17/07 |
| 16621549 |
Novel 5-azaindole factor VIIa inhibitors. |
Celera |
04/17/07 |
| 17276055 |
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. |
GlaxoSmithKline |
04/17/07 |
| 14561087 |
Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
Boehringer Ingelheim Pharmaceuticals Inc. |
04/17/07 |
| 14561086 |
Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals Inc. |
04/17/07 |
| 15857116 |
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities. |
Abbott Laboratories |
04/10/07 |
| 15055996 |
Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening. |
AstraZeneca |
04/10/07 |
| 15084132 |
Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
Canadian Institutes of Health Research |
04/09/07 |
| 17228859 |
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors. |
Pfizer |
04/09/07 |
| 16574416 |
Identification of chemically diverse Chk1 inhibitors by receptor-based virtual screening. |
Vernalis (R&D) Ltd |
04/09/07 |
| 15576036 |
Structural basis for the activity of drugs that inhibit phosphodiesterases. |
Plexxikon |
04/09/07 |
| 15974586 |
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity. |
Vernalis (R&D) Ltd |
04/09/07 |
| 15685167 |
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design. |
Plexxikon |
04/08/07 |
| 16517596 |
A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity. |
Duke University Medical Center |
04/03/07 |
| 15632123 |
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo. |
Genentech |
04/03/07 |
| 16446090 |
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors. |
Abbott Laboratories |
04/03/07 |
| 17228860 |
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase. |
University of Leeds |
04/02/07 |
| 12954058 |
Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. |
Pharmacia Corporation |
04/02/07 |
| 14561089 |
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors. |
Pharmacia Corporation |
04/02/07 |
| 14613321 |
Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors. |
Aventis Pharma |
04/02/07 |
| 16242328 |
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors. |
Abbott Laboratories |
04/02/07 |
| 13678408 |
Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors. |
Pharmacia Corporation |
04/02/07 |
| 17154503 |
Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes. |
Abbott Laboratories |
03/27/07 |
| 9822558 |
(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
Schering-Plough Research Institute |
03/26/07 |
| 15715490 |
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors. |
Purdue Pharma LP |
03/26/07 |
| 16759100 |
A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. |
Pfizer |
03/26/07 |
| 15911281 |
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity. |
Abbott Laboratories |
03/26/07 |
| 15808463 |
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
Abbott Laboratories |
03/26/07 |
| 15522303 |
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA). |
Celera |
03/26/07 |
| 16539372 |
Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. |
University of North Carolina at Chapel Hill |
03/26/07 |
| 17266195 |
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a. |
Cephalon |
03/13/07 |
| 16949284 |
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors. |
Johnson & Johnson Pharmaceutical |
03/13/07 |
| 12742021 |
Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors. |
Celera |
03/12/07 |
| 16806920 |
Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48. |
Wyeth Research |
03/12/07 |
| 16681368 |
Structure-guided design of peptide-based tryptase inhibitors. |
Celera |
03/12/07 |
| 17097290 |
Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors. |
Incyte Corporation |
03/11/07 |
| 16303309 |
Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors. |
Wyeth Research |
03/11/07 |
| 10966741 |
Crystal structures of human factor Xa complexed with potent inhibitors. |
Aventis Pharma |
03/06/07 |
| 17201404 |
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity. |
GlaxoSmithKline |
03/06/07 |
| 11731301 |
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets. |
Axys Pharmaceutical |
03/06/07 |
| 15771442 |
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design. |
Johnson & Johnson Pharmaceutical |
03/06/07 |
| 14695818 |
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
University of Queensland |
03/06/07 |
| 10779411 |
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator. |
Axys Pharmaceutical |
03/06/07 |
| 17201405 |
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors. |
GlaxoSmithKline |
03/05/07 |
| 12036349 |
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. |
Merck Research Laboratories |
02/27/07 |
| 12747781 |
Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B. |
Abbott Laboratories |
02/27/07 |
| 16699172 |
Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity. |
German Cancer Research Center |
02/27/07 |
| 16249185 |
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity. |
Vertex Pharmaceuticals |
02/27/07 |
| 11292354 |
A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site. |
Axys Pharmaceuticals Corporation |
02/26/07 |
| 12670229 |
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy. |
Abbott Laboratories |
02/26/07 |
| 14592481 |
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B. |
Abbott Laboratories |
02/25/07 |
| 15482920 |
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors. |
Abbott Laboratories |
02/25/07 |
| 1611188 |
A variant serum cholinesterase and a confirmed point mutation at Gly-365 to Arg found in a patient with liver cirrhosis. |
Hyogo College of Medicine |
02/20/07 |
| 15379553 |
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease. |
University of Florida College of Medicine |
02/20/07 |
| 16634628 |
Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir. |
Johnson & Johnson Pharmaceutical |
02/19/07 |
| 12061878 |
Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa. |
Aventis Pharma Deutschland GmbH |
02/19/07 |
| 16277992 |
Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. |
Georgia State University |
02/19/07 |
| 10387041 |
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease. |
University of Queensland |
02/19/07 |
| 16913714 |
Structure-Based Design of Novel HIV-1 Protease Inhibitors To Combat Drug Resistance. |
Purdue University |
02/19/07 |
| 17110106 |
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation. |
Abbott Laboratories |
02/13/07 |
| 16460932 |
Discovery of novel heterocyclic factor VIIa inhibitors. |
Celera |
02/13/07 |
| 17010607 |
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors. |
Abbott Laboratories |
02/13/07 |
| 17266194 |
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1. |
Amgen |
02/12/07 |
| 16407290 |
Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase. |
Merck Frosst Center for Therapeutic Research |
02/12/07 |
| 16904316 |
New, potent P1/P2-morpholinone-based HIV-protease inhibitors. |
GlaxoSmithKline |
02/12/07 |
| 15125936 |
Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand. |
Aventis Pharma Deutschland GmbH |
02/12/07 |
| 15857135 |
Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions. |
Aventis Pharma Deutschland GmbH |
02/12/07 |
| 16916797 |
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics. |
Incyte Corporation |
02/11/07 |
| 11341829 |
Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action. |
Pharmacia Corporation |
02/06/07 |
| 15664864 |
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. |
F. Hoffmann-La Roche Ltd. |
02/05/07 |
| 16621574 |
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity. |
F. Hoffmann-La Roche Ltd. |
02/05/07 |
| 16046538 |
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. |
Ambit, Inc. |
02/05/07 |
| 17149883 |
Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. |
Rheinische Friedrich-Wilhelms-Universitat Bonn |
02/05/07 |
| 16213138 |
Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors. |
F. Hoffmann-La Roche Ltd. |
02/05/07 |
| 14516196 |
The structural basis for the selectivity of benzotriazole inhibitors of PTP1B. |
Merck Research Laboratories |
02/05/07 |
| 14981513 |
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. |
Vertex Pharmaceuticals (Europe) Limited |
02/05/07 |
| 17055272 |
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Merck Research Laboratories |
01/29/07 |
| 16386905 |
1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors. |
Procter & Gamble Pharmaceuticals |
01/29/07 |
| 14736242 |
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors. |
Globe Pharmaceutical R and Abbott Laboratories |
01/29/07 |
| 12767917 |
Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates. |
St. Maryamppound39s Hospital |
01/29/07 |
| 17028182 |
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B. |
Incyte Corporation |
01/29/07 |
| 16539374 |
Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors. |
Universita di Napoli Federico II |
01/29/07 |
| 16970397 |
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites. |
Yale University |
01/23/07 |
| 17154512 |
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase i |
Bristol-Myers Squibb Company |
01/22/07 |
| 17181177 |
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic. |
University of Michigan |
01/22/07 |
| 15317454 |
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. |
Abbott Laboratories |
01/22/07 |
| 15658855 |
Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation. |
Astex |
01/22/07 |
| 10479289 |
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization. |
Rhone-Poulenc Rorer |
01/22/07 |
| 15664855 |
Non-peptidic small molecule inhibitors of XIAP. |
Abbott Laboratories |
01/20/07 |
| 15293984 |
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site. |
University of Michigan |
01/20/07 |
| 17125255 |
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
Universite Montpellier II |
01/15/07 |
| 15453828 |
Crystal structure of human carbonic anhydrase II at 1.95 A resolution in complex with 667-coumate, a novel anti-cancer agent. |
University of Bath |
01/15/07 |
| 16962773 |
Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein. |
University of Michigan |
01/15/07 |
| 9258358 |
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits. |
Novartis Pharmaceuticals |
01/15/07 |
| 15865431 |
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors. |
University of Bath |
01/15/07 |
| 15664859 |
Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics. |
University of Michigan |
01/15/07 |
| 12166932 |
Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
University of Marburg |
01/15/07 |
| 14736236 |
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
University of Marburg |
01/15/07 |
| 17125279 |
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. |
Nerviano Medical Sciences |
01/09/07 |
| 16942016 |
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase. |
University of Kansas |
01/09/07 |
| 16161994 |
Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. |
Bayer HealthCare AG |
01/09/07 |
| 17181170 |
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. |
Wyeth Research |
01/09/07 |
| 17181160 |
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants. |
Daiichi Asubio Medical Research Laboratories LLC (DAIAMED) |
01/08/07 |
| 17064072 |
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". |
Griffith University |
01/07/07 |
| 15657054 |
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002. |
Vertex Pharmaceuticals |
01/03/07 |
| 17149864 |
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
University of Massachusetts Medical School |
01/02/07 |
| 16870435 |
Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
01/02/07 |
| 15454208 |
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa. |
Bristol-Myers Squibb Company |
01/02/07 |
| 15582405 |
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
01/01/07 |
| 15454209 |
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa. |
Bristol-Myers Squibb Company |
01/01/07 |
| 16434195 |
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
01/01/07 |
| 16730984 |
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12/19/06 |
| 16480269 |
Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors. |
Astex |
12/19/06 |
| 17064063 |
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Abbott Laboratories |
12/19/06 |
| 15771420 |
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12/19/06 |
| 17034148 |
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes. |
Abbott Laboratories |
12/19/06 |
| 16963264 |
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12/19/06 |
| 12593649 |
Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket. |
Aventis Pharma |
12/19/06 |
| 16682200 |
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa. |
Bristol-Myers Squibb Company |
12/19/06 |
| 17064073 |
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. |
Hoffmann-La Roche Inc. |
12/18/06 |
| 16536518 |
Enthalpy versus entropy-driven binding of bisphosphonates to farnesyl diphosphate synthase. |
University of Illinois at Urbana-Champaign |
12/13/06 |
| 16697194 |
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors. |
GlaxoSmithKline |
12/12/06 |
| 16451065 |
Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles. |
Schering-Plough Research Institute |
12/12/06 |
| 16982190 |
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs. |
GlaxoSmithKline |
12/12/06 |
| 16982192 |
Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors. |
GlaxoSmithKline |
12/11/06 |
| 15999990 |
Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography. |
Aventis Pharma |
12/11/06 |
| 16337122 |
SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors. |
AstraZeneca |
12/11/06 |
| 16506782 |
Ultrahigh resolution crystal structures of human carbonic anhydrases I and II complexed with "two-prong" inhibitors reveal the molecular basis of high affinity. |
University of Pennsylvania |
12/11/06 |
| 15771423 |
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases. |
University of Antwerp |
12/10/06 |
| 17004721 |
Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor |
Schering-Plough Research Institute |
12/05/06 |
| 16979339 |
Synthesis and biological study of 4-aminopyrimidine-5-carboxaldehyde oximes as antiproliferative VEGFR-2 inhibitors. |
Johnson & Johnson Pharmaceutical |
12/05/06 |
| 17125252 |
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization. |
Human BioMolecular Research Institute |
12/05/06 |
| 17064066 |
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
AstraZeneca |
12/04/06 |
| 12694187 |
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors. |
Uppsala University |
12/04/06 |
| 15837308 |
Oximinoarylsulfonamides as potent HIV protease inhibitors. |
Abbott Laboratories |
12/03/06 |
| 16978863 |
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6. |
Merck Research Laboratories |
11/27/06 |
| 15771455 |
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties. |
Universita degli Studi di Firenze |
11/27/06 |
| 16942020 |
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. |
University of Oxford |
11/27/06 |
| 15664838 |
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8. |
National Health Research Institutes |
11/27/06 |
| 16581245 |
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors. |
National Health Research Institutes |
11/27/06 |
| 16290148 |
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors. |
Nerviano Medical Sciences |
11/26/06 |
| 16616492 |
A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor. |
Nerviano Medical Sciences |
11/26/06 |
| 16451058 |
Structural Insight into the Stereoselective Inhibition of MMP-8 by Enantiomeric Sulfonamide Phosphonates. |
Istituto di Cristallografia |
11/26/06 |
| 11738604 |
Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1). |
Pfizer |
11/26/06 |
| 15887974 |
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives. |
Universidad Central de Venezuela |
11/26/06 |
| 15828847 |
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. |
Nerviano Medical Sciences |
11/25/06 |
| 15537346 |
Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1. |
University of Oxford |
11/24/06 |
| 11591522 |
Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide. |
Pfizer |
11/24/06 |
| 16913712 |
Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening. |
Montana State University |
11/14/06 |
| 16870442 |
Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease. |
Hawaii Biotech Inc. |
11/14/06 |
| 17064068 |
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
Palacky University |
11/13/06 |
| 15837304 |
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole. |
Merck Research Laboratories |
11/13/06 |
| 11572683 |
Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II. |
University of Pennsylvania |
11/13/06 |
| 14871097 |
Thermodynamics of binding of 2-methoxy-3-isopropylpyrazine and 2-methoxy-3-isobutylpyrazine to the major urinary protein. |
University of Leeds |
11/12/06 |
| 16445284 |
Global effects of the energetics of coenzyme binding: NADPH controls the protein interaction properties of human cytochrome P450 reductase. |
University of Leicester |
11/07/06 |
| 16376077 |
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
11/07/06 |
| 9865942 |
Structural analysis of inhibitor binding to human carbonic anhydrase II. |
University of Pennsylvania |
11/07/06 |
| 16220987 |
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy. |
Pfizer |
11/07/06 |
| 16046120 |
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
11/06/06 |
| 12217351 |
Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zinc binding functions. |
Universita degli Studi di Firenze |
11/06/06 |
| 15634010 |
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants. |
Max-Planck-Institut fuer Biochemie |
10/31/06 |
| 16392822 |
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. |
National Health Research Institutes |
10/30/06 |
| 10732980 |
Protease inhibitors. Part 8: synthesis of potent Clostridium histolyticum collagenase inhibitors incorporating sulfonylated L-alanine hydroxamate moieties. |
Universita degli Studi di Firenze |
10/30/06 |
| 14998327 |
Structure-based optimization of novel azepane derivatives as PKB inhibitors. |
Roche Diagnostics GmbH |
10/30/06 |
| 16302800 |
Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase. |
Oxford University |
10/29/06 |
| 16913695 |
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819). |
Istituto di Cristallografia |
10/24/06 |
| 16134940 |
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II. |
Istituto di Biostrutture e Bioimmagini-CNR |
10/23/06 |
| 16768443 |
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors. |
Abbott Laboratories |
10/23/06 |
| 16919457 |
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
10/23/06 |
| 12747790 |
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
University of Agricultural Sciences and Veterinary Medicine |
10/22/06 |
| 15006388 |
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents. |
Hoffmann-La Roche Inc. |
10/17/06 |
| 16033281 |
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
10/17/06 |
| 15163180 |
Sultam hydroxamates as novel matrix metalloproteinase inhibitors. |
Bristol-Myers Squibb Company |
10/17/06 |
| 16376544 |
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors. |
Santhera Pharmaceuticals |
10/17/06 |
| 11020282 |
Carbonic anhydrase and matrix metalloproteinase inhibitors: sulfonylated amino acid hydroxamates with MMP inhibitory properties act as efficient inhibitors of CA isozymes I, II, and IV, and N-hydroxysulfonamides inhibit both these zinc enzymes. |
Universita degli Studi |
10/15/06 |
| 15863311 |
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
10/14/06 |
| 11170642 |
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717. |
Lawrence Berkeley National Laboratory |
10/10/06 |
| 16325401 |
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. |
Vernalis (R&D) Ltd |
10/10/06 |
| 15686876 |
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2. |
Vernalis (R&D) Ltd |
10/03/06 |
| 10882008 |
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit. |
Alcon Research, Ltd. |
10/02/06 |
| 11831900 |
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV. |
University of Pennsylvania |
10/02/06 |
| 12816539 |
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). |
University of Padova |
09/26/06 |
| 16759091 |
Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies. |
National Tsing Hua University |
09/26/06 |
| 15974598 |
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease. |
National Taiwan University |
09/26/06 |
| 12419810 |
Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight. |
University of Padova |
09/26/06 |
| 15994085 |
Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic alpha,beta-unsaturated esters. |
National Taiwan University |
09/26/06 |
| 16913704 |
Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease. |
National Defense Medical Center |
09/26/06 |
| 16332437 |
Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors. |
Merck Research Laboratories |
09/25/06 |
| 15908206 |
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
09/24/06 |
| 16884309 |
Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor. |
TaiGen Biotechnology Co. |
09/23/06 |
| 15710600 |
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors. |
Emory University |
09/19/06 |
| 16759103 |
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Merck Research Laboratories |
09/18/06 |
| 16942027 |
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
Istituto di Biostrutture e Bioimmagini-CNR |
09/18/06 |
| 16759095 |
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors. |
Abbott Laboratories |
09/18/06 |
| 16640335 |
Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
University of Namur |
09/18/06 |
| 15634008 |
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Merck Research Laboratories |
09/17/06 |
| 16236500 |
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors. |
Johnson & Johnson Pharmaceutical |
09/17/06 |
| 12773032 |
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy. |
University of Bologna |
09/12/06 |
| 12166941 |
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
National Institutes of Health |
09/12/06 |
| 16366596 |
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis. |
University of Pavia |
09/12/06 |
| 15689148 |
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors. |
Shanghai Institute of Materia Medica |
09/12/06 |
| 16302824 |
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors. |
Kochi Medical School |
09/12/06 |
| 15537349 |
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues. |
University of Bologna |
09/12/06 |
| 15027867 |
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues. |
Emory University |
09/12/06 |
| 11708910 |
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action. |
National Institutes of Health |
09/12/06 |
| 16279769 |
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives. |
Universita degli Studi di Roma La Sapienza |
09/12/06 |
| 9767635 |
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives. |
University of Bologna |
09/05/06 |
| 16539401 |
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. |
Kochi Medical School |
09/04/06 |
| 15985434 |
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. |
Chinese Academy of Sciences |
09/04/06 |
| 11052800 |
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. |
Institut Curie |
09/03/06 |
| 16183021 |
Methylxanthine drugs are chitinase inhibitors: investigation of inhibition and binding modes. |
University of Dundee |
08/30/06 |
| 15664516 |
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases. |
University of Dundee |
08/30/06 |
| 12431053 |
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease. |
Teva Pharmaceutical Industries |
08/28/06 |
| 15026054 |
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. |
CNRS |
08/26/06 |
| 9632370 |
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine. |
University of North Carolina at Chapel Hill |
08/22/06 |
| 11689067 |
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives. |
University of Bologna |
08/21/06 |
| 15974596 |
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation. |
University of Bologna |
08/21/06 |
| 14741294 |
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors. |
Merck Frosst Canada & Co. |
08/15/06 |
| 16570913 |
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
National Institutes of Health |
08/13/06 |
| 11888271 |
Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine. |
Weizmann Institute of Science |
08/13/06 |
| 10891109 |
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2. |
Palacky University |
08/12/06 |
| 15115390 |
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis. |
Merck Research Laboratories |
08/12/06 |
| 16616489 |
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors. |
Institut Curie |
08/12/06 |
| 12196020 |
X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement. |
Weizmann Institute of Science |
08/12/06 |
| 15771413 |
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors. |
Universitat de Barcelona |
08/08/06 |
| 16023344 |
Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors. |
Merck Frosst Canada & Co. |
08/07/06 |
| 12798321 |
Nicotinyl aspartyl ketones as inhibitors of caspase-3. |
Merck Frosst Canada & Co. |
08/07/06 |
| 16722663 |
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites. |
Universita di Siena |
08/05/06 |
| 11563919 |
A structure-based design approach to the development of novel, reversible AChE inhibitors. |
Syngenta |
08/01/06 |
| 12517147 |
Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity. |
Weizmann Institute of Science |
08/01/06 |
| 10218828 |
Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis. |
Hong Kong University of Science and Technology |
08/01/06 |
| 11425559 |
Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. |
Universita degli Studi di Siena |
08/01/06 |
| 15658850 |
Rational approach to discover multipotent anti-Alzheimer drugs. |
University of Bologna |
08/01/06 |
| 15563167 |
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design. |
Weizmann Institute of Science |
08/01/06 |
| 10632067 |
Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities. |
Hong Kong University of Science and Technology |
07/31/06 |
| 8798583 |
Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. Steps toward novel drugs for treating Alzheimer's disease. |
Mayo Foundation for Medical Education and Research |
07/31/06 |
| 9839013 |
Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series. |
CNRS |
07/31/06 |
| 16302804 |
N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies. |
Washington University School of Medicine |
07/25/06 |
| 15916416 |
Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. |
Chemical Diversity Research Institute |
07/25/06 |
| 15780618 |
1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors. |
Chemical Diversity Research Institute |
07/18/06 |
| 16509578 |
Design, synthesis, and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors. |
Shanghai Institutes for Biological Sciences |
07/04/06 |
| 11384246 |
Potent and selective nonpeptide inhibitors of caspases 3 and 7. |
GlaxoSmithKline |
07/04/06 |
| 15857150 |
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT. |
Universita di Messina |
06/29/06 |
| 15743206 |
Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach. |
Burnham Institute |
06/29/06 |
| 14552750 |
Identification of potent and novel small-molecule inhibitors of caspase-3. |
Sunesis Pharmaceuticals |
06/29/06 |
| 14741280 |
Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives. |
Boehringer Ingelheim (Canada) Ltd. |
06/29/06 |
| 16644213 |
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids. |
Ambrilia Biopharma Inc. |
06/28/06 |
| 12659774 |
Synthesis of potent oxindole CDK2 inhibitors. |
Hoffmann-La Roche Inc. |
06/28/06 |
| 12852944 |
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors. |
Hoffmann-La Roche Inc. |
06/27/06 |
| 15012993 |
A new series of potent oxindole inhibitors of CDK2. |
Hoffmann-La Roche Inc. |
06/27/06 |
| 10794700 |
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase. |
Universitat des Saarlandes |
06/20/06 |
| 11708928 |
Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C(19) steroids to the active site of aromatase. |
Tohoku Pharmaceutical University |
06/20/06 |
| 8576919 |
Structure-activity relationships of a new family of steroidal aromatase inhibitors. 1. Synthesis and evaluation of a series of analogs related to 19-[(methylthio)methyl]androstenedione (RU54115). |
Centre de Recherche de Roussel Uclaf |
06/20/06 |
| 8667367 |
Synthesis and structure-activity relationships of 6-substituted androst-4-ene analogs as aromatase inhibitors. |
Tohoku College of Pharmacy |
06/20/06 |
| 8676338 |
Time-dependent inactivation of aromatase by 6-alkylandrosta-1,4-diene-3,17-diones. Effects of length and configuration of 6-alkyl group. |
Tohoku College of Pharmacy |
06/20/06 |
| 12852749 |
First dual aromatase-steroid sulfatase inhibitors. |
University of Bath |
06/19/06 |
| 16451067 |
Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation. |
Cardiff University |
06/19/06 |
| 16246562 |
Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2). |
Saarland University |
06/13/06 |
| 16279787 |
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach. |
University of Bologna |
06/13/06 |
| 15911319 |
Synthesis and characterization of azole isoflavone inhibitors of aromatase. |
Ohio State University |
06/13/06 |
| 15713418 |
Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure-activity relationship studies. |
Pharmacor Inc |
06/12/06 |
| 15225709 |
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas. |
Procyon Biopharma Inc. |
06/12/06 |
| 16387495 |
Depeptidization efforts on P3-P2' alpha-ketoamide inhibitors of HCV NS3-4A serine protease: effect on HCV replicon activity. |
Schering-Plough Research Institute |
06/11/06 |
| 16112862 |
Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency. |
Schering-Plough Research Institute |
06/11/06 |
| 16125392 |
Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors. |
Ohio State University |
06/11/06 |
| 14643311 |
Lysine sulfonamides as novel HIV-protease inhibitors: optimization of the Nepsilon-acyl-phenyl spacer. |
Pharmacor Inc |
06/11/06 |
| 8709110 |
Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design. |
Agouron Pharmaceuticals, Inc. |
06/06/06 |
| 16640336 |
Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication. |
Schering-Plough Research Institute |
06/06/06 |
| 16087332 |
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency. |
Schering-Plough Research Institute |
06/06/06 |
| 15501035 |
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex. |
Schering-Plough Research Institute |
06/06/06 |
| 16413182 |
Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid. |
Schering-Plough Research Institute |
06/06/06 |
| 16420042 |
Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease. |
Schering-Plough Research Institute |
06/06/06 |
| 8568831 |
Potent human immunodeficiency virus type 1 protease inhibitors that utilize noncoded D-amino acids as P2/P3 ligands. |
Lilly Research Laboratories |
06/06/06 |
| 14505679 |
1,2,5,6-tetra-O-benzyl-D-mannitol derivatives as novel HIV protease inhibitors. |
Pharmacor Inc |
06/05/06 |
| 16460936 |
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template. |
Chemical Diversity, Inc |
05/30/06 |
| 15615528 |
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors. |
University of Bari |
05/29/06 |
| 16275072 |
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II. |
Chemical Diversity, Inc |
05/29/06 |
| 15267241 |
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones. |
Ohio State University |
05/29/06 |
| 10514292 |
Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions. |
Hong Kong University of Science and Technology |
05/25/06 |
| 2754707 |
9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
Hoechst-Roussel Pharmaceuticals, Inc. |
05/24/06 |
| 2362265 |
Novel piperidine derivatives. Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine derivatives. |
Tsukuba Research Laboratories |
05/24/06 |
| 8784449 |
Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas. |
DuPont Merck Pharmaceutical Company |
05/23/06 |
| 8360874 |
Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands. |
Merck Research Laboratories |
05/23/06 |
| 12113826 |
Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy. |
University of Illinois at Chicago |
05/22/06 |
| 9871583 |
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere. |
University of Illinois at Chicago |
05/22/06 |
| 15887965 |
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors. |
University of Illinois at Chicago |
05/22/06 |
| 16480871 |
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands. |
Purdue University |
05/21/06 |
| 14592500 |
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir. |
Merck Research Laboratories |
05/16/06 |
| 10866371 |
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds. |
GlaxoSmithKline |
05/16/06 |
| 12419377 |
Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease. |
GlaxoSmithKline |
05/16/06 |
| 15582415 |
Optimization of pyrrolidinone based HIV protease inhibitors. |
GlaxoSmithKline |
05/16/06 |
| 15975788 |
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors. |
GlaxoSmithKline |
05/16/06 |
| 15482949 |
Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties. |
GlaxoSmithKline |
05/14/06 |
| 12852968 |
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent. |
Merck Research Laboratories |
05/14/06 |
| 12951118 |
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent. |
Merck Research Laboratories |
05/14/06 |
| 15482948 |
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold. |
GlaxoSmithKline |
05/14/06 |
| 12852969 |
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains. |
Merck Research Laboratories |
05/14/06 |
| 10732965 |
Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives. |
University of Bologna |
05/09/06 |
| 16203148 |
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus. |
Merck Research Laboratories |
05/09/06 |
| 16279781 |
Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease. |
Neuropharma |
05/08/06 |
| 16230018 |
Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE. |
Neuropharma |
05/08/06 |
| 12014965 |
Homodimeric tacrine congeners as acetylcholinesterase inhibitors. |
National Defense Medical Center |
05/08/06 |
| 16420031 |
Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. |
Instituto de Quimica Medica (CSIC) |
05/08/06 |
| 15324882 |
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1. |
Merck Research Laboratories |
05/07/06 |
| 15771436 |
Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
Universita di Siena |
05/02/06 |
| 10821713 |
SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. |
University of Bologna |
05/02/06 |
| 15324879 |
Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
Shanghai Institute of Materia Medica |
05/02/06 |
| 16220979 |
Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
Saarland University |
05/01/06 |
| 16570918 |
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
Saarland University |
05/01/06 |
| 15771425 |
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
Saarland University |
05/01/06 |
| 15202489 |
Synthesis of hydroxy derivatives of highly potent non-steroidal CYP 17 inhibitors as potential metabolites and evaluation of their activity by a non cellular assay using recombinant human enzyme. |
Saarland University |
05/01/06 |
| 16162008 |
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. |
Abbott Laboratories |
04/25/06 |
| 11527706 |
Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents. |
GlaxoSmithKline |
04/18/06 |
| 11514139 |
1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI). |
GlaxoSmithKline |
04/17/06 |
| 12109908 |
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI). |
GlaxoSmithKline |
04/17/06 |
| 12699381 |
Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK. |
GlaxoSmithKline |
04/17/06 |
| 12039591 |
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight. |
Abbott Bioresearch Center |
04/16/06 |
| 15080992 |
Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors. |
GlaxoSmithKline |
04/10/06 |
| 15743198 |
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
Saarland University |
04/10/06 |
| 16386899 |
Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors. |
Hawaii Biotech Inc. |
04/06/06 |
| 15225695 |
4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors. |
Tsukuba Research Laboratories |
04/04/06 |
| 16298527 |
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains. |
University of Pennsylvania |
04/04/06 |
| 12031334 |
Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. |
Novo Nordisk A/S |
04/04/06 |
| 16460937 |
Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3. |
GlaxoSmithKline |
04/04/06 |
| 16392787 |
Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies. |
Burnham Institute |
04/03/06 |
| 15983377 |
Efficient synthetic inhibitors of anthrax lethal factor. |
Burnham Institute for Medical Research |
04/03/06 |
| 16338135 |
The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection. |
Merck Research Laboratories |
04/03/06 |
| 12941332 |
6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
GlaxoSmithKline |
03/29/06 |
| 12941333 |
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). |
GlaxoSmithKline |
03/29/06 |
| 12941317 |
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis. |
GlaxoSmithKline |
03/29/06 |
| 11266159 |
3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). |
SmithKline Beecham Pharmaceuticals |
03/28/06 |
| 12699760 |
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
GlaxoSmithKline |
03/28/06 |
| 12699759 |
5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
GlaxoSmithKline |
03/28/06 |
| 11033082 |
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. |
SmithKline Beecham Pharmaceuticals |
03/28/06 |
| 15341487 |
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. |
GlaxoSmithKline |
03/21/06 |
| 16480273 |
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. |
Georgia State University |
03/14/06 |
| 16220977 |
Hydroxyethylene sulfones as a new scaffold to address aspartic proteases: design, synthesis, and structural characterization. |
Philipps-Universitat Marburg |
03/14/06 |
| 15027857 |
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity. |
Cyclacel Limited |
03/13/06 |
| 15261277 |
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors. |
Cyclacel Limited |
03/13/06 |
| 12857114 |
High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II. |
Uppsala University |
03/12/06 |
| 12593654 |
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes. |
Uppsala University |
03/06/06 |
| 15189032 |
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs. |
Linkoping University |
03/06/06 |
| 14695825 |
Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity. |
Uppsala University |
03/06/06 |
| 14522962 |
Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators. |
Probiodrug AG |
02/28/06 |
| 16201766 |
Isolation, catalytic properties, and competitive inhibitors of the zinc-dependent murine glutaminyl cyclase. |
Probiodrug AG |
02/28/06 |
| 16420052 |
The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. |
Probiodrug AG |
02/28/06 |
| 11881998 |
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. |
Instituto de Quimica Medica (CSIC) |
02/27/06 |
| 16279768 |
SAR and 3D-QSAR studies on thiadiazolidinone derivatives: exploration of structural requirements for glycogen synthase kinase 3 inhibitors. |
Instituto de Quimica Medica (CSIC) |
02/27/06 |
| 14561081 |
Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3beta) from a library of compound searching. |
Instituto de Quimica Medica (CSIC) |
02/27/06 |
| 11728181 |
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis. |
GlaxoSmithKline |
02/21/06 |
| 12941311 |
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines. |
AstraZeneca |
02/13/06 |
| 12941312 |
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines. |
AstraZeneca |
02/13/06 |
| 15081017 |
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors. |
AstraZeneca |
02/13/06 |
| 12941325 |
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation. |
AstraZeneca |
02/13/06 |
| 15081018 |
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors. |
AstraZeneca |
02/13/06 |
| 10969976 |
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1. |
Korea Research Institute of Bioscience and Biotechnology |
02/08/06 |
| 10753466 |
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex. |
Institut Curie |
02/08/06 |
| 11983514 |
Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors. |
Universidad de Navarra |
02/07/06 |
| 11960485 |
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics. |
Novartis Pharmaceuticals |
02/07/06 |
| 10465404 |
Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors. |
Institut Curie |
02/07/06 |
| 9871543 |
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases. |
Institut Curie |
02/07/06 |
| 14698171 |
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. |
Technische Universitat Braunschweig |
02/06/06 |
| 16250643 |
Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases. |
Universidad San Pablo CEU |
02/06/06 |
| 15689157 |
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. |
Lawrence Berkeley National Laboratory |
01/31/06 |
| 15664865 |
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes. |
Martin-Luther-University Halle-Wittenberg |
01/30/06 |
| 14761195 |
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. |
University of Athens |
01/29/06 |
| 12519061 |
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. |
Faculte de Medecine et de Pharmacie |
01/23/06 |
| 14695817 |
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones. |
Universitat Hamburg |
01/23/06 |
| 10998059 |
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. |
CNRS |
01/23/06 |
| 15830466 |
Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-beta-carbolines. |
CNRS |
01/21/06 |
| 12749903 |
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors. |
SUGEN, Inc. |
01/11/06 |
| 15189033 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. |
Pharmacia Italia |
01/10/06 |
| 15828833 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization. |
Nerviano Medical Sciences |
01/10/06 |
| 15713378 |
Benzodipyrazoles: a new class of potent CDK2 inhibitors. |
Nerviano Medical Sciences |
01/10/06 |
| 9154969 |
Improved P1/P1' substituents for cyclic urea based HIV-1 protease inhibitors: synthesis, structure-activity relationship, and X-ray crystal structure analysis. |
DuPont Merck Pharmaceutical Company |
01/09/06 |
| 8667359 |
Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors. |
DuPont Merck Pharmaceutical Company |
01/09/06 |
| 9871711 |
The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors. |
DuPont Merck Pharmaceutical Company |
01/09/06 |
| 11514172 |
Identification of selective inhibitors of cyclin dependent kinase 4. |
DuPont Pharmaceuticals Company |
12/23/05 |
| 11311054 |
Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors. |
DuPont Merck Pharmaceutical Company |
12/23/05 |
| 15482910 |
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors. |
DuPont Pharmaceuticals Company |
12/23/05 |
| 11354366 |
Quinazolines as cyclin dependent kinase inhibitors. |
DuPont Merck Pharmaceutical Company |
12/23/05 |
| 15974571 |
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. |
Johnson & Johnson Pharmaceutical |
12/22/05 |
| 15837297 |
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. |
Johnson & Johnson Pharmaceutical |
12/22/05 |
| 12747775 |
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
Lilly Research Laboratories |
12/21/05 |
| 15149678 |
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors. |
Lilly Research Laboratories |
12/13/05 |
| 12824014 |
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
Lilly Research Laboratories |
12/13/05 |
| 15225699 |
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors. |
Lilly Research Laboratories |
12/13/05 |
| 14552792 |
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
DCR&T, Lilly Spain S.A. |
12/13/05 |
| 15149644 |
Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors. |
Lilly Research Laboratories |
12/13/05 |
| 15546737 |
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation. |
Avenida de la Industria |
12/08/05 |
| 15780638 |
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases. |
Lilly Research Laboratories |
12/08/05 |
| 11741480 |
A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues. |
Banyu Tsukuba Research Institute |
12/07/05 |
| 11855980 |
Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase. |
University of Regensburg |
12/07/05 |
| 11741479 |
Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design. |
Banyu Tsukuba Research Institute |
12/07/05 |
| 10974196 |
Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. |
Parke-Davis Pharmaceutical Research |
11/16/05 |
| 16161995 |
4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors. |
Wyeth Research |
11/15/05 |
| 15745832 |
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor. |
Wyeth-Ayerst Research |
11/15/05 |
| 11078204 |
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines. |
Wyeth-Ayerst Research |
11/15/05 |
| 12270190 |
Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors. |
Wyeth Research |
11/15/05 |
| 15080999 |
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles. |
Wyeth Research |
11/15/05 |
| 15615514 |
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors. |
Wyeth Research |
11/14/05 |
| 16125383 |
Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles. |
Wyeth Research |
11/14/05 |
| 15771433 |
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. |
Johnson & Johnson Pharmaceutical |
11/09/05 |
| 16033269 |
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors. |
Johnson & Johnson Pharmaceutical |
11/09/05 |
| 15801830 |
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4. |
Pfizer |
11/03/05 |
| 15993068 |
2-Aminoquinazoline inhibitors of cyclin-dependent kinases. |
NAEJA Pharmaceutical Inc. |
11/02/05 |
| 15801831 |
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
Pfizer |
10/27/05 |
| 11101352 |
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
Parke-Davis Pharmaceutical Research |
10/20/05 |
| 14761189 |
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src. |
AstraZeneca |
10/18/05 |
| 16000000 |
Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. |
University of Auckland |
10/07/05 |
| 12217371 |
8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors. |
Wyeth-Ayerst Research |
09/28/05 |
| 12113830 |
Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles. |
Wyeth Research |
09/28/05 |
| 14552782 |
Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity. |
Wyeth Research |
09/28/05 |
| 15027848 |
7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases. |
Wyeth Research |
09/27/05 |
| 15916442 |
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles. |
Wyeth Research |
09/27/05 |
| 14698155 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3. |
Bristol-Myers Squibb Company |
09/27/05 |
| 15537345 |
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases. |
Bristol-Myers Squibb Company |
09/26/05 |
| 15027863 |
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent. |
Bristol-Myers Squibb Company |
09/14/05 |
| 15357981 |
Isoindolinone ureas: a novel class of KDR kinase inhibitors. |
Abbott Laboratories |
09/13/05 |
| 15743202 |
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. |
GlaxoSmithKline |
09/09/05 |
| 12643928 |
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases. |
Bristol-Myers Squibb Company |
09/07/05 |
| 12824044 |
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. |
Bristol-Myers Squibb Company |
09/07/05 |
| 15990302 |
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. |
GlaxoSmithKline |
09/07/05 |
| 15837294 |
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors. |
GlaxoSmithKline |
09/07/05 |
| 12431050 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern. |
Bristol-Myers Squibb Company |
09/06/05 |
| 12190313 |
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
08/31/05 |
| 15125971 |
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases. |
Bristol-Myers Squibb Company |
08/30/05 |
| 11063609 |
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
08/30/05 |
| 12482427 |
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. |
University of Newcastle |
08/23/05 |
| 10956187 |
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. |
University of Newcastle |
08/23/05 |
| 12431051 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2). |
Bristol-Myers Squibb Company |
08/23/05 |
| 12941338 |
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. |
University of Newcastle |
08/22/05 |
| 15239650 |
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. |
University of Newcastle |
08/17/05 |
| 12139449 |
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. |
University of Newcastle |
08/17/05 |
| 12639547 |
Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. |
GlaxoSmithKline |
08/11/05 |
| 14684309 |
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors. |
GlaxoSmithKline |
08/11/05 |
| 12729639 |
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors. |
Merck Research Laboratories |
08/10/05 |
| 12443771 |
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics. |
Merck Research Laboratories |
08/10/05 |
| 12217372 |
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors. |
Merck Research Laboratories |
08/10/05 |
| 12852948 |
Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR. |
Merck Research Laboratories |
08/09/05 |
| 15012992 |
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR. |
Merck Research Laboratories |
08/09/05 |
| 12941314 |
Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors. |
Merck Research Laboratories |
08/09/05 |
| 14698157 |
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding. |
Merck Research Laboratories |
08/09/05 |
| 15566305 |
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel. |
Merck Research Laboratories |
08/09/05 |
| 15125964 |
The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase. |
Merck Research Laboratories |
08/09/05 |
| 10866394 |
Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity. |
Gilead Sciences Inc. |
07/28/05 |
| 10450950 |
Design of benzoic acid inhibitors of influenza neuraminidase containing a cyclic substitution for the N-acetyl grouping. |
University of Alabama at Birmingham |
07/28/05 |
| 10632058 |
Hydrophobic benzoic acids as inhibitors of influenza neuraminidase. |
University of Alabama at Birmingham |
07/28/05 |
| 10522696 |
Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity. |
Gilead Sciences Inc. |
07/28/05 |
| 10406636 |
Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors. |
Gilead Sciences Inc. |
07/28/05 |
| 9873727 |
A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity. |
Gilead Sciences Inc. |
07/27/05 |
| 15943472 |
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors. |
Abbott Laboratories |
07/27/05 |
| 15519161 |
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides. |
Yamanouchi Pharmaceutical Co. Ltd |
07/19/05 |
| 8667360 |
Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. |
Hebrew University of Jerusalem |
07/19/05 |
| 8960549 |
Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro. |
Hebrew University of Jerusalem |
07/19/05 |
| 12127526 |
Rational design of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2(p185(erbB)) tyrosine kinases. |
SUGEN, Inc. |
07/18/05 |
| 10514279 |
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70. |
ARIAD Pharmaceuticals, Inc. |
07/13/05 |
| 15670903 |
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives. |
Yamanouchi Pharmaceutical Co. Ltd |
07/07/05 |
| 9526555 |
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides. |
Glaxo Wellcome Research and Development Limited |
07/05/05 |
| 9651151 |
Structure-activity relationship studies of novel carbocyclic influenza neuraminidase inhibitors. |
Gilead Sciences Inc. |
07/05/05 |
| 11728184 |
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity. |
BioCryst Pharmaceuticals, Inc. |
07/05/05 |
| 10602697 |
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. |
SUGEN, Inc. |
06/29/05 |
| 10893303 |
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases. |
SUGEN, Inc. |
06/29/05 |
| 10882357 |
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
Novartis Pharmaceuticals |
06/10/05 |
| 12646019 |
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. |
SUGEN, Inc. |
06/09/05 |
| 11462982 |
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. |
University of Auckland |
06/02/05 |
| 9406595 |
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design. |
BioCryst Pharmaceuticals, Inc. |
06/01/05 |
| 15533054 |
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides. |
GlaxoSmithKline |
06/01/05 |
| 15013001 |
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains. |
GlaxoSmithKline |
06/01/05 |
| 15055992 |
Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. |
BioCryst Pharmaceuticals, Inc. |
05/31/05 |
| 15755666 |
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase. |
BioCryst Pharmaceuticals, Inc. |
05/31/05 |
| 10639280 |
Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. |
AstraZeneca |
05/24/05 |
| 11881999 |
Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. |
AstraZeneca |
05/24/05 |
| 11495584 |
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
Wyeth-Ayerst Research |
05/18/05 |
| 11063616 |
3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. |
University of Auckland |
05/17/05 |
| 10966743 |
4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors. |
Wyeth-Ayerst Research |
05/17/05 |
| 15653343 |
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'. |
Uppsala University |
05/17/05 |
| 11689083 |
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. |
Wyeth-Ayerst Research |
05/17/05 |
| 11262092 |
Synthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles. |
Wyeth-Ayerst Research |
05/17/05 |
| 8879541 |
Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines. |
Hebrew University of Jerusalem |
05/11/05 |
| 2552117 |
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. |
Hebrew University of Jerusalem |
05/10/05 |
| 1676428 |
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. |
Hebrew University of Jerusalem |
05/10/05 |
| 9629473 |
Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site. |
Sankyo Co. Ltd. |
05/04/05 |
| 8879560 |
Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline. |
Sankyo Co. Ltd. |
05/04/05 |
| 10956222 |
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src). |
University of Auckland |
05/02/05 |
| 10530956 |
Structure-activity relationship of HIV-1 protease inhibitors containing alpha-hydroxy-beta-amino acids. Detailed study of P1 site. |
Sankyo Co. Ltd. |
04/29/05 |
| 7518523 |
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors. |
Pfizer |
04/28/05 |
| 9784112 |
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors. |
Parke-Davis Pharmaceutical Research |
04/28/05 |
| 8355247 |
Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids). |
University of Auckland |
04/21/05 |
| 7510340 |
Tyrosine kinase inhibitors. 2. Synthesis of 2,2'-dithiobis(1H-indole-3-alkanamides) and investigation of their inhibitory activity against epidermal growth factor receptor and pp60v-src protein tyrosine kinases. |
University of Auckland |
04/21/05 |
| 8027985 |
Tyrosine kinase inhibitors. 3. Structure-activity relationships for inhibition of protein tyrosine kinases by nuclear-substituted derivatives of 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide). |
University of Auckland |
04/20/05 |
| 10395478 |
Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor. |
University of Auckland |
04/19/05 |
| 7769699 |
A central region in the hepatitis C virus NS4A protein allows formation of an active NS3-NS4A serine proteinase complex in vivo and in vitro. |
Washington University School of Medicine |
04/13/05 |
| 15239657 |
Novel azapeptide inhibitors of hepatitis C virus serine protease. |
Boehringer Ingelheim (Canada) Ltd. |
04/13/05 |
| 15491144 |
Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance. |
University of Alabama at Birmingham |
04/13/05 |
| 9876115 |
Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor. |
University of Auckland |
04/08/05 |
| 9191958 |
Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor. |
University of Auckland |
03/14/05 |
| 9513602 |
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors. |
University of Auckland |
03/14/05 |
| 10639288 |
Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase. |
Parke-Davis Pharmaceutical Research |
03/14/05 |
| 8632415 |
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. |
University of Auckland |
03/09/05 |
| 9154973 |
Tyrosine kinase inhibitors. 11. Soluble analogues of pyrrolo- and pyrazoloquinazolines as epidermal growth factor receptor inhibitors: synthesis, biological evaluation, and modeling of the mode of binding. |
University of Auckland |
03/08/05 |
| 9397172 |
Tyrosine kinase inhibitors. 13. Structure-activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. |
University of Auckland |
03/08/05 |
| 11384237 |
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. |
Pfizer |
03/03/05 |
| 7724556 |
Protein structure-based design of potent orally bioavailable, nonpeptide inhibitors of human immunodeficiency virus protease. |
Agouron Pharmaceuticals, Inc. |
02/26/05 |
| 8709109 |
Structure-based design and synthesis of substituted 2-butanols as nonpeptidic inhibitors of HIV protease: secondary amide series. |
Agouron Pharmaceuticals, Inc. |
02/25/05 |
| 7504733 |
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. |
Glaxo Group Research Ltd. |
02/24/05 |
| 9046331 |
Tyrosine kinase inhibitors. 6. Structure-activity relationships among N- and 3-substituted 2,2'-diselenobis(1H-indoles) for inhibition of protein tyrosine kinases and comparative in vitro and in vivo studies against selected sulfur congeners. |
Parke-Davis Pharmaceutical Research |
02/22/05 |
| 7658435 |
Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor. |
University of Auckland |
02/21/05 |
| 7562908 |
Tyrosine kinase inhibitors. 7. 7-Amino-4-(phenylamino)- and 7-amino-4-[(phenylmethyl)amino]pyrido[4,3-d]pyrimidines: a new class of inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. |
University of Auckland |
02/21/05 |
| 12036372 |
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits. |
Sphinx Laboratories |
02/07/05 |
| 8978850 |
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. |
Sphinx Laboratories |
02/02/05 |
| 1552513 |
Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity. |
Roche Products Limited |
01/25/05 |
| 7520079 |
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
Merck Research Laboratories |
01/24/05 |
| 9703473 |
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity. |
Parke-Davis Pharmaceutical Research |
01/18/05 |
| 9357527 |
Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines. |
Novartis Pharmaceuticals |
01/11/05 |
| 10821714 |
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
DuPont Pharmaceuticals Company |
01/04/05 |
| 10522695 |
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors. |
DuPont Pharmaceuticals Company |
01/04/05 |
| 11459666 |
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
DuPont Pharmaceuticals Company |
01/04/05 |
| 10937734 |
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors. |
DuPont Pharmaceuticals Company |
01/04/05 |
| 10698450 |
Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation. |
Medivir AB |
01/03/05 |
| 10579849 |
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors. |
Purdue University |
01/03/05 |
| 12057671 |
Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents. |
Purdue University |
01/03/05 |
| 9622549 |
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors. |
Purdue University |
12/29/04 |
| 11741777 |
Synthesis of alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors with non-identical aromatic rings. |
Purdue University |
12/29/04 |
| 11708913 |
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
Purdue University |
12/29/04 |
| 10514285 |
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
Medivir AB |
12/28/04 |
| 8421286 |
Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. |
Roche Products Limited |
12/27/04 |
| 1874734 |
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. |
Laboratoires Glaxo |
12/27/04 |
| 8809165 |
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
Upjohn |
12/16/04 |
| 1732526 |
Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. |
Roche Products Limited |
12/15/04 |
| 8894098 |
Discovery and optimization of nonpeptide HIV-1 protease inhibitors. |
Parke-Davis Pharmaceutical Research |
12/09/04 |
| 10465549 |
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety. |
Parke-Davis Pharmaceutical Research |
12/09/04 |
| 7699705 |
Nonpeptidic potent HIV-1 protease inhibitors: (4-hydroxy-6-phenyl-2-oxo-2H- pyran-3-yl)thiomethanes that span P1-P2' subsites in a unique mode of active site binding. |
Parke-Davis Pharmaceutical Research |
12/08/04 |
| 9371233 |
Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: the profound effect of polarity on antiviral activity. |
Parke-Davis Pharmaceutical Research |
12/08/04 |
| 14761194 |
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant. |
Universita degli Studi di Roma La Sapienza |
12/07/04 |
| 7684215 |
Diarylsulfones, a new chemical class of nonnucleoside antiviral inhibitors of human immunodeficiency virus type 1 reverse transcriptase. |
NCI-FCRDC |
12/06/04 |
| 12773052 |
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
Universita degli Studi di Roma La Sapienza |
12/06/04 |
| 7650679 |
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. |
Universita di Roma La Sapienza |
12/01/04 |
| 10698447 |
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs. |
Universita degli Studi di Roma La Sapienza |
11/29/04 |
| 9154967 |
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
Universita di Roma La Sapienza |
11/29/04 |
| 11931611 |
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase. |
Universita degli Studi di Roma La Sapienza |
11/29/04 |
| 7678654 |
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one. |
Merck Research Laboratories |
11/28/04 |
| 10794705 |
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations. |
Universita degli Studi di Roma La Sapienza |
11/24/04 |
| 10052969 |
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives. |
Universita degli Studi di Roma La Sapienza |
11/23/04 |
| 8558522 |
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. |
Universita di Roma |
11/22/04 |
| 11472208 |
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
Universita degli Studi di Roma La Sapienza |
11/22/04 |
| 8818233 |
5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors. |
Universita di Roma La Sapienza |
11/21/04 |
| 10715167 |
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. |
Upjohn |
11/18/04 |
| 7683725 |
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
Merck Research Laboratories |
11/17/04 |
| 7684450 |
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a |
Upjohn |
11/17/04 |
| 7683054 |
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues. |
Merck Research Laboratories |
11/16/04 |
| 1716683 |
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors. |
Merck Sharp and Dohme Research Laboratories |
11/11/04 |
| 10658583 |
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor. |
Parke-Davis Pharmaceutical Research |
11/10/04 |
| 8863804 |
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs. |
Lilly Research Laboratories |
11/08/04 |
| 9685235 |
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes. |
Boehringer Ingelheim Pharmaceuticals Inc. |
11/04/04 |
| 9685236 |
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. |
Boehringer Ingelheim Pharmaceuticals Inc. |
11/02/04 |
| 11378361 |
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors. |
DuPont Pharmaceuticals Company |
10/28/04 |
| 9240358 |
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 6. 2-Indol-3-yl- and 2-azaindol-3-yl-dipyridodiazepinones. |
Boehringer Ingelheim Pharmaceuticals Inc. |
10/28/04 |
| 10576692 |
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA). |
DuPont Pharmaceuticals Company |
10/28/04 |
| 1375293 |
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones. |
Boehringer Ingelheim Pharmaceuticals Inc. |
10/27/04 |
| 7658450 |
Structure-based design of novel HIV protease inhibitors: carboxamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent nonpeptidic inhibitors. |
Upjohn |
10/26/04 |
| 8523406 |
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs. |
Lilly Research Laboratories |
10/25/04 |
| 9371244 |
4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease. |
Parke-Davis Pharmaceutical Research |
10/21/04 |
| 11384233 |
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
GlaxoSmithKline |
10/20/04 |
| 9554878 |
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies. |
The DuPont Merck Pharmaceutical Company |
10/19/04 |
| 9836627 |
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities. |
DuPont Merck Pharmaceutical Company |
10/19/04 |
| 1712395 |
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. |
Boehringer Ingelheim Pharmaceuticals Inc. |
10/14/04 |
| 7490733 |
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine. |
Boehringer Ingelheim Pharmaceuticals Inc. |
10/13/04 |
| 7490732 |
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes. |
Boehringer Ingelheim Pharmaceuticals Inc. |
10/12/04 |
| 9089336 |
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones. |
Upjohn |
10/04/04 |
| 7689109 |
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity. |
Boehringer Mannheim GmbH |
10/01/04 |
| 1279173 |
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one. |
Merck Research Laboratories |
09/29/04 |
| 1910089 |
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679. |
Merck Sharp and Dohme Research Laboratories |
09/28/04 |
| 9216835 |
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere. |
Boehringer Ingelheim (Canada) Ltd. |
09/28/04 |
| 8642565 |
Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability. |
Sandoz Research Institute |
09/27/04 |
| 9083477 |
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities. |
Uppsala University |
09/23/04 |
| 8691434 |
Structure-based design of novel HIV protease inhibitors: sulfonamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent non-peptidic inhibitors. |
Upjohn |
09/23/04 |
| 9888839 |
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors. |
DuPont Pharmaceuticals Company |
09/22/04 |
| 9171880 |
Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors. |
DuPont Merck Pharmaceutical Company |
09/21/04 |
| 1279172 |
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues. |
Merck Research Laboratories |
09/20/04 |
| 1588552 |
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity. |
Merck Research Laboratories |
09/13/04 |
| 9719600 |
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class. |
Upjohn |
09/10/04 |
| 8064795 |
A novel nonpeptide HIV-1 protease inhibitor: elucidation of the binding mode and its application in the design of related analogs. |
Parke-Davis Pharmaceutical Research |
08/23/04 |
| 7932531 |
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity. |
SANDOZ Forschungsinstitut Ges.m.b.H. |
07/09/04 |
| 8021916 |
Aminodiol HIV protease inhibitors. 1. Design, synthesis, and preliminary SAR. |
Bristol-Myers Squibb Company |
07/08/04 |
| 8057276 |
Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease. |
Agouron Pharmaceuticals, Inc. |
07/08/04 |
| 8295206 |
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport. |
University of Pennsylvania |
07/08/04 |
| 1588551 |
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design. |
Merck Research Laboratories |
07/07/04 |
| 8765512 |
Paracyclophanes: a novel class of water-soluble inhibitors of HIV proteinase. |
Sandoz Research Institute |
07/06/04 |
| 2002466 |
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors. |
Merck Sharp and Dohme Research Laboratories |
06/24/04 |
| 10508432 |
Design and fast synthesis of C-terminal duplicated potent C(2)-symmetric P1/P1'-modified HIV-1 protease inhibitors. |
Uppsala University |
06/24/04 |
| 12534275 |
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance. |
Johns Hopkins University |
06/23/04 |
| 12093278 |
Amplification of the effects of drug resistance mutations by background polymorphisms in HIV-1 protease from African subtypes. |
Johns Hopkins University |
06/22/04 |
| 12699382 |
An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study. |
Academy of Sciences of the Czech Republic |
06/22/04 |
| 11906284 |
Hydroxyethylamine isostere of an HIV-1 protease inhibitor prefers its amine to the hydroxy group in binding to catalytic aspartates. A synchrotron study of HIV-1 protease in complex with a peptidomimetic inhibitor. |
Academy of Sciences of the Czech Republic |
06/22/04 |
| 11784141 |
Beta-strand mimicking macrocyclic amino acids: templates for protease inhibitors with antiviral activity. |
University of Queensland |
06/17/04 |
| 8494379 |
In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine. |
National Cancer Institute |
06/17/04 |
| 14690411 |
Secondary mutations M36I and A71V in the human immunodeficiency virus type 1 protease can provide an advantage for the emergence of the primary mutation D30N. |
University of Florida College of Medicine |
06/16/04 |
| 7783120 |
Use of medium-sized cycloalkyl rings to enhance secondary binding: discovery of a new class of human immunodeficiency virus (HIV) protease inhibitors. |
Upjohn |
06/16/04 |
| 12940739 |
Understanding binding affinity: a combined isothermal titration calorimetry/molecular dynamics study of the binding of a series of hydrophobically modified benzamidinium chloride inhibitors to trypsin. |
University of Groningen |
06/15/04 |
| 8171040 |
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor. |
Merck Research Laboratories |
06/14/04 |
| 7932546 |
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. |
Upjohn |
06/14/04 |
| 8544171 |
Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors. |
Upjohn |
06/14/04 |
| 2002465 |
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor. |
Merck Research Laboratories |
06/03/04 |
| 12723947 |
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors. |
University of Pennsylvania |
06/02/04 |
| 10346931 |
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine. |
Japan Energy Corporation |
06/02/04 |
| 10737742 |
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors. |
Boehringer Ingelheim Pharmaceuticals Inc. |
05/17/04 |
| 11585445 |
Synthesis of potent C(2)-symmetric, diol-based hiv-1 protease inhibitors. Investigation of thioalkyl and thioaryl P1/P1' substituents. |
Stockholm University |
05/13/04 |
| 8230098 |
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships. |
Glaxo Group Research Ltd. |
05/11/04 |
| 11585446 |
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal. |
Stockholm University |
05/11/04 |
| 14622012 |
Multidrug resistance to HIV-1 protease inhibition requires cooperative coupling between distal mutations. |
Johns Hopkins University |
05/10/04 |
| 8893827 |
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors. |
Upjohn |
04/27/04 |
| 8642558 |
Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity. |
Bristol-Myers Squibb Company |
04/21/04 |
| 8765511 |
Nonpeptidal P2 ligands for HIV protease inhibitors: structure-based design, synthesis, and biological evaluation. |
University of Illinois at Chicago |
04/21/04 |
| 8230099 |
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere. |
Glaxo Group Research Ltd. |
04/21/04 |
| 8164260 |
The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors. |
Merck Research Laboratories |
04/21/04 |
| 11009599 |
Thermodynamic basis of resistance to HIV-1 protease inhibition: calorimetric analysis of the V82F/I84V active site resistant mutant. |
Johns Hopkins University |
04/20/04 |
| 8642563 |
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching. |
National Institutes of Health |
04/08/04 |
| 8423599 |
Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere. |
Monsanto Corporate Research |
04/07/04 |
| 10715152 |
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease. |
Parke-Davis Pharmaceutical Research |
04/06/04 |
| 8423600 |
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors. |
Merck Research Laboratories |
03/31/04 |
| 8464047 |
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors. |
Merck Research Laboratories |
03/31/04 |
| 11543677 |
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution. |
Linkoping University |
03/30/04 |
| 11170625 |
Synthesis and comparative molecular field analysis (CoMFA) of symmetric and nonsymmetric cyclic sulfamide HIV-1 protease inhibitors. |
Uppsala University |
03/30/04 |
| 11112523 |
Estimation of the hydrophobic effect in an antigen-antibody protein-protein interface. |
University of Maryland Biotechnology Institute |
05/23/03 |
| 12408711 |
Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design. |
Sunesis Pharmaceuticals |
04/02/03 |
| 9829999 |
Inhibition of human caspases by peptide-based and macromolecular inhibitors. |
Merck Research Laboratories |
04/01/03 |
| 10381624 |
Purification and catalytic properties of human caspase family members. |
Merck Research Laboratories |
04/01/03 |
| 12044152 |
DNA gyrase interaction with coumarin-based inhibitors: the role of the hydroxybenzoate isopentenyl moiety and the 5'-methyl group of the noviose. |
UFR de Pharmacie |
03/31/03 |
| 8961940 |
Properties of tetrahydropteroylpentaglutamate bound to 10-formyltetrahydrofolate dehydrogenase. |
Virginia Commonwealth University |
03/31/03 |
| 2757186 |
Rapid measurement of binding constants and heats of binding using a new titration calorimeter. |
MicroCal, Inc. |
03/31/03 |
| 1621989 |
Synthesis of (6S)-5-formyltetrahydropteroyl-polyglutamates and interconversion to other reduced pteroylpolyglutamate derivatives. |
Virginia Commonwealth University |
03/31/03 |
| 9753439 |
Thermodynamic analysis of the binding of the polyglutamate chain of 5-formyltetrahydropteroylpolyglutamates to serine hydroxymethyltransferase. |
Virginia Commonwealth University |
03/31/03 |
| 12014967 |
Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. |
Novartis Pharmaceuticals |
03/05/03 |
| 9836373 |
Role of pro-inflammatory cytokines in rheumatoid arthritis. |
Kennedy Institute of Rheumatology |
03/05/03 |
| 8311464 |
Thioester hydrolysis by matrix metalloproteinases. |
Merck Research Laboratories |
03/05/03 |
| 1577761 |
Arginine residues involved in binding of tetrahydrofolate to sheep liver serine hydroxymethyltransferase. |
Indian Institute of Science |
02/25/03 |
| 8759643 |
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability. |
Ciba-Geigy Ltd. |
05/09/02 |
| 7613867 |
Comparative analysis of the X-ray structures of HIV-1 and HIV-2 proteases in complex with CGP 53820, a novel pseudosymmetric inhibitor. |
Ciba-Geigy Ltd. |
05/09/02 |
| 2200122 |
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease. |
Abbott Laboratories |
05/07/02 |
| 8558507 |
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease. |
Abbott Laboratories |
04/01/02 |
| 11305907 |
The vnd/NK-2 homeodomain: thermodynamics of reversible unfolding and DNA binding for wild-type and with residue replacements H52R and H52R/T56W in helix III. |
National Institutes of Health |
08/31/01 |
| 10531324 |
Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor. |
Indian Institute of Science |
12/20/00 |
| 10777579 |
Thermodynamic consequences of grafting enhanced affinity toward the mutated antigen onto an antibody. The case of anti-lysozyme antibody, HyHEL-10. |
Tohoku University |
12/20/00 |
| 9601024 |
Energetic roles of hydrogen bonds at the ureido oxygen binding pocket in the streptavidin-biotin complex. |
University of Washington at Seattle |
12/19/00 |
| 10908357 |
Recognition of a cognate RNA aptamer by neomycin B: quantitative evaluation of hydrogen bonding and electrostatic interactions. |
Ohio State University |
12/19/00 |
| 10606521 |
Equilibrium thermodynamics of a physiologically-relevant heme-protein complex. |
University of North Carolina at Chapel Hill |
12/15/00 |
| 10480891 |
Salt links dominate affinity of antibody HyHEL-5 for lysozyme through enthalpic contributions. |
University of Houston |
12/13/00 |
| 10747922 |
Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study. |
Swiss Federal Institute of Technology |
12/13/00 |
| 10694412 |
Thermodynamics of substrate binding to the chaperone SecB. |
Indian Institute of Science |
12/13/00 |
| 10869183 |
Thermodynamics of sequence-specific binding of PNA to DNA. |
Chalmers University of Technology |
12/12/00 |
| 8302837 |
Bound water molecules and conformational stabilization help mediate an antigen-antibody association. |
Institut Pasteur |
12/11/00 |
| 8955089 |
Role of salt bridge formation in antigen-antibody interaction. Entropic contribution to the complex between hen egg white lysozyme and its monoclonal antibody HyHEL10. |
Tohoku University |
12/11/00 |
| 9636058 |
Calorimetric investigation of ethidium and netropsin binding to chicken erythrocyte chromatin. |
Universite de Liege |
12/11/00 |
| 9677382 |
Thermodynamics of binding of calcium, magnesium, and zinc to the N-methyl-D-aspartate receptor ion channel peptidic inhibitors, conantokin-G and conantokin-T. |
University of Notre Dame |
12/11/00 |
| 9843408 |
Role of the cofactor calcium in the activation of outer membrane phospholipase A. |
Utrecht University |
12/11/00 |
| 7705353 |
Thermodynamics of antigen-antibody binding using specific anti-lysozyme antibodies. |
University of Maryland Biotechnology Institute |
12/11/00 |
| 10852706 |
Inhibiting protein-protein interactions: a model for antagonist design. |
Pfizer |
12/05/00 |
| 9405047 |
Energetics of heme binding to native and denatured states of cytochrome b562. |
University of Illinois at Urbana-Champaign |
12/04/00 |
| 10777500 |
Distinct Ca2+ binding properties of novel C2 domains of plant phospholipase dalpha and beta. |
Kansas State University |
12/04/00 |
| 7673199 |
The affinity maturation of anti-4-hydroxy-3-nitrophenylacetyl mouse monoclonal antibody. A calorimetric study of the antigen-antibody interaction. |
Institute of Physical and Chemical Research (RIKEN) |
12/04/00 |
| 9254595 |
Thermodynamic and structural analysis of phosphotyrosine polypeptide binding to Grb2-SH2. |
Schering-Plough Research Institute |
11/29/00 |