The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Article Title | Organization | Depostion |
|---|
| 17985858 |
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1. |
eorgetown 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 Company |
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-Ayerst Research |
04/30/08 |
| TBD |
Molecular Origins of the Slow Streptavidin-Biotin Dissociation Kinetics. |
University of Washington at Seattle |
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 Inc. |
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. |
Università 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. |
Università 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 Università di 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. |
Università 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 (Ramppound38amp;D) Ltd |
03/28/08 |
| 17709247 |
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors. |
Amgen Inc. |
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 Inc. |
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 Inc. |
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 Inc. |
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 Inc. |
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 |
| TBD |
AR-709-An Investigational diaminopyrimidine: Inhibition, Binding and Mode of Action. |
ARPIDA AG |
09/28/07 |
| 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 amppound38amp; 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 amppound38amp; 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 amppound38amp; 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 |
| TBD |
Synthesis and biological evaluation of (R)- and (S)-2-(phosphonomethyl)pentanedioic acids as inhibitors of glutamate carboxypeptidase II |
Guilford |
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 amppound38amp; 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 (Ramppound38amp;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 amppound38amp; 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 amppound38amp; 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 amppound38amp; 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. |
Université de la Méditerranée |
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. |
Università 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 (Ramppound38amp;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 |
| 17083960 |
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes. |
Medical College of Wiscosin |
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 |
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 (Ramppound38amp;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 (Ramppound38amp;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 (Ramppound38amp;D) Ltd |
05/04/07 |
| 16202589 |
Structure-based discovery of a new class of Hsp90 inhibitors. |
Vernalis (Ramppound38amp;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 Inc. |
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 Inc. |
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 (Ramppound38amp;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 (Ramppound38amp;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 amppound38amp; 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 |
|