442 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
12
Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics.
Abbott Laboratories
18
Synthesis and activity of nonhydrolyzable pseudomonic acid analogues.
Abbott Laboratories
16
Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.
Abbott Laboratories
28
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
Abbott Laboratories
37
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
Abbott Laboratories
13
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).
Abbott Laboratories
60
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.
Abbott Laboratories
22
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
Abbott Laboratories
45
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
Abbott Laboratories
13
Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.
Abbott Laboratories
31
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Abbott Laboratories
45
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
Abbott Laboratories
6
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Abbott Laboratories
303
Large-scale application of high-throughput molecular mechanics with Poisson-Boltzmann surface area for routine physics-based scoring of protein-ligand complexes.
Abbott Laboratories
59
Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.
Abbott Laboratories
35
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Abbott Laboratories
38
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Abbott Laboratories
23
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.
Abbott Laboratories
50
Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.
Abbott Laboratories
30
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
Abbott Laboratories
25
Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.
Abbott Laboratories
37
Active reduced-size hexapeptide analogues of luteinizing hormone-releasing hormone.
Abbott Laboratories
48
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Abbott Laboratories
53
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.
Abbott Laboratories
51
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
11
Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.
Abbott Laboratories
34
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Abbott Laboratories
33
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.
Abbott Laboratories
35
Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.
Abbott Laboratories
1
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²¿ channel blockers with analgesic activity.
Abbott Laboratories
31
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
13
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management.
Abbott Laboratories
28
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.
Abbott Laboratories
19
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
2
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
Abbott Laboratories
2
Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors.
Abbott Laboratories
38
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.
Abbott Laboratories
21
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.
Abbott Laboratories
23
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
Abbott Laboratories
5
Allosteric modulators of the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
15
Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R).
Abbott Laboratories
2
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
60
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Abbott Laboratories
34
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.
Abbott Laboratories
29
Synthesis of potent pyrrolidine influenza neuraminidase inhibitors.
Abbott Laboratories
28
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Abbott Laboratories
37
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
55
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.
Abbott Laboratories
50
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
36
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
12
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
Abbott Laboratories
20
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Abbott Laboratories
20
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Abbott Laboratories
29
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
Abbott Laboratories
22
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Abbott Laboratories
22
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
Abbott Laboratories
11
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
Abbott Laboratories
15
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Abbott Laboratories
29
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
Abbott Laboratories
14
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
Abbott Laboratories
82
Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.
Abbott Laboratories
7
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
Abbott Laboratories
30
Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase.
Abbott Laboratories
15
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
Abbott Laboratories
127
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
Abbott Laboratories
36
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.
Abbott Laboratories
10
(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor.
Abbott Laboratories
6
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).
Abbott Laboratories
35
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Abbott Laboratories
17
Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity.
Abbott Laboratories
24
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
Abbott Laboratories
93
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
Abbott Laboratories
2
CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.
Abbott Laboratories
12
Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes.
Abbott Laboratories
50
Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung.
Abbott Laboratories
8
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
Abbott Laboratories
56
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.
Abbott Laboratories
12
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.
Abbott Laboratories
17
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
Abbott Laboratories
19
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.
Abbott Laboratories
13
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
Abbott Laboratories
4
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.
Abbott Laboratories
15
Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue.
Abbott Laboratories
35
Optimization and in vivo evaluations of a series of small, potent, and specific renin inhibitors containing a novel Leu-Val replacement.
Abbott Laboratories
44
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Abbott Laboratories
2
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.
Abbott Laboratories
6
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
Abbott Laboratories
9
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Abbott Laboratories
54
SAR ofa7 nicotinic receptor agonists derived from tilorone: exploration of a novel nicotinic pharmacophore.
Abbott Laboratories
1
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
Abbott Laboratories
7
Cracking the molecular weight barrier: fragment screening of an aminotransferase using an NMR-based functional assay.
Abbott Laboratories
17
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.
Abbott Laboratories
22
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.
Abbott Laboratories
35
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
Abbott Laboratories
21
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.
Abbott Laboratories
27
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.
Abbott Laboratories
23
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Abbott Laboratories
11
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
Abbott Laboratories
24
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Abbott Laboratories
26
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Abbott Laboratories
28
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
Abbott Laboratories
28
Biochemical and biophysical characterization of unique switch pocket inhibitors of p38a.
Abbott Laboratories
41
Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
Abbott Laboratories
75
In vitro studies on a class of quinoline containing histamine H3 antagonists.
Abbott Laboratories
24
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Abbott Laboratories
30
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Abbott Laboratories
38
Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs.
Abbott Laboratories
17
Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
26
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
69
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
Abbott Laboratories
23
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Abbott Laboratories
23
Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Abbott Laboratories
36
Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.
Abbott Laboratories
18
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
2
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
Abbott Laboratories
11
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.
Abbott Laboratories
3
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Abbott Laboratories
28
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Abbott Laboratories
18
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
31
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Abbott Laboratories
42
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
14
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Abbott Laboratories
1
Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase.
Abbott Laboratories
5
Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.
Abbott Laboratories
11
Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor.
Abbott Laboratories
4
Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies.
Abbott Laboratories
37
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.
Abbott Laboratories
42
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors.
Abbott Laboratories
7
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
Abbott Laboratories
28
Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.
Abbott Laboratories
31
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
Abbott Laboratories
42
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.
Abbott Laboratories
49
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.
Abbott Laboratories
22
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Abbott Laboratories
38
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Abbott Laboratories
52
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Abbott Laboratories
32
Discovery of a novel small molecule binding site of human survivin.
Abbott Laboratories
20
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
19
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Abbott Laboratories
45
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
Abbott Laboratories
14
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
Abbott Laboratories
39
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Abbott Laboratories
28
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.
Abbott Laboratories
30
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.
Abbott Laboratories
17
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Abbott Laboratories
22
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Abbott Laboratories
59
4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.
Abbott Laboratories
6
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Abbott Laboratories
24
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
Abbott Laboratories
71
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Abbott Laboratories
45
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Abbott Laboratories
13
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Abbott Laboratories
27
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
Abbott Laboratories
19
Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.
Abbott Laboratories
41
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Abbott Laboratories
55
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Abbott Laboratories
94
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Abbott Laboratories
17
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.
Abbott Laboratories
17
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Abbott Laboratories
5
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Abbott Laboratories
49
1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
28
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Abbott Laboratories
20
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Abbott Laboratories
31
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring.
Abbott Laboratories
42
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides.
Abbott Laboratories
16
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Abbott Laboratories
31
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Abbott Laboratories
41
Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.
Abbott Laboratories
58
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Abbott Laboratories
51
Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels.
Abbott Laboratories
52
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Abbott Laboratories
22
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
Abbott Laboratories
5
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
Abbott Laboratories
31
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Abbott Laboratories
30
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.
Abbott Laboratories
15
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Abbott Laboratories
44
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Abbott Laboratories
36
Identification of aminopiperidine benzamides as MCHr1 antagonists.
Abbott Laboratories
26
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors.
Abbott Laboratories
26
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Abbott Laboratories
42
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.
Abbott Laboratories
9
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Abbott Laboratories
33
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Abbott Laboratories
6
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
Abbott Laboratories
81
Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.
Abbott Laboratories
68
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Abbott Laboratories
3
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.
Abbott Laboratories
27
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Abbott Laboratories
39
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.
Abbott Laboratories
8
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Abbott Laboratories
25
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Abbott Laboratories
14
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Abbott Laboratories
16
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Abbott Laboratories
21
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.
Abbott Laboratories
37
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
Abbott Laboratories
55
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Abbott Laboratories
14
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Abbott Laboratories
25
Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
Abbott Laboratories
14
Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.
Abbott Laboratories
4
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
Abbott Laboratories
18
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Abbott Laboratories
43
Discovery of novel nonsteroidal glucocorticoid receptor modulators.
Abbott Laboratories
29
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
Abbott Laboratories
99
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
Abbott Laboratories
38
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.
Abbott Laboratories
100
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Abbott Laboratories
28
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
Abbott Laboratories
35
Structure-activity relationships of novel potent MurF inhibitors.
Abbott Laboratories
23
5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.
Abbott Laboratories
44
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Abbott Laboratories
18
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
Abbott Laboratories
6
Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor.
Abbott Laboratories
13
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors.
Abbott Laboratories
15
Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.
Abbott Laboratories
14
Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.
Abbott Laboratories
26
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.
Abbott Laboratories
12
The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles.
Abbott Laboratories
51
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
Abbott Laboratories
37
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Abbott Laboratories
19
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.
Abbott Laboratories
13
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Abbott Laboratories
22
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Abbott Laboratories
36
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Abbott Laboratories
27
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.
Abbott Laboratories
45
Synthesis and evaluation of potent pyrrolidine H(3) antagonists.
Abbott Laboratories
4
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
Abbott Laboratories
26
Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors.
Abbott Laboratories
23
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
Abbott Laboratories
20
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
Abbott Laboratories
45
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Abbott Laboratories
24
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Abbott Laboratories
37
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.
Abbott Laboratories
20
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.
Abbott Laboratories
17
Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.
Abbott Laboratories
87
Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides.
Abbott Laboratories
17
Synthesis and biological evaluation of clitocine analogues as adenosine kinase inhibitors.
Abbott Laboratories
25
Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.
Abbott Laboratories
13
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Abbott Laboratories
21
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.
Abbott Laboratories
23
Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.
Abbott Laboratories
21
Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor..
Abbott Laboratories
13
Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors.
Abbott Laboratories
42
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
Abbott Laboratories
3
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Abbott Laboratories
16
Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists.
Abbott Laboratories
23
Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.
Abbott Laboratories
20
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.
Abbott Laboratories
56
Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression.
Abbott Laboratories
9
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
Abbott Laboratories
29
Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.
Abbott Laboratories
33
Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.
Abbott Laboratories
5
Design of adenosine kinase inhibitors from the NMR-based screening of fragments.
Abbott Laboratories
65
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.
Abbott Laboratories
6
Identification of novel inhibitors of urokinase via NMR-based screening.
Abbott Laboratories
5
Antifungal rapamycin analogues with reduced immunosuppressive activity.
Abbott Laboratories
44
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Abbott Laboratories
27
Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.
Abbott Laboratories
4
Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.
Abbott Laboratories
27
Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.
Abbott Laboratories
24
Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
Abbott Laboratories
27
Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.
Abbott Laboratories
26
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.
Abbott Laboratories
27
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.
Abbott Laboratories
15
NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.
Abbott Laboratories
19
Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.
Abbott Laboratories
15
trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.
Abbott Laboratories
27
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.
Abbott Laboratories
34
Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.
Abbott Laboratories
7
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.
Abbott Laboratories
28
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Abbott Laboratories
14
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.
Abbott Laboratories
13
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.
Abbott Laboratories
32
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Abbott Laboratories
5
Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.
Abbott Laboratories
8
Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.
Abbott Laboratories
47
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).
Abbott Laboratories
23
Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase.
Abbott Laboratories
27
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency.
Abbott Laboratories
12
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.
Abbott Laboratories
90
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.
Abbott Laboratories
38
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.
Abbott Laboratories
37
NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.
Abbott Laboratories
3
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign pr
Abbott Laboratories
14
(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.
Abbott Laboratories
15
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.
Abbott Laboratories
58
Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.
Abbott Laboratories
10
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
Abbott Laboratories
7
Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.
Abbott Laboratories
29
Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.
Abbott Laboratories
65
5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.
Abbott Laboratories
64
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Abbott Laboratories
16
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
Abbott Laboratories
25
Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.
Abbott Laboratories
22
Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-725
Abbott Laboratories
30
Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides.
Abbott Laboratories
46
Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol.
Abbott Laboratories
20
Novel Asp32-replacement tetrapeptide analogues as potent and selective CCK-A agonists.
Abbott Laboratories
54
Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog.
Abbott Laboratories
8
Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores.
Abbott Laboratories
38
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.
Abbott Laboratories
57
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
Abbott Laboratories
78
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
Abbott Laboratories
52
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Abbott Laboratories
6
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
Abbott Laboratories
7
The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists.
Abbott Laboratories
11
In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase.
Abbott Laboratories
8
Orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
Abbott Laboratories
33
Renin inhibitors based on novel dipeptide analogues. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond.
Abbott Laboratories
21
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.
Abbott Laboratories
16
New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site.
Abbott Laboratories
7
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.
Abbott Laboratories
33
Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
Abbott Laboratories
14
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.
Abbott Laboratories
49
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.
Abbott Laboratories
10
Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists.
Abbott Laboratories
10
LH-RH antagonists: design and synthesis of a novel series of peptidomimetics.
Abbott Laboratories
19
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.
Abbott Laboratories
110
Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships.
Abbott Laboratories
21
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.
Abbott Laboratories
14
New inhibitors of renin that contain novel phosphostatine Leu-Val replacements.
Abbott Laboratories
8
Identification and synthesis of a receptor binding site of human anaphylatoxin C5a.
Abbott Laboratories
5
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Abbott Laboratories
50
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
Abbott Laboratories
15
Improvements in the minimum binding sequence of C5a: examination of His-67.
Abbott Laboratories
10
Structure-function studies in a series of carboxyl-terminal octapeptide analogues of anaphylatoxin C5a.
Abbott Laboratories
32
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
Abbott Laboratories
34
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.
Abbott Laboratories
44
C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties.
Abbott Laboratories
35
Nonpeptide renin inhibitors employing a novel 3-aza(or oxa)-2,4-dialkyl glutaric acid moiety as a P2/P3 amide bond replacement.
Abbott Laboratories
13
Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
Abbott Laboratories
19
Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.
Abbott Laboratories
7
Discovery of a novel class of orally active, non-peptide angiotensin II antagonists.
Abbott Laboratories
28
Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists.
Abbott Laboratories
2
Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes.
Abbott Laboratories
4
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
Abbott Laboratories
1
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.
Abbott Laboratories
5
Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.
Abbott Laboratories
25
[3H]A-317491, a novel high-affinity non-nucleotide antagonist that specifically labels human P2X2/3 and P2X3 receptors.
Abbott Laboratories
8
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.
Abbott Laboratories
5
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Abbott Laboratories
3
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.
Abbott Laboratories
1
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Abbott Laboratories
4
Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.
Abbott Laboratories
3
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.
Abbott Laboratories
16
Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor.
Abbott Laboratories
34
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
Abbott Laboratories
3
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.
Abbott Laboratories
6
Characterization of the striatal M2 muscarinic receptor mediating inhibition of cyclic AMP using selective antagonists: a comparison with the brainstem M2 receptor.
Abbott Laboratories
5
Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors.
Abbott Laboratories
7
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.
Abbott Laboratories
69
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
12
Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production.
Abbott Laboratories
10
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
24
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Abbott Laboratories
36
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
45
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
28
Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors.
Abbott Laboratories
11
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
14
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
3
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.
Abbott Laboratories
2
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
21
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.
Abbott Laboratories
54
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.
Abbott Laboratories
41
3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.
Abbott Laboratories
14
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
13
[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
29
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Abbott Laboratories
20
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
28
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
49
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
35
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.
Abbott Laboratories
25
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Abbott Laboratories
7
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
Abbott Laboratories
27
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.
Abbott Laboratories
14
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Abbott Laboratories
9
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.
Abbott Laboratories
109
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Abbott Laboratories
11
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Abbott Laboratories
28
Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Abbott Laboratories
37
Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.
Abbott Laboratories
16
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt.
Abbott Laboratories
63
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.
Abbott Laboratories
38
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.
Abbott Laboratories
56
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Abbott Laboratories
16
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
Abbott Laboratories
39
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
24
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Abbott Laboratories
29
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Abbott Laboratories
51
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.
Abbott Laboratories
27
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Abbott Laboratories
52
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
49
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
5
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
26
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.
Abbott Laboratories
42
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.
Abbott Laboratories
8
Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.
Abbott Laboratories
21
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Abbott Laboratories
18
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.
Abbott Laboratories
8
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.
Abbott Laboratories
14
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
Abbott Laboratories
21
Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.
Abbott Laboratories
4
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.
Abbott Laboratories
20
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.
Abbott Laboratories
15
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
Abbott Laboratories
8
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
25
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
4
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.
Abbott Laboratories
56
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
Abbott Laboratories
63
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
17
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
Abbott Laboratories
1
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease.
Abbott Laboratories