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Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives.

Bristol-Myers Squibb Pharmaceutical Research Institute

Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships.

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility.

Bristol-Myers Squibb Pharmaceutical Research Institute

Hydroxytriamides as potent gamma-secretase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of hydroxyl 1,2-diphenylethanamine analogs as potent cholesterol ester transfer protein inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.

Bristol-Myers Squibb Pharmaceutical Research Institute

Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).

Bristol-Myers Squibb Pharmaceutical Research Institute

(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Pyrano-[2,3b]-pyridines as potassium channel antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis.

Bristol-Myers Squibb Pharmaceutical Research Institute

Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.

Bristol-Myers Squibb Pharmaceutical Research Institute

Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.

Bristol-Myers Squibb Pharmaceutical Research Institute

A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of a potent and novel motilin agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

Bristol-Myers Squibb Pharmaceutical Research Institute

Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).

Bristol-Myers Squibb Pharmaceutical Research Institute

Sulfated galactocerebrosides as potential antiinflammatory agents.

Bristol-Myers Squibb Pharmaceutical Research Institute

Development of potent thrombin receptor antagonist peptides.

Bristol-Myers Squibb Pharmaceutical Research Institute

Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators.

Bristol-Myers Squibb Pharmaceutical Research Institute

Dihydropyrimidine angiotensin II receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.

Bristol-Myers Squibb Pharmaceutical Research Institute

Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.

Bristol-Myers Squibb Pharmaceutical Research Institute

Beta 3 agonists. Part 1: evolution from inception to BMS-194449.

Bristol-Myers Squibb Pharmaceutical Research Institute

Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38a MAP kinase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Isolation and structure determination of sulfonoquinovosyl dipalmitoyl glyceride, a P-selectin receptor inhibitor from the alga Dictyochloris fragrans.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation.

Bristol-Myers Squibb Pharmaceutical Research Institute

Recent natural products based drug development: a pharmaceutical industry perspective.

Bristol-Myers Squibb Pharmaceutical Research Institute

2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.

Bristol-Myers Squibb Pharmaceutical Research Institute

Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.

Bristol-Myers Squibb Pharmaceutical Research Institute

5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.

Bristol-Myers Squibb Pharmaceutical Research Institute

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

Bristol-Myers Squibb Pharmaceutical Research Institute

Benzopyran sulfonamides as KV1.5 potassium channel blockers.

Bristol-Myers Squibb Pharmaceutical Research Institute

CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.

Bristol-Myers Squibb Pharmaceutical Research Institute

Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.

Bristol-Myers Squibb Pharmaceutical Research Institute

A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Core exploration in optimization of chemokine receptor CCR4 antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.

Bristol-Myers Squibb Pharmaceutical Research Institute

NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.

Bristol-Myers Squibb Pharmaceutical Research Institute

Conversion of potent MMP inhibitors into selective TACE inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Optimization of CCR4 antagonists: side-chain exploration.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.

Bristol-Myers Squibb Pharmaceutical Research Institute

A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of chemokine receptor CCR4 antagonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Bristol-Myers Squibb Pharmaceutical Research Institute

Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.

Bristol-Myers Squibb Pharmaceutical Research Institute

Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.

Bristol-Myers Squibb Pharmaceutical Research Institute

Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.

Bristol-Myers Squibb Pharmaceutical Research Institute

Diaminopyrimidine and diaminopyridine 5-HT7 ligands.

Bristol-Myers Squibb Pharmaceutical Research Institute

Aminotriazine 5-HT7 antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

BMS-201620: a selective beta 3 agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of purine inhibitors of phosphodiesterase 7 (PDE7).

Bristol-Myers Squibb Pharmaceutical Research Institute

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

4-Substituted anilides as selective melatonin MT2 receptor agonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of benzoxazole derivatives as novel melatoninergic ligands.

Bristol-Myers Squibb Pharmaceutical Research Institute

Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1.

Bristol-Myers Squibb Pharmaceutical Research Institute

Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

Bristol-Myers Squibb Pharmaceutical Research Institute

beta-alanine dipeptides as MC4R agonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.

Bristol-Myers Squibb Pharmaceutical Research Institute

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.

Bristol-Myers Squibb Pharmaceutical Research Institute

Differentially functionalized diamines as novel ligands for the NPY2 receptor.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Bristol-Myers Squibb Pharmaceutical Research Institute

2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.

Bristol-Myers Squibb Pharmaceutical Research Institute

3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Bristol-Myers Squibb Pharmaceutical Research Institute

Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.

Bristol-Myers Squibb Pharmaceutical Research Institute

Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.

Bristol-Myers Squibb Pharmaceutical Research Institute

Indanyl piperazines as melatonergic MT2 selective agents.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.

Bristol-Myers Squibb Pharmaceutical Research Institute

Development of a presynaptic 5-HT1A antagonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.

Bristol-Myers Squibb Pharmaceutical Research Institute

Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.

Bristol-Myers Squibb Pharmaceutical Research Institute

A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel diamide-based inhibitors of IMPDH.

Bristol-Myers Squibb Pharmaceutical Research Institute

Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel dihydropyrazine analogues as NPY antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.

Bristol-Myers Squibb Pharmaceutical Research Institute

Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1.

Bristol-Myers Squibb Pharmaceutical Research Institute

The discovery of novel, potent and selective PDE5 inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Structure-activity relationship studies of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of HCV NS3 serine protease.

Bristol-Myers Squibb Pharmaceutical Research Institute

Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.

Bristol-Myers Squibb Pharmaceutical Research Institute

Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.

Bristol-Myers Squibb Pharmaceutical Research Institute

Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.

Bristol-Myers Squibb Pharmaceutical Research Institute

3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.

Bristol-Myers Squibb Pharmaceutical Research Institute

1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.

Bristol-Myers Squibb Pharmaceutical Research Institute

1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.

Bristol-Myers Squibb Pharmaceutical Research Institute

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Dual metalloprotease inhibitors. 6. Incorporation of bicyclic and substituted monocyclic azepinones as dipeptide surrogates in angiotensin-converting enzyme/neutral endopeptidase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Interphenylene 7-oxabicyclo[2.2.1]heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series.

Bristol-Myers Squibb Pharmaceutical Research Institute

The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.

Bristol-Myers Squibb Pharmaceutical Research Institute

Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.

Bristol-Myers Squibb Pharmaceutical Research Institute

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.

Bristol-Myers Squibb Pharmaceutical Research Institute

Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate.

Bristol-Myers Squibb Pharmaceutical Research Institute

alpha-Hydroxy phosphinyl-based inhibitors of human renin.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor.

Bristol-Myers Squibb Pharmaceutical Research Institute

Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2 antagonists. Semicarbazone omega-chains.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.

Bristol-Myers Squibb Pharmaceutical Research Institute

1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.

Bristol-Myers Squibb Pharmaceutical Research Institute

Structure-activity relationships associated with 3,4,5-triphenyl-1H-pyrazole-1-nonanoic acid, a nonprostanoid prostacyclin mimetic.

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.

Bristol-Myers Squibb Pharmaceutical Research Institute

Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site.

Bristol-Myers Squibb Pharmaceutical Research Institute

6,7-dihydropyrido[2,1-A]phthalazin-2-ones for the treatment and prophylaxis of hepatitis B virus infection

Hoffmann-La Roche

Pyrazolopyridines and pyrazolopyrimidines

Pfizer

Modulators of ATP-binding cassette transporters

Vertex Pharmaceuticals

Soluble guanylate cyclase stimulators

Merck Sharp & Dohme

Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists

Rugen Holdings (Cayman)

Iminothiadiazine dioxides bearing an amine-linked substituent as BACE inhibitors, compositions, and their use

TBA

Bicyclic heterocycles as FGFR4 inhibitors

Incyte

Substituted pyrido[3,4-b]pyrazines as GPR6 modulators

Takeda Pharmaceutical

The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.

Vertex Pharmaceuticals

3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.

Johnson & Johnson Pharmaceutical

Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.

Hebrew University of Jerusalem

Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site.

Sankyo

Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.

University of Auckland

Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.

University of Auckland