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197 articles for Bristol-Myers Squibb Pharmaceutical Research Institute

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDArticle TitlePublishedDeposition
15050627 Hydroxytriamides as potent gamma-secretase inhibitors. 19-APR-2004 28-NOV-2018
10201825 Solid-phase synthesis of benzisothiazolones as serine protease inhibitors. 08-MAR-1999 20-OCT-2018
27256912 Discovery of hydroxyl 1,2-diphenylethanamine analogs as potent cholesterol ester transfer protein inhibitors. 12-JUN-2016 18-SEP-2017
26320619 Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2). 10-SEP-2015 09-DEC-2016
8863797 Hydroxamic acid-based bisubstrate analog inhibitors of Ras farnesyl protein transferase. 25-NOV-1996 14-DEC-2014
23478148 Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor. 26-MAR-2013 13-APR-2014
23414838 Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists. 04-MAR-2013 24-SEP-2013
9171867 Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics as inhibitors of angiotensin-converting enzyme and neutral endopeptidase. 27-JUN-1997 20-MAY-2013
15780609 Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues. 22-MAR-2005 20-MAY-2013
15603955 (S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity. 17-DEC-2004 20-MAY-2013
15745809 Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs). 04-MAR-2005 20-MAY-2013
8355245 Activated ketone based inhibitors of human renin. 23-SEP-1993 19-MAY-2013
7636851 Farnesyl diphosphate-based inhibitors of Ras farnesyl protein transferase. 12-SEP-1995 19-MAY-2013
7853336 Phosphinyl acid-based bisubstrate analog inhibitors of Ras farnesyl protein transferase. 10-MAR-1995 19-MAY-2013
2231594 Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis. 06-DEC-1990 19-MAY-2013
1895299 Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety. 22-OCT-1991 19-MAY-2013
18374566 2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis. 15-APR-2008 15-DEC-2012
18374568 Pyrano-[2,3b]-pyridines as potassium channel antagonists. 15-APR-2008 15-DEC-2012
18282707 Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues. 17-MAR-2008 14-DEC-2012
17766113 Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor. 18-SEP-2007 13-DEC-2012
17188861 A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE. 19-FEB-2007 12-DEC-2012
16730979 Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors. 20-JUN-2006 08-DEC-2012
16162005 Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors. 15-SEP-2005 04-DEC-2012
15780616 Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships. 22-MAR-2005 02-DEC-2012
15780629 Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors. 22-MAR-2005 02-DEC-2012
15027861 Discovery of a potent and novel motilin agonist. 18-MAR-2004 30-NOV-2012
12930139 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. 21-AUG-2003 29-NOV-2012
12502366 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. 27-DEC-2002 27-NOV-2012
9857090 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). 21-JAN-1999 09-NOV-2012
9379443 Sulfated galactocerebrosides as potential antiinflammatory agents. 10-NOV-1997 05-NOV-2012
8960546 Development of potent thrombin receptor antagonist peptides. 23-JAN-1997 03-NOV-2012
7837222 Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators. 28-FEB-1995 29-OCT-2012
1469703 Dihydropyrimidine angiotensin II receptor antagonists. 27-JAN-1993 23-OCT-2012
2061928 Isoprenyl phosphinylformates: new inhibitors of squalene synthetase. 06-AUG-1991 21-OCT-2012
15081034 Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists. 14-APR-2004 12-OCT-2012
11738569 Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues. 12-DEC-2001 05-OCT-2012
11738570 Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664. 12-DEC-2001 05-OCT-2012
11714605 Beta 3 agonists. Part 1: evolution from inception to BMS-194449. 20-NOV-2001 04-OCT-2012
14759732 Synthesis and SAR exploration of dinapsoline analogues. 15-XXX-2004 29-MAY-2012
20732813 Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38a MAP kinase inhibitors. 13-SEP-2010 12-JUN-2011
20471832 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. 04-JUN-2010 20-NOV-2010
9134746 Isolation and structure determination of sulfonoquinovosyl dipalmitoyl glyceride, a P-selectin receptor inhibitor from the alga Dictyochloris fragrans. 12-JUN-1997 25-AUG-2010
19272774 Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation. 16-MAR-2009 11-JAN-2010
9722499 Recent natural products based drug development: a pharmaceutical industry perspective. 19-OCT-1998 11-JAN-2010
18258427 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. 10-MAR-2008 11-NOV-2009
17933529 Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors. 06-NOV-2007 11-NOV-2009
1370696 Structure-activity relationships associated with 3,4,5-triphenyl-1H-pyrazole-1-nonanoic acid, a nonprostanoid prostacyclin mimetic. 25-FEB-1992 10-NOV-2009
1321910 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. 26-AUG-1992 10-NOV-2009
1683407 Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. 31-DEC-1991 10-NOV-2009
8558502 Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase. 28-FEB-1996 10-NOV-2009
8568812 Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity. 01-MAR-1996 10-NOV-2009
8496908 Interphenylene 7-oxabicyclo[2.2.1]heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists. 22-JUN-1993 10-NOV-2009
7731020 Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists. 31-MAY-1995 10-NOV-2009
8308857 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. 15-MAR-1994 10-NOV-2009
9464357 Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies. 27-FEB-1998 10-NOV-2009
8423602 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. 19-FEB-1993 10-NOV-2009
8558518 Dual metalloprotease inhibitors. 6. Incorporation of bicyclic and substituted monocyclic azepinones as dipeptide surrogates in angiotensin-converting enzyme/neutral endopeptidase inhibitors. 28-FEB-1996 10-NOV-2009
8576905 alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase. 08-MAR-1996 10-NOV-2009
7861414 Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors. 21-MAR-1995 10-NOV-2009
8035417 Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling. 18-AUG-1994 10-NOV-2009
7473584 alpha-Hydroxy phosphinyl-based inhibitors of human renin. 26-DEC-1995 10-NOV-2009
17383874 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. 14-MAY-2007 10-NOV-2009
1654430 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation. 22-OCT-1991 10-NOV-2009
1311765 Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site. 03-APR-1992 10-NOV-2009
17098428 Core exploration in optimization of chemokine receptor CCR4 antagonists. 22-JAN-2007 10-NOV-2009
10698452 3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors. 28-MAR-2000 10-NOV-2009
15125967 Identification of purine inhibitors of phosphodiesterase 7 (PDE7). 05-MAY-2004 10-NOV-2009
12781190 Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). 03-JUN-2003 10-NOV-2009
11020273 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. 24-OCT-2000 10-NOV-2009
17664068 Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds. 22-AUG-2007 10-NOV-2009
9871562 1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase. 26-JAN-1999 10-NOV-2009
12781195 Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety. 03-JUN-2003 10-NOV-2009
12392738 The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors. 23-OCT-2002 10-NOV-2009
12127522 Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase. 19-JUL-2002 10-NOV-2009
9822554 1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase. 17-DEC-1998 10-NOV-2009
1910091 Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2 antagonists. Semicarbazone omega-chains. 22-OCT-1991 10-NOV-2009
10753463 N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction. 26-JAN-2001 10-NOV-2009
11563929 Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1. 20-SEP-2001 10-NOV-2009
11549447 The discovery of novel, potent and selective PDE5 inhibitors. 10-SEP-2001 10-NOV-2009
12643944 Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives. 19-MAR-2003 10-NOV-2009
12372529 Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity. 09-OCT-2002 10-NOV-2009
11965381 Novel diamide-based inhibitors of IMPDH. 19-APR-2002 10-NOV-2009
14980664 Design and synthesis of benzoxazole derivatives as novel melatoninergic ligands. 24-FEB-2004 10-NOV-2009
12190306 Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. 22-AUG-2002 10-NOV-2009
10741553 Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay. 13-JUN-2000 10-NOV-2009
12482441 Development of a presynaptic 5-HT1A antagonist. 16-DEC-2002 10-NOV-2009
11527730 Structure-activity relationship studies of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of HCV NS3 serine protease. 30-AUG-2001 10-NOV-2009
12166939 (+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist. 08-AUG-2002 10-NOV-2009
12657277 Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents. 26-MAR-2003 10-NOV-2009
11814791 Novel dihydropyrazine analogues as NPY antagonists. 29-JAN-2002 10-NOV-2009
10602709 Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase. 24-JAN-2000 10-NOV-2009
12372516 A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase. 09-OCT-2002 10-NOV-2009
16386902 Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3. 07-FEB-2006 10-NOV-2009
11714606 BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor. 20-NOV-2001 10-NOV-2009
10698448 N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors. 28-MAR-2000 10-NOV-2009
11844662 Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. 07-MAR-2002 10-NOV-2009
14611849 Differentially functionalized diamines as novel ligands for the NPY2 receptor. 12-NOV-2003 10-NOV-2009
12270177 Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase. 24-SEP-2002 10-NOV-2009
15050644 (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. 30-MAR-2004 10-NOV-2009
12570368 Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. 06-FEB-2003 10-NOV-2009
12617891 Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors. 05-MAR-2003 10-NOV-2009
11150175 Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors. 18-JAN-2001 10-NOV-2009
10956219 Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. 08-SEP-2000 10-NOV-2009
11297448 Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. 12-APR-2001 10-NOV-2009
14592495 Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck). 31-OCT-2003 10-NOV-2009
15026042 Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists. 17-MAR-2004 10-NOV-2009
15863339 Identification of chemokine receptor CCR4 antagonist. 02-MAY-2005 10-NOV-2009
12372533 P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease. 09-OCT-2002 10-NOV-2009
15713401 Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors. 16-FEB-2005 10-NOV-2009
15546711 Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists. 19-NOV-2004 10-NOV-2009
15261279 Aminotriazine 5-HT7 antagonists. 20-JUL-2004 10-NOV-2009
15380200 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. 21-SEP-2004 10-NOV-2009
15177466 BMS-201620: a selective beta 3 agonist. 04-JUN-2004 10-NOV-2009
12643919 Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists. 19-MAR-2003 10-NOV-2009
12657268 Potent and selective aggrecanase inhibitors containing cyclic P1 substituents. 26-MAR-2003 10-NOV-2009
15603938 Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. 17-DEC-2004 10-NOV-2009
12646021 Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. 20-MAR-2003 10-NOV-2009
15943473 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. 09-JUN-2005 10-NOV-2009
14592493 2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy. 31-OCT-2003 10-NOV-2009
15603960 Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. 17-DEC-2004 10-NOV-2009
14643330 Heterocyclic aminopyrrolidine derivatives as melatoninergic agents. 03-DEC-2003 10-NOV-2009
12643943 Indanyl piperazines as melatonergic MT2 selective agents. 19-MAR-2003 10-NOV-2009
15615512 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. 23-DEC-2004 10-NOV-2009
14643312 Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification. 03-DEC-2003 10-NOV-2009
12798323 Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117. 11-JUN-2003 10-NOV-2009
12723945 Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors. 01-MAY-2003 10-NOV-2009
12852750 (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. 10-JUL-2003 10-NOV-2009
12657279 Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors. 26-MAR-2003 10-NOV-2009
16682193 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. 05-JUN-2006 10-NOV-2009
12852972 Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors. 10-JUL-2003 10-NOV-2009
14584934 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. 30-OCT-2003 10-NOV-2009
15908214 Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme. 31-MAY-2005 10-NOV-2009
15261280 Diaminopyrimidine and diaminopyridine 5-HT7 ligands. 20-JUL-2004 10-NOV-2009
16289878 Conversion of potent MMP inhibitors into selective TACE inhibitors. 09-JAN-2006 10-NOV-2009
16111887 New dual inhibitors of EGFR and HER2 protein tyrosine kinases. 26-SEP-2005 10-NOV-2009
16236499 Optimization of CCR4 antagonists: side-chain exploration. 18-NOV-2005 10-NOV-2009
14643322 beta-alanine dipeptides as MC4R agonists. 03-DEC-2003 10-NOV-2009
15603967 Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis. 17-DEC-2004 10-NOV-2009
16216508 Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists. 01-NOV-2005 10-NOV-2009
14684323 Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1. 19-DEC-2003 10-NOV-2009
15509177 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. 28-OCT-2004 10-NOV-2009
14505670 3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships. 24-SEP-2003 10-NOV-2009
16061379 Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes. 22-AUG-2005 10-NOV-2009
15713384 (R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents. 16-FEB-2005 10-NOV-2009
15013015 4-Substituted anilides as selective melatonin MT2 receptor agonists. 11-MAR-2004 10-NOV-2009
15993593 A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series. 02-AUG-2005 10-NOV-2009
15380218 N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist. 21-SEP-2004 10-NOV-2009
15357971 Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors. 10-SEP-2004 10-NOV-2009
16884313 NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein. 03-AUG-2006 10-NOV-2009
15357973 Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity. 10-SEP-2004 10-NOV-2009
17606372 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. 07-AUG-2007 10-NOV-2009
15267243 Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template. 22-JUL-2004 10-NOV-2009
15006407 Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction. 09-MAR-2004 10-NOV-2009
16516466 Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors. 03-APR-2006 10-NOV-2009
16931001 2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity. 25-SEP-2006 10-NOV-2009
15317463 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. 19-AUG-2004 10-NOV-2009
15771468 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. 17-MAR-2005 10-NOV-2009
17027261 Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). 25-DEC-2006 10-NOV-2009
15203165 Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists. 18-JUN-2004 10-NOV-2009
14643313 Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization. 03-DEC-2003 10-NOV-2009
17188863 Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). 19-FEB-2007 10-NOV-2009
16789733 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. 22-JUN-2006 10-NOV-2009
16213711 Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. 01-NOV-2005 10-NOV-2009
16481166 Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors. 20-MAR-2006 10-NOV-2009
15686947 Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists. 02-FEB-2005 10-NOV-2009
15546739 The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists. 19-NOV-2004 10-NOV-2009
17391962 Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors. 14-MAY-2007 10-NOV-2009
15546730 Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. 19-NOV-2004 10-NOV-2009
17187980 Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase. 05-FEB-2007 10-NOV-2009
17869100 Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues. 01-OCT-2007 10-NOV-2009
17855089 Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors. 01-OCT-2007 10-NOV-2009
15501061 Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists. 25-OCT-2004 10-NOV-2009
17292606 Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I. 02-APR-2007 10-NOV-2009
17462888 Benzopyran sulfonamides as KV1.5 potassium channel blockers. 04-JUN-2007 10-NOV-2009
17533126 Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations. 10-JUL-2007 10-NOV-2009
16473009 Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. 20-MAR-2006 10-NOV-2009
17576061 Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors. 30-JUL-2007 10-NOV-2009
17317169 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). 02-APR-2007 10-NOV-2009
17276676 A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors. 13-MAR-2007 10-NOV-2009
17398093 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. 14-MAY-2007 10-NOV-2009
17270437 New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. 13-MAR-2007 10-NOV-2009
17418570 CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity. 14-MAY-2007 10-NOV-2009
17368021 Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). 30-APR-2007 10-NOV-2009
17368025 Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. 30-APR-2007 10-NOV-2009
17973363 Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180). 29-NOV-2007 30-APR-2008
17552509 Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications. 28-JUN-2007 08-OCT-2007
16870435 Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa. 01-OCT-2006 02-JAN-2007
16434195 Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. 01-APR-2006 01-JAN-2007
15582405 5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa. 03-JAN-2005 01-JAN-2007
16730984 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. 01-AUG-2006 19-DEC-2006
16963264 Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties. 01-NOV-2006 19-DEC-2006
15771420 Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor. 24-MAR-2005 19-DEC-2006
16376077 Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1. 15-MAR-2006 07-NOV-2006
16046120 Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors. 15-SEP-2005 06-NOV-2006
16033281 Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. 28-JUL-2005 17-OCT-2006
12190313 Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. 29-AUG-2002 31-AUG-2005
11063609 Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. 02-NOV-2000 30-AUG-2005