PMID
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Article Title
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Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke

Bristol-Myers Squibb Research and Development
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

Bristol-Myers Squibb
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

Bristol-Myers Squibb Research and Development
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

Bristol-Myers Squibb Research and Development
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.

Bristol-Myers Squibb
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.

Bristol-Myers Squibb
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

Bristol-Myers Squibb
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.

Bristol-Myers Squibb
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

Bristol-Myers Squibb
Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.

Bristol-Myers Squibb
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.

Ironwood Pharmaceuticals
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.

Bristol-Myers Squibb
Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

Cerep
Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls

TBA
Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides

TBA
Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.

Bristol-Myers Squibb
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.

Bristol-Myers Squibb
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.

Bristol-Myers Squibb
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Bristol-Myers Squibb
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

Bristol-Myers Squibb
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Bristol-Myers Squibb Research and Development
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215

Bristol-Myers Squibb Research and Development
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.

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
Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.

TBA
Solid phase synthesis of phosphinic acid endothelin converting enzyme inhibitors

TBA
Mercaptoacyl dipeptides as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase. Preliminary structure-activity studies

TBA
Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2).

Bristol-Myers Squibb
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Bristol-Myers Squibb Research and Development
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791

Bristol-Myers Squibb
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.

Bristol-Myers Squibb
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

Bristol-Myers Squibb
5-amino-pyrazoles as potent and selective p38a inhibitors.

Bristol-Myers Squibb Research and Development
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 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases.

Bristol-Myers Squibb Research and Development
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

Bristol-Myers Squibb Research and Development
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

Bristol-Myers Squibb Research and Development
α-hydroxyamide derived aminodiols as potent inhibitors of hiv protease

TBA
Thromboxane receptor antagonist BMS-180291: A new pre-clinical lead

TBA
Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.

Bristol-Myers Squibb
Selective Itk inhibitors block T-cell activation and murine lung inflammation.

Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

Bristol-Myers Squibb
Benzothiazole based inhibitors of p38alpha MAP kinase.

Bristol-Myers Squibb Research and Development
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.

Bristol-Myers Squibb Pharmaceutical Research Institute
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.

Bristol Myers Squibb
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
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

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
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
De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.

Cerep
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
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
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1

Bristol Myers Squibb
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
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).

Bristol-Myers Squibb Pharmaceutical Research Institute
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.

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

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

Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute
Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.

Bristol-Myers Squibb Pri
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P

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

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
Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase.

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

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

Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P

Bristol-Myers Squibb
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.

Bristol Myers Squibb Research
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.

Biocon Bristol Myers Squibb Research Center
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
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).

Bristol-Myers Squibb Research and Development
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Bristol-Myers Squibb
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Bristol-Myers Squibb
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.

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

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
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.

Bristol-Myers Squibb
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Bristol-Myers Squibb Research and Development
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.

Bristol-Myers Squibb
Discovery of highly potent, selective, covalent inhibitors of JAK3.

Bristol-Myers Squibb Research and Development
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.

Bristol-Myers Squibb
Tetrazole derivatives as TRPA1 inhibitors

Boehringer Ingelheim International
TYK2 inhibitors and uses thereof

Nimbus Lakshmi
Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof

Pharmaxis
Selective inhibitors of protein arginine methlytransferase 5 (PRMT5)

Prelude Therapeutics
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity

Shionogi
Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors

Array Biopharma
Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer

Kainos Medicine
Inhibitors of indoleamine 2,3-dioxygenase (IDO)

Bristol-Myers Squibb
Pyridine derivatives as soft rock inhibitors

Redx Pharma
Carbonic anhydrase and matrix metalloproteinase inhibitors: sulfonylated amino acid hydroxamates with MMP inhibitory properties act as efficient inhibitors of CA isozymes I, II, and IV, and N-hydroxysulfonamides inhibit both these zinc enzymes.

Universita Degli Studi
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.

Martin-Luther-University Halle-Wittenberg
8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors.

Wyeth-Ayerst Research