63 articles for JA Robl
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT
Bristol-Myers Squibb
Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor.
Bristol-Myers Squibb Research & Development
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.
Bristol-Myers Squibb Research and Development
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.
Bristol-Myers Squibb Research and Development
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Discovery of pyridyl sulfonamide 11-beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors for the treatment of metabolic disorders.
Bristol-Myers Squibb
Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.
Departments of Discovery Chemistry, Metabolic Diseases, Lead Evaluation, Computer-Assisted Drug Design, Discovery Toxicology, Exploratory Clinical and Translational Research, and Pharmaceutical Candi
Synthesis and structure-activity relationship of dihydrobenzofuran derivatives as novel human GPR119 agonists.
Bristol-Myers Squibb
Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Bristol-Myers Squibb
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.
Bristol-Myers Squibb Research and Development
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
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Bristol-Myers Squibb Pharmaceutical Research Institute
Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls
TBA
Dual metalloprotease inhibitors. II. Effect of substitution and stereochemistry on benzazepinone based mercaptoacetyls
TBA
(D)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: synthesis and incorporation into the growth hormone secretagogues.
Bristol Myers Squibb
Tetrazole based amides as growth hormone secretagogues.
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
Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.
Bristol Myers Squibb
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Pharmaceutical Research Institute
Mercaptoacyl dipeptides as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase. Preliminary structure-activity studies
TBA
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11ß-hydroxydehydrogenase 1 (11ß-HSD1).
Bristol-Myers Squibb Research & Development
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.
Bristol-Myers Squibb Research and Development
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Bristol-Myers Squibb
Exploring monocyclic core: Discovery of pyrrol-2-one derivatives as a new series of potent MCHR1 antagonists with in vivo efficacy.
Biocon-Bristol Myers Squibb Research and Development Centre
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Bristol-Myers Squibb Research and Development
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
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
Bristol-Myers Squibb Pharmaceutical Research Institute
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.
Pharmaceutical Research Institute
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Bristol Myers Squibb
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Bristol Myers Squibb
NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein.
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
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Bristol-Myers Squibb Pharmaceutical Research Institute
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
TBA
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
A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors.
The 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
Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
Bristol-Myers Squibb
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
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.
Bristol-Myers Squibb Research and Development
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Bristol-Myers Squibb
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Bristol-Myers Squibb
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
Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
University of North Carolina at Chapel Hill
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
Shionogi
6,7-dihydropyrido[2,1-A]phthalazin-2-ones for the treatment and prophylaxis of hepatitis B virus infection
Hoffmann-La Roche
Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
Effector Therapeutics
Iminothiadiazine dioxides bearing an amine-linked substituent as BACE inhibitors, compositions, and their use
TBA
Tripeptides with non-code amino acids as potential serine proteases inhibitors.
Medical University of Bialystok
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.
Uppsala University
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
Martin-Luther-University Halle-Wittenberg
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