Research Topics
| Jagabandhu DasSummaryAffiliation: Bristol-Myers Squibb Country: USA Publications
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Detail Information
Publications
Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analoguesJagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:41-4. 2002..BMS-189090 (5) is identified as a potent, selective, and reversible inhibitor of human alpha-thrombin that is efficacious in vivo in a mice lethality model, and in inhibiting both arterial and venous thrombosis in a rat model...- 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 assaysLouis J Lombardo
Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 4000, Princeton, New Jersey 08543 4000, USA
J Med Chem 47:6658-61. 2004..On the basis of its robust in vivo activity and favorable pharmacokinetic profile, 13 was selected for additional characterization for oncology indications... - 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinJagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, Post Office Box 4000, Princeton, New Jersey 08543 4000, USA
J Med Chem 49:6819-32. 2006..3 and 3 mg/kg twice daily. Dasatinib (2) is currently in clinical trials for the treatment of chronic myelogenous leukemia... - Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitorsJagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 16:3706-12. 2006.... - Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitorsJagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 16:2411-5. 2006..Compound 2 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo... 
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitorsJagabandhu Das
Bristol Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 18:2652-7. 2008..X-ray co-crystallography of a pyrazolo-pyrimidine analog 2b bound to unphosphorylated p38 alpha is also disclosed...- Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitorsJagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:2587-90. 2003..BMS-350751 (2) and BMS-358233 (3) are identified as potent Lck inhibitors with excellent cellular activities against T-cell proliferation... - Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117Jagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, 08543 4000, Princeton, NJ, USA
Bioorg Med Chem Lett 13:2145-9. 2003..BMS-243117 (compound 2) is identified as a potent, and selective Lck inhibitor with good cellular activity (IC(50)=1.1 microM) against T-cell proliferation... - 5-amino-pyrazoles as potent and selective p38α inhibitorsJagabandhu Das
Bristol Myers Squibb Research and Development, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 20:6886-9. 2010..Compound 2j was highly efficacious in vivo in inhibiting TNFα production in an acute murine model of TNFα production. X-ray co-crystallography of a 5-amino-pyrazole analog 2f bound to unphosphorylated p38α is also disclosed... - Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664Jagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:45-9. 2002.... - Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck)John Wityak
Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:4007-10. 2003..Structure-activity studies demonstrate the structural requirements for potent Lck activity. Cyclopropylamide 11d is a potent Lck inhibitor having sub-micromolar activity in a PBL proliferation assay... - Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitorsPing Chen
Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 14:6061-6. 2004..Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy... - Novel tricyclic inhibitors of IkappaB kinaseJames Kempson
Departments of Discovery Chemistry, Discovery Biology, and Metabolism and Pharmacokinetics and Synthesis and Analysis Technology Team, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543 4000, USA
J Med Chem 52:1994-2005. 2009..This, combined with an iterative rat cassette dosing strategy, was used to identify compounds with improved pharmacokinetic (PK) profiles to advance for in vivo evaluation... - Selective Itk inhibitors block T-cell activation and murine lung inflammationTai an Lin
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
Biochemistry 43:11056-62. 2004..Our findings represent the first description of selective inhibitors to probe human Itk function and its associated pathway, and support the hypothesis that Itk is a therapeutic target for immunosuppressive and inflammatory diseases... - 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)Scott H Watterson
Bristol Myers Squibb Research and Development, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 21:7006-12. 2011..Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease... - Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potencyPing Chen
Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
Bioorg Med Chem Lett 12:3153-6. 2002..Significant improvement of the cellular activity was achieved over the initial lead, compound 2... - Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinaseJames Kempson
Bristol Myers Squibb Research and Development, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 19:2646-9. 2009..A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS...