Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.

Autor: Hartz RA, Ahuja VT, Luo G, Chen L, Sivaprakasam P, Xiao H, Krause CM, Clarke WJ, Xu S, Tokarski JS, Kish K, Lewis H, Szapiel N, Ravirala R; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Mutalik S; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Nakmode D; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Shah D; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Burton CR, Macor JE, Dubowchik GM

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2023 Jun 08; Vol. 66 (11), pp. 7534-7552. Date of Electronic Publication: 2023 May 26.

Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.

Autor: Hartz RA; Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Ahuja VT; Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Nara SJ; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Kumar CMV; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Manepalli RKVLP; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Sarvasiddhi SK; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Honkhambe S; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Patankar V; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Dasgupta B; Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Rajamani R; Department of Molecular Structure and Design, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Muckelbauer JK; Department of Molecular Structure and Design, Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543, United States., Camac DM; Department of Molecular Structure and Design, Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543, United States., Ghosh K; Biocon-Bristol Myers Squibb Research and Development Center, Biocon Park, Plot No. 2 & 3, Bommasandra Phase IV, Jigani Link Road, Bangalore 560099, India., Pokross M; Department of Molecular Structure and Design, Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543, United States., Kiefer SE; Department of Protein Science, Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543, United States., Brown JM; Department of Neuroscience Discovery Biology, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Hunihan L; Department of Neuroscience Discovery Biology, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Gulianello M; Department of Neuroscience Discovery Biology, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Lewis M; Department of Neuroscience Discovery Biology, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Lippy JS; Department of Lead Evaluation, Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543, United States., Surti N; Department of Lead Evaluation, Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543, United States., Hamman BD; Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, Texas 77381, United States., Allen J; Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, Texas 77381, United States., Kostich WA; Department of Neuroscience Discovery Biology, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Bronson JJ; Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Macor JE; Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Dzierba CD; Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 Mar 10; Vol. 65 (5), pp. 4121-4155. Date of Electronic Publication: 2022 Feb 16.

Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF 1 ) receptor antagonist BMS-665053 leading to improved oral bioavailability.

Autor: Hartz RA; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA. Electronic address: richard.hartz@bms.com., Vrudhula VM; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA., Ahuja VT; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA., Grace JE; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA., Lodge NJ; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA., Bronson JJ; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA., Macor JE; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Mar 15; Vol. 27 (6), pp. 1360-1363. Date of Electronic Publication: 2017 Feb 10.

Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones.

Autor: Denhart DJ; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. derek.denhart@bms.com, Zuev D, Ditta JL, Hartz RA, Ahuja VT, Mattson RJ, Huang H, Mattson GK, Zueva L, Nielsen JM, Kozlowski ES, Lodge NJ, Bronson JJ, Macor JE

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Apr 01; Vol. 23 (7), pp. 2052-5. Date of Electronic Publication: 2013 Feb 13.

Chiral separation of potent corticotropin-releasing factor-1 receptor antagonists by supercritical fluid chromatography.

Autor: Qian-Cutrone J; Bristol-Myers Squibb Co., Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. jingfang.cutrone@bms.com, Hartz R, Ahuja VT, Vrudhula VM, Wu DR, Dalterio RA, Wang-Iverson D, Bronson JJ

Publikováno v: Journal of pharmaceutical and biomedical analysis [J Pharm Biomed Anal] 2011 Feb 20; Vol. 54 (3), pp. 602-6. Date of Electronic Publication: 2010 Oct 30.