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.

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Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

Autor: Liu C; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Lin J; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Hynes J; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Wu H; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Wrobleski ST; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Lin S; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Dhar TG; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Vrudhula VM; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Sun JH; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Chao S; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Zhao R; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Wang B; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Chen BC; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Everlof G; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Gesenberg C; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Zhang H; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Marathe PH; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., McIntyre KW; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Taylor TL; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Gillooly K; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Shuster DJ; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., McKinnon M; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Dodd JH; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Barrish JC; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Schieven GL; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States., Leftheris K; Research and Development, Bristol-Myers Squibb , Princeton, New Jersey 08543, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2015 Oct 08; Vol. 58 (19), pp. 7775-84. Date of Electronic Publication: 2015 Sep 22.

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.