302964-07-4Relevant articles and documents
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38α MAP kinase inhibitor
Hynes Jr., John,Wu, Hong,Pitt, Sidney,Shen, Ding Ren,Zhang, Rosemary,Schieven, Gary L.,Gillooly, Kathleen M.,Shuster, David J.,Taylor, Tracy L.,Yang, XiaoXia,McIntyre, Kim W.,McKinnon, Murray,Zhang, Hongjian,Marathe, Punit H.,Doweyko, Arthur M.,Kish, Kevin,Kiefer, Susan E.,Sack, John S.,Newitt, John A.,Barrish, Joel C.,Dodd, John,Leftheris, Katerina
, p. 1762 - 1767 (2008/12/20)
A novel structural class of p38α MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38α inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56Lck inhibitors
Chen, Ping,Norris, Derek,Das, Jagabandhu,Spergel, Steven H.,Wityak, John,Leith, Leslie,Zhao, Rulin,Chen, Bang-Chi,Pitt, Sidney,Pang, Suhong,Shen, Ding Ren,Zhang, Rosemary,De Fex, Henry F.,Doweyko, Arthur M.,McIntyre, Kim W.,Shuster, David J.,Behnia, Kamelia,Schieven, Gary L.,Barrish, Joel C.
, p. 6061 - 6066 (2007/10/03)
A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy. A series of substituted 2-(aminoheteroaryl)- thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy.
