258502-87-3Relevant academic research and scientific papers
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity
Lyne, Paul D.,Aquila, Brian,Cook, Donald J.,Dakin, Les A.,Ezhuthachan, Jay,Ioannidis, Stephanos,Pontz, Timothy,Su, Mei,Ye, Qing,Zheng, Xiaolan,Block, Michael H.,Cowen, Scott,Deegan, Tracy L.,Lee, John W.,Scott, David A.,Custeau, Dominique,Drew, Lisa,Poondru, Srinivasu,Shen, Minhui,Wu, Allan
scheme or table, p. 1026 - 1029 (2009/08/15)
A series of amidoheteroaryl compounds were designed and synthesized as inhibitors of B-Raf kinase. Several compounds from the series show excellent potency in biochemical, phenotypic and mode of action cellular assays. Potent examples from the series have also demonstrated good plasma exposure following an oral dose in rodents and activity against the Ras-Raf pathway in tumor bearing mice.
Amide derivatives useful as inhibitors of the production of cytokines
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, (2008/06/13)
The invention concerns amide derivatives of formula (I) wherein R3is (1-6C)alkyl or halogeno; Q1is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2is a substituent such as hydroxy and halogeno; q is 0-4; and Q2includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
