896160-75-1Relevant 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.
CHEMICAL COMPOUNDS
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Page/Page column 52, (2008/06/13)
The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
