Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol- 5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth
A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound. These prodrugs were evaluated for their ability t
Cai, Zhen-Wei,Zhang, Yongzheng,Borzilleri, Robert M.,Qian, Ligang,Barbosa, Stephanie,Wei, Donna,Zheng, Xiaoping,Wu, Lawrence,Fan, Junying,Shi, Zhongping,Wautlet, Barri S.,Mortillo, Steve,Jeyaseelan Sr., Robert,Kukral, Daniel W.,Kamath, Amrita,Marathe, Punit,D'Arienzo, Celia,Derbin, George,Barrish, Joel C.,Robl, Jeffrey A.,Hunt, John T.,Lombardo, Louis J.,Fargnoli, Joseph,Bhide, Rajeev S.
p. 1976 - 1980
(2008/12/22)
PROCESS FOR PREPARING CERTAIN PYRROLOTRIAZINE COMPOUNDS
The present invention relates to a process for preparing certain pyrrolotriazine compounds of the formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
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Page 31; 32
(2008/06/13)
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