649735-63-7Relevant academic research and scientific papers
Control Strategy for the Manufacture of Brivanib Alaninate, a Novel Pyrrolotriazine VEGFR/FGFR Inhibitor
Lobben, Paul C.,Barlow, Evan,Bergum, James S.,Braem, Alan,Chang, Shih-Ying,Gibson, Frank,Kopp, Nathaniel,Lai, Chiajen,Laporte, Thomas L.,Leahy, David K.,Müslehiddinolu, Jale,Quiroz, Fernando,Skliar, Dimitri,Spangler, Lori,Srivastava, Sushil,Wasser, Daniel,Wasylyk, John,Wethman, Robert,Xu, Zhongmin
, p. 900 - 907 (2015/09/01)
This manuscript describes the control strategy for the commercial process to manufacture brivanib alaninate. The active pharmaceutical ingredient is a prodrug which is susceptible to hydrolysis. In addition to controlling hydrolysis, a robust strategy was
The 14C, 13C, and 15N syntheses of a potent VEGFR-2 kinase inhibitor, Brivanib, and its prodrug, Brivanib Alaninate
Tran, Scott B.,Lago, Michael W.,Tian, Yuan,Gong, Sharon X.,Batra, Indu,Allentoff, Alban J.,Maxwell, Brad D.,Bonacorsi, Samuel J.,Ogan, Marc,Rinehart, J. Kent,Balasubramanian, Balu
scheme or table, p. 324 - 331 (2012/06/04)
The interruption of tyrosine kinase vascular endothelial growth factor receptor-2 (VEGFR-2) signaling by the binding of a small molecule inhibitor, for example, Brivanib, to VEGFR-2 kinase domain has been shown as an effective method of slowing angiogenes
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
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)
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
PROCESS FOR THE PREPARATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY]-1-METHYLETHYL ESTER
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Page/Page column 5; 9-10, (2008/06/13)
The invention relates to an improved process for preparing [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful f
