Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
摘要:
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
[EN] CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR<br/>[FR] CERTAINES TRIAZOLOPYRIDINES ET TRIAZOLOPYRAZINES, LEURS COMPOSITIONS ET LEURS PROCEDES D'UTILISATION
申请人:HUTCHISON MEDIPHARMA LTD
公开号:WO2011079804A1
公开(公告)日:2011-07-07
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
Certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor
申请人:Su Wei-Guo
公开号:US08507487B2
公开(公告)日:2013-08-13
Provided are certain triazolopyridines and triazolopyrazines of Formula 1.
wherein X, Y, R1, R2, R3, R4 and R5 have any of the meanings described herein; processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of cell proliferative disorders.
[EN] PYRAZOLE COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] COMPOSÉ PYRAZOLE ET SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 吡唑类化合物及其制备方法和用途
申请人:SICHUAN KELUN BIOTECH BIOPHARMACEUTICAL CO LTD