75177-60-5Relevant articles and documents
FGFR INHIBITOR AND APPLICATION THEREOF
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Paragraph 0123; 0125, (2020/01/22)
An azatricyclic compound (as represented by formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like. AA%%%Formula (I).
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping
Wang, Yikai,Chen, Zhengxia,Dai, Meibi,Sun, Peipei,Wang, Chunqiu,Gao, Yang,Zhao, Haixia,Zeng, Wenqin,Shen, Liang,Mao, Weifeng,Wang, Tian,Hu, Guoping,Li, Jian,Chen, Shuhui,Long, Chaofeng,Chen, Xiaoxin,Liu, Junhua,Zhang, Yang
, p. 2420 - 2423 (2017/05/10)
Introduction of a Michael acceptor on a flexible scaffold derived from pan-FGFR inhibitors has successfully yielded a novel series of highly potent FGFR4 inhibitors with selectivity over FGFR1. Due to reduced lipophilicity and aromatic ring count, this series demonstrated improved solubility and permeability. However, plasma instability and fast metabolism limited its potential for in vivo studies. Efforts have been made to address these problems, which led to the discovery of compound (?)-11 with improved stability, CYP inhibition, and good activity/selectivity for further optimization.
Synthesis of 6-chloro-3,5-dimethoxyhomophthalic acid, a key intermediate for the synthesis of radicicol and natural isocoumarin
Nozawa,Nakajima,Kawai
, p. 1112 - 1116 (2007/10/02)
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