75177-60-5Relevant academic research and scientific papers
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).
FGFR4 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0156-0158, (2019/10/10)
Provided are a class of compounds as shown in formula (I) as FGFR4 inhibitors, and pharmaceutically acceptable salts thereof, preparation methods therefor and the use thereof in the preparation of drugs for treating FGFR4-related diseases.
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.
Intramolecular transition-metal catalyzed cyclizations of electron rich chloroarenes
Braese, Stefan
, p. 6757 - 6759 (2007/10/03)
Electron rich chromium tricarbonylchloroarene complexes bearing an allyl ether moiety were cyclized under palladium catalysis with concomitant loss of the metal carbonyl fragment to give heterocyclic systems in moderate to good yields. Bimetallic catalysis with palladium and chromium compounds gave rise to cyclization of the parent chloroarenes in moderate yields and with low turnover numbers.
