1453211-57-8Relevant articles and documents
Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency
Kuriwaki, Ikumi,Kameda, Minoru,Iikubo, Kazuhiko,Hisamichi, Hiroyuki,Kawamoto, Yuichiro,Kikuchi, Shigetoshi,Moritomo, Hiroyuki,Kondoh, Yutaka,Terasaka, Tadashi,Amano, Yasushi,Tateishi, Yukihiro,Echizen, Yuka,Iwai, Yoshinori,Noda, Atsushi,Tomiyama, Hiroshi,Nakazawa, Taisuke,Hirano, Masaaki
, (2021/01/25)
Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target for the treatment of patients with bladder cancer harboring genetic alterations in FGFR3. We identified pyrimidine derivative 20b, which induced tumor regression following ora
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.
NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
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Paragraph 0270, (2014/05/25)
Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.
