Title:
ｏ−アミノヘテロアリールアルキニル基含有化合物およびその製造方法と用途
Document Type and Number:
Japanese Patent JP6965360
Kind Code:
B2
Abstract:
Ano-aminoheteroaryl alkynyl-containing compound, a preparation method therefor and a use thereof. Theo-aminoheteroaryl alkynyl-containing compound has a structure represented by formula (I), and the compound of formula (I) has advantages of a high FGFR and RET double target inhibitory activity and a relatively low KDR activity, and the compound of formula (I) exhibits a strong inhibitory activity in a human lung cancer cell line NCI-H1581 and a gastric cancer cell line SNU16 as well as an RET-dependent sensitive cell line BaF3-CCDC6-Ret and a mutant thereof. Pharmacokinetic data has showed that theo-aminoheteroaryl alkynyl-containing compound has druggability, and exhibits significant relevant inhibition of the growth of related tumors in a long-term animal model of drug efficacy and results in favorable animal condition at effective doses.
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Inventors:
Fu, You Hong
Gaan, Mayu
Ren, Wen Min
Jin, Din
Gwang, Xiao Zhong
Eye, gin
One, run
Pon, shea
Riu, Yang
Dai, Yang
Zhang, Lee Min
Gaan, Mayu
Ren, Wen Min
Jin, Din
Gwang, Xiao Zhong
Eye, gin
One, run
Pon, shea
Riu, Yang
Dai, Yang
Zhang, Lee Min
Application Number:
JP2019544871A
Publication Date:
November 10, 2021
Filing Date:
February 12, 2018
Export Citation:
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
International Classes:
C07D213/73; A61K31/4545; A61K31/496; A61K31/497; A61P35/00; A61P35/02; A61P43/00; C07D241/20
Domestic Patent References:
| JP2019527725A | ||||
| JP2008535780A | ||||
| JP2015523402A | ||||
| JP2014530865A |
Foreign References:
| WO2015108490A2 | ||||
| WO2016165658A1 | ||||
| WO2006077901A1 |
Attorney, Agent or Firm:
Kiyoji Kuzuwa