Chinese Academy of Sciences;Shanghai Institute of Materia Medica
发明人:
申请号：
EP18753647.9
公开号：
EP3584239A1
申请日:
2018.02.12
申请国别(地区):
EP
年份:
2019
代理人:
摘要：
An o-aminoheteroaryl alkynyl-containing compound, a preparation method therefor and a use thereof. The o-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 the o-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.
