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O-AMINOHETEROARYL ALKYNYL-CONTAINING COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF
专利权人:
SHANGHAI INSTITUTE OF MATERIA MEDICA; CHINESE ACADEMY OF SCIENCES
发明人:
Youhong HU,Meiyu GENG,Wenming REN,Jian DING,Xiaocong GUAN,Jing AI,Lang WANG,Xia PENG,Yang LIU,Yang DAI,Limin ZENG
申请号:
US16487385
公开号:
US20200055838A1
申请日:
2018.02.12
申请国别(地区):
US
年份:
2020
代理人:
摘要:
An 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 shows 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.
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中国工程科技知识中心
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