公开(公告)号：EP3584239A1

公开(公告)日：2019-12-25

申请号：EP18753647.9

申请日：2018-02-12

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： HU, Youhong ,  GENG, Meiyu ,  REN, Wenming ,  DING, Jian ,  GUAN, Xiaocong ,  AI, Jing ,  WANG, Lang ,  PENG, Xia ,  LIU, Yang ,  DAI, Yang ,  ZENG, Limin

IPC分类号： C07D213/73 ,  C07D213/75 ,  C07D241/20 ,  A61K31/4965 ,  A61K31/44 ,  A61P35/00

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.