公开(公告)号：US20200055838A1

公开(公告)日：2020-02-20

申请号：US16487385

申请日：2018-02-12

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC: C07D401/12 ,  C07D405/14 ,  C07D403/12 ,  A61P35/00 ,  B01J31/24 ,  B01J27/122 ,  B01J31/30

Abstract: 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.

公开(公告)号：US20180237399A1

公开(公告)日：2018-08-23

申请号：US15772105

申请日：2016-11-01

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun NAN ,  Xin XIE ,  Yang LIU ,  Qing ZHANG ,  Linhai CHEN ,  Hui YANG

IPC: C07D239/60 ,  C07D239/52 ,  C07D213/69 ,  C07C49/825 ,  C07C39/19

CPC classification number: C07D239/60 ,  A61K31/505 ,  C07C39/08 ,  C07C39/19 ,  C07C49/825 ,  C07D213/69 ,  C07D239/48 ,  C07D239/52 ,  C07D239/54 ,  C07D239/545 ,  C07D239/56 ,  C07D251/20 ,  C07D309/38

Abstract: The present invention relates to a class of compounds represented by the formula I, or pharmaceutically acceptable salts thereof, methods for their preparation, and application as small molecule tools that function as GPR84 agonists, and their use in preparing a medicament for the treatment of septicemia.