公开(公告)号：EP3225619A4

公开(公告)日：2018-05-23

申请号：EP15863532

申请日：2015-11-18

申请人： SHANGHAI INST MATERIA MEDICA CAS ,  GUANGZHOU INST BIOMED & HEALTH

发明人： DING KE ,  DING JIAN ,  CHAN SHINGPAN ,  GENG MEIYU ,  REN XIAOMEI ,  XIE HUA ,  TU ZHENGCHAO ,  CHEN YI

IPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  C07D239/47 ,  C07D401/02 ,  C07D403/12

CPC分类号： C07D403/12 ,  A61K31/4523 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/551 ,  C07D239/47 ,  C07D239/48 ,  C07D401/02 ,  C07D401/12

摘要： Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.

公开(公告)号：EP3299369A4

公开(公告)日：2018-05-02

申请号：EP16795921

申请日：2016-05-23

申请人： SHANGHAI INST MATERIA MEDICA CAS

发明人： LONG YAQIU ,  GENG MEIYU ,  XU ZHONGLIANG ,  AI JING

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5377 ,  A61P35/00

CPC分类号： A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5377 ,  C07D471/04

摘要： The present inveniton discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.