公开(公告)号：US20190211010A1

公开(公告)日：2019-07-11

申请号：US16331090

申请日：2017-09-06

Applicant: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Xuxing CHEN ,  Meiyu GENG ,  Lei JIANG ,  Yi CHEN ,  Jianhua CAO ,  Qingyun JIANG ,  Qianqian SHEN ,  Jian DING ,  Yucai YAO ,  Zhao ZHAO ,  Yuanfang XIONG

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P37/06 ,  C07D519/00

Abstract: The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.

公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

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

Inventor： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.