公开(公告)号：EP4279486A1

公开(公告)日：2023-11-22

申请号：EP21917356.4

申请日：2021-12-31

申请人： Guangzhou Salustier Biosciences Co., Ltd. ,  Jinan University

发明人： DING, Ke ,  LI, Shan ,  ZHANG, Zhang ,  SI, Hongfei ,  TU, Zhengchao ,  REN, Xiaomei ,  LEI, Chong ,  TANG, Xia ,  GAO, Yueyi ,  CHAN, Shingpan

IPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D471/02 ,  C07D471/04 ,  A61K31/505 ,  A61K31/506 ,  A61P29/00 ,  A61P35/00

摘要： The present disclosure provides a class of 2-aminopyrimidine compounds with a structure shown in Formula (I) or their pharmaceutically acceptable salts, isotope derivatives, solvates, or their stereoisomers, geometric isomers, tautomers, or prodrug molecules or metabolites and pharmaceutical compositions and application thereof. The compounds of the present disclosure can efficiently and selectively inhibit the kinase activity of Janus Kinase 3 (JAK3), and have strong signal inhibition and cell proliferation inhibition effects on various blood tumor cells (especially human acute myeloid leukemia cell U937 cells) and solid tumor cells. They can be used to prepare anti-tumor drugs and drugs for preventing and treating inflammatory diseases.

公开(公告)号：EP3778585A1

公开(公告)日：2021-02-17

申请号：EP19777026.6

申请日：2019-03-29

申请人： Haihe Biopharma Co., Ltd. ,  Jinan University ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： DING, Ke ,  GENG, Meiyu ,  CHAN, Shingpan ,  DING, Jian ,  TAN, Li ,  AI, Jing ,  ZHANG, Zhang ,  PENG, Xia ,  REN, Xiaomei ,  JI, Yinchun ,  TU, Zhengchao ,  DAI, Yang ,  LU, Xiaoyun

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D215/233 ,  A61K31/4709 ,  A61P35/00

摘要： The present invention relates to quinoline or quinazoline compound represented by the formula (I), a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a prodrug molecule thereof, or a deuterated compound thereof. The compound of the present invention is effective in inhibiting the action of AXL protein kinase and can inhibit proliferation, migration, and invasion of various tumor cells. Further, the quinoline or quinazoline compound of the present invention has excellent metabolic stability, high in vivo antitumor activity, low toxic side effects, and can be used for preparing a drug for preventing hyperproliferative diseases such as tumors in humans and other mammals.

公开(公告)号：EP4056558A1

公开(公告)日：2022-09-14

申请号：EP20884968.7

申请日：2020-11-04

申请人： Jinan University

发明人： DING, Ke ,  CHAN, Shingpan ,  ZHANG, Zhang ,  DUAN, Yunxin ,  WANG, Jie ,  REN, Xiaomei ,  TU, Zhengchao

IPC分类号： C07D231/56 ,  C07D471/00 ,  C07D471/04 ,  C07D487/04 ,  A61K31/416 ,  A61P35/00

摘要： The present invention provides indazole derivatives or their pharmaceutically acceptable salts or stereoisomers having the structure shown in formula (I), and their pharmaceutical compositions and applications thereof. Such compounds can be used as protein kinase inhibitors, which can effectively inhibit the activity of tropomyosin receptor kinase (TRK) protein kinase and can inhibit the proliferation, migration and invasion of a variety of tumor cells.

公开(公告)号：EP3339294A1

公开(公告)日：2018-06-27

申请号：EP16836661.5

申请日：2016-08-18

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

发明人： DING, Ke ,  GENG, Meiyu ,  TAN, Li ,  DING, Jian ,  ZHANG, Zhang ,  AI, Jing ,  REN, Xiaomei ,  GAO, Donglin ,  TU, Zhengchao ,  LU, Xiaoyun ,  ZHANG, Dongmei

IPC分类号： C07D215/233 ,  C07D487/04 ,  C07D401/12 ,  A61K31/4709 ,  A61P35/00

CPC分类号： C07D401/12 ,  A61K31/4709 ,  C07D215/233 ,  C07D471/04 ,  C07D471/06 ,  C07D487/04 ,  C07D491/048 ,  C07D498/06 ,  C07D513/04 ,  C07D519/00

摘要： Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.