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.

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：EP3225619A1

公开(公告)日：2017-10-04

申请号：EP15863532.6

申请日：2015-11-18

申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences ,  Guangzhou Institute Of Biomedicine And Health, Chinese Academy Of Sciences

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 ,  C07D401/02 ,  C07D403/12 ,  C07D239/47 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02

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.

摘要翻译： 公开了2-氨基嘧啶化合物和药物组合物及其用途。 2-氨基嘧啶化合物的结构如式I所示，在结构式中，R 1，R 2，R 3，R 4，R 5，X，Y，Z，W，（i）如说明书和权利要求书中所定义。 这类化合物能有效抑制多种肿瘤细胞的生长，对EGFR和IGF1R蛋白酶具有抑制作用，可用于制备抗肿瘤药物，克服现有药物如吉非替尼，厄洛替尼等引起的耐受性。 该化合物对肿瘤具有选择性，特别是野生型非小细胞肺癌，并具有良好的药代动力学特征。

公开(公告)号：EP4310084A1

公开(公告)日：2024-01-24

申请号：EP22766278.0

申请日：2022-03-07

申请人： Jinan University ,  Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences

发明人： DING, Ke ,  ZHANG, Xin ,  XU, Fang ,  REN, Xiaomei ,  LU, Xiaoyun ,  MA, Dawei ,  HUANG, Weixue

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P35/00

摘要： The present disclosure provides a class of Pyridopyrimidine compounds having a structure shown in Formula (I) or their pharmaceutically acceptable salts, or stereoisomers or prodrug molecules and applications thereof. The compounds in the present disclosure can efficiently and selectively degrade AKT3 protein in cells without affecting AKT1/2, thereby significantly inhibiting tumor cell proliferation mediated by high expression of AKT3 protein. It can be used to prepare therapeutic drugs for cancer and other diseases related to abnormal expression of AKT3 protein.

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：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.