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：EP2746283A1

公开(公告)日：2014-06-25

申请号：EP11867338.3

申请日：2011-12-21

申请人： Guangzhou Institute Of Biomedicine And Health, Chinese Academy Of Sciences

发明人： DING, Ke ,  CHANG, Shaohua ,  XU, Shilin ,  ZHANG, Lianwen ,  TU, Zhengchao ,  DING, Jian ,  GENG, Meiyu ,  CHEN, Yi

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/541 ,  A61P35/00 ,  A61P35/02

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551

摘要： A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.

摘要翻译： 公开了式（I）或（II）的化合物和该化合物在制备用于治疗癌症的药物中的用途。 研究表明，该化合物可抑制多种肿瘤细胞的生长，可用于靶向表皮生长因子受体（EGFR），特别是可以用EGFR或T790M单突变或多重突变抑制肿瘤细胞。 因此，该化合物可用作EGFR抑制剂治疗癌症，具有较大的应用价值。

公开(公告)号：EP3299369B1

公开(公告)日：2020-11-11

申请号：EP16795921.2

申请日：2016-05-23

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

发明人： LONG, Yaqiu ,  GENG, Meiyu ,  XU, Zhongliang ,  AI, Jing

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

公开(公告)号：EP3584239A1

公开(公告)日：2019-12-25

申请号：EP18753647.9

申请日：2018-02-12

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

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

IPC分类号： C07D213/73 ,  C07D213/75 ,  C07D241/20 ,  A61K31/4965 ,  A61K31/44 ,  A61P35/00

摘要： An o -aminoheteroaryl alkynyl-containing compound, a preparation method therefor and a use thereof. The 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 has showed 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：EP3470415A1

公开(公告)日：2019-04-17

申请号：EP17802189.5

申请日：2017-05-24

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

发明人： JIANG, Hualiang ,  LIU, Hong ,  GENG, Meiyu ,  ZHENG, Mingyue ,  AI, Jing ,  WANG, Yulan ,  WU, Xiaowei ,  LI, Shuangjie ,  PENG, Xia ,  LI, Chunpu ,  CHEN, Kaixian ,  WANG, Bao

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541

摘要： The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a compound as represented by formula (I). Various radicals are as defined in the specification. The compound provided by the invention effectively inhibits an activity of an FGFR kinase, and can be used to manufacture a pharmaceutical product for treating a disease related to the activity of the FGFR kinase.

公开(公告)号：EP4296266A1

公开(公告)日：2023-12-27

申请号：EP22755576.0

申请日：2022-02-18

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

发明人： HU, Youhong ,  GENG, Meiyu ,  LI, Daqiang ,  SHEN, Aijun ,  ZHANG, Zhuo ,  LI, Yalei ,  YANG, Huajie ,  LIU, Hongchun ,  ZHONG, Hanyue ,  DING, Jian

IPC分类号： C07D237/14 ,  C07D401/04 ,  C07D403/04 ,  A61K31/50 ,  A61K31/501 ,  A61P3/10 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P33/06 ,  A61P35/00

摘要： The present invention relates to an S-configuration-containing amino benzamide pyridazinone compound, a preparation method therefor, and a pharmaceutical composition and application thereof. Specifically, the present invention relates to a compound represented by the following general formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition and application thereof. The S-configuration compound of the present application has very strong binding activity on class I histone deacetylase (HDAC1), and shows inhibitory activity on in-vitro proliferation of various tumor cells.

公开(公告)号：EP3815692A1

公开(公告)日：2021-05-05

申请号：EP19825647.1

申请日：2019-06-28

申请人： Shanghai Green Valley Pharmaceutical Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： GENG, Meiyu ,  ZHANG, Zhenqing ,  JIN, Yingshen ,  XIAO, Zhongping ,  DING, Jian

IPC分类号： A61K31/702 ,  A61P25/28 ,  A61P25/16 ,  A61P29/00 ,  A61P25/04 ,  A61P3/10

摘要： The present invention relates to an alginic oligosaccharic diacid composition comprising a mannuronic diacid of Formula (IV) or a pharmaceutically acceptable salt thereof, wherein n is an integer selected from 1 to 9, m is selected from 0, 1 or 2, m' is selected from 0 or 1, and wherein the total weight of alginic oligosaccharic diacid wherein n=1-5 accounts for more than 60% of the total weight of the composition; the total weight of guluronic acids accounts for less than 50% of the total weight of the composition.

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：EP3546460B1

公开(公告)日：2020-07-08

申请号：EP17874613.7

申请日：2017-11-24

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

发明人： ZHANG, Ao ,  DING, Jian ,  XIE, Hua ,  SONG, Zilan ,  XUE, Yu ,  TONG, Linjiang ,  GENG, Meiyu

IPC分类号： C07D471/14 ,  C07D487/14 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02 ,  A61P29/00 ,  A61P37/02

公开(公告)号：EP2917210B1

公开(公告)日：2019-02-27

申请号：EP13853072.0

申请日：2013-11-05

申请人： Shanghai Fochon Pharmaceutical Co. Ltd ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： WANG, Weibo ,  GENG, Meiyu ,  DING, Jian ,  ZHAO, Xingdong ,  AI, Jing ,  TIAN, Qiang ,  PENG, Xia ,  ZHANG, Weipeng ,  LIU, Hongbin ,  TAN, Haohan ,  CHEN, Ling

IPC分类号： C07D405/14 ,  A61K31/558 ,  A61P35/00