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：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：EP3299014B1

公开(公告)日：2019-11-20

申请号：EP16795854.5

申请日：2016-05-13

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Shanghai Acebright Pharmaceuticals Co. Ltd.

发明人： GUO, Shiyan ,  GAN, Yong ,  ZHANG, Ao ,  MIAO, Zehong ,  GAO, Li ,  DING, Jian

IPC分类号： A61K9/28 ,  A61K9/48 ,  A61K31/502 ,  A61K47/32 ,  A61K47/38 ,  A61K47/40 ,  A61K47/34 ,  A61P35/00 ,  A61K47/10 ,  A61K9/08 ,  A61K9/10 ,  A61K9/14 ,  A61K9/20

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

公开(公告)号：EP3418277A1

公开(公告)日：2018-12-26

申请号：EP17752701.7

申请日：2017-02-17

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

发明人： ZHANG, Ao ,  GENG, Meiyu ,  XING, Li ,  AI, Jing ,  SONG, Zilan ,  PENG, Xia ,  GU, Wangting ,  DING, Jian

IPC分类号： C07D401/12 ,  C07D213/75 ,  C07D413/12 ,  C07D417/12 ,  C07D403/12 ,  C07D405/12 ,  A61K31/4427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4545 ,  A61P35/00

CPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/4545 ,  C07D213/75 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.

公开(公告)号：EP3018147A1

公开(公告)日：2016-05-11

申请号：EP14819337.8

申请日：2014-07-02

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

发明人： DING, Jian ,  AI, Jing ,  CHEN, Yi ,  HUANG, Xun

IPC分类号： C08B37/04 ,  A61K31/734 ,  A61K31/737 ,  A61P35/00 ,  A61P35/04

CPC分类号： A61K31/737 ,  C08B37/0084 ,  C08L5/00

摘要： A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerising factor activity inhibitors and actin-aggregation inhibitors.

摘要翻译： 甲polygulonic酸硫酸盐或其药学上可接受的盐，制备方法以及在肿瘤的生长和/或转移抑制剂的制备中的用途是游离缺失盘。 本发明的polygulonic酸式硫酸酯或药学上可接受的盐可以以肿瘤生长抑制剂，肿瘤转移抑制剂，血管生成抑制剂，乙酰肝素酶抑制剂，c-Met的酶抑制剂，微管聚合抑制剂，肌动蛋白的任何一个或多个的制备中可以使用的 -depolymerising因子抑制剂活性和肌动蛋白聚合抑制剂。

公开(公告)号：EP2881395A1

公开(公告)日：2015-06-10

申请号：EP13825341.4

申请日：2013-07-24

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

发明人： ZHANG, Ao ,  MIAO, Zehong ,  YE, Na ,  HUAN, Xiajuan ,  SONG, Zilan ,  CHEN, Chuanhuizi ,  CHEN, Yi ,  DING, Jian

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502 ,  A61P9/10 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502

摘要： Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.

摘要翻译： 本发明提供一种由通式表示的异构体，药学上可接受的盐，酯，前药或水合物的I或其化合物piperazinotriazole。 这样提供了用于制备所述化合物，药物组合物含有该化合物，并且作为高选择性的聚（ADP-核糖）在制备药物用于预防聚合酶-1（PARP 1）抑制剂及其使用的方法和/ 或治疗的PARP有关的疾病。