公开(公告)号：EP3524602A1

公开(公告)日：2019-08-14

申请号：EP17848144.6

申请日：2017-09-06

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

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

IPC分类号： C07D471/04 ,  C07D519/00 ,  C07D471/14 ,  C07D491/147 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61P35/00 ,  A61P37/06 ,  A61K31/437

摘要： 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：EP3434674A1

公开(公告)日：2019-01-30

申请号：EP17769410.6

申请日：2017-03-21

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

发明人： JIANG, Lei ,  GENG, Meiyu ,  ZHENG, Qiangang ,  HUANG, Min ,  WAN, Huixin ,  TANG, Shuai ,  FU, Xianlei ,  LAN, Xiaojing ,  CAO, Jianhua ,  LIU, Feifei ,  DING, Jian

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  A61K31/506 ,  A61P35/00 ,  A61P35/02

摘要： Provided in the present invention are a compound having the effects of preventing and treating diseases related to IDH mutation, and a preparation method and use thereof. In particular, provided in the present invention are the compound as shown in formula (I), a stereoisomer, a racemic body or a pharmaceutically acceptable salt thereof, and the use thereof in preparing drugs for preventing and treating diseases related to IDH mutation

公开(公告)号：EP2857403B1

公开(公告)日：2018-10-10

申请号：EP13798006.6

申请日：2013-04-23

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

发明人： YANG, Chunhao ,  MENG, Linghua ,  CHEN, Yanhong ,  WANG, Xiang ,  TAN, Cun ,  LI, Jiapeng ,  DING, Jian ,  CHEN, Yi

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/5377 ,  A61K31/5386 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/5377 ,  A61K31/5386 ,  C07D498/08 ,  C07D519/00

摘要： The present invention relates to a pyrrolo[2,1- f ][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1- f ][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1- f ][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.

公开(公告)号：EP3012259B1

公开(公告)日：2020-06-03

申请号：EP14813825.8

申请日：2014-06-18

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

发明人： SHEN, Jingkang ,  GENG, Meiyu ,  DING, Jian ,  XIONG, Bing ,  AI, Jing ,  MA, Yuchi ,  WANG, Xin ,  PENG, Xia ,  CHEN, Yuelei ,  CHEN, Danqi ,  MENG, Tao ,  MA, Lanping ,  JI, Yinchun

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/635 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61P35/00 ,  A61P35/04

公开(公告)号：EP2857403A1

公开(公告)日：2015-04-08

申请号：EP13798006.6

申请日：2013-04-23

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

发明人： YANG, Chunhao ,  MENG, Linghua ,  CHEN, Yanhong ,  WANG, Xiang ,  TAN, Cun ,  LI, Jiapeng ,  DING, Jian ,  CHEN, Yi

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/5377 ,  A61K31/5386 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/5377 ,  A61K31/5386 ,  C07D498/08 ,  C07D519/00

摘要： The present invention relates to a pyrrolo[2,1- f ][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1- f ][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1- f ][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.

摘要翻译： 本发明涉及吡咯并[2,1-f] [1,2,4]三嗪化合物，其异构体或其药学上可接受的盐，酯或水合物及其制备方法和应用。 吡咯并[2,1-f] [1,2,4]三嗪化合物具有通式（I）表示的结构。 通式（I）表示的吡咯并[2,1-f] [1,2,4]三嗪化合物可抑制磷脂酰肌醇-3激酶（PI3K）信号通路，从而用于制备治疗磷脂酰肌醇-3激酶 相关疾病如癌症。

公开(公告)号：EP3763712A1

公开(公告)日：2021-01-13

申请号：EP19763371.2

申请日：2019-03-05

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

发明人： CHEN, Xuxing ,  CHEN, Yi ,  HUANG, Ying ,  GENG, Meiyu ,  ZHANG, Qiong ,  DING, Jian ,  YAO, Yucai ,  SHEN, Qianqian ,  SHEN, Yanyan

IPC分类号： C07D471/04 ,  C07D519/00 ,  C07D471/14 ,  C07D491/147 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61P35/00 ,  A61P37/06

摘要： The invention provides an indolizine compound represented by formula I or a pharmaceutically acceptable salt thereof, a preparation method and a use thereof. The indolizine compound has an inhibitory effect on wild-type and/or mutant EZH2 or EZH1, and is expected to be developed into a novel drug for anti-tumor or for the treatment of autoimmune diseases.

公开(公告)号：EP3702354A1

公开(公告)日：2020-09-02

申请号：EP18862819.2

申请日：2018-09-29

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

发明人： LI, Lei ,  GENG, Meiyu ,  HUANG, Ying ,  DING, Jian ,  ZHANG, Qiong ,  HUANG, Min ,  TANG, Shuai ,  SHEN, Ning ,  CHEN, Yi

IPC分类号： C07D403/14 ,  C07D401/14 ,  A61K31/506 ,  A61K31/404 ,  A61P35/00

摘要： The invention relates to a compound of formula (I):

wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.

公开(公告)号：EP3184521A1

公开(公告)日：2017-06-28

申请号：EP15833329.4

申请日：2015-08-19

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

发明人： GENG, Meiyu ,  LIU, Lei ,  JIANG, Lei ,  HUANG, Min ,  ZHA, Chuantao ,  AI, Jing ,  WANG, Lei ,  CAO, Jianhua ,  DING, Jian

IPC分类号： C07D403/12 ,  C07D405/14 ,  C07D231/56 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D401/14 ,  C07D417/12 ,  A61K31/496 ,  A61K31/416 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/416 ,  A61K31/496 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00

摘要： The present invention provides an indazole compound as a FGFR kinase inhibitor, preparation and use thereof. Specifically, the present invention provides a compound represented by formula (I), wherein the definitions of each group are described in the specification. The compound of the present invention has good FGFR kinase-inhibiting activity, and can be used in preparing a series of medicines for treating FGFR kinase activity related diseases.

摘要翻译： 本发明提供了一种吲唑化合物作为FGFR激酶抑制剂及其制备和应用。 具体而言，本发明提供了由式（I）表示的化合物，其中每个基团的定义在说明书中描述。 本发明化合物具有良好的FGFR激酶抑制活性，可用于制备一系列治疗FGFR激酶活性相关疾病的药物。

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.