公开(公告)号：EP3275882B1

公开(公告)日：2020-09-23

申请号：EP16767773.1

申请日：2016-03-24

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.

发明人： SHEN, Jingkang ,  MENG, Tao ,  YU, Ting ,  MA, Lanping ,  WANG, Xin ,  CHEN, Lin

IPC分类号： C07D471/04 ,  C07D519/00

公开(公告)号：EP2966079A1

公开(公告)日：2016-01-13

申请号：EP14760712.1

申请日：2014-02-28

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

发明人： SHEN, Jingkang ,  YU, Ke ,  MENG, Tao ,  MA, Lanping ,  ZASK, Arie ,  MENG, Lanfang ,  WANG, Xin ,  CHEN, Yiyi

IPC分类号： C07D519/00 ,  C07D471/04 ,  C07D487/04 ,  A61K31/5386 ,  A61K31/5377 ,  A61P35/02 ,  A61P35/00

CPC分类号： C07D519/00 ,  C07D471/04 ,  C07D487/04

摘要： The present invention belongs to the field of pharmaceutical Chemistry. In particular, the present invention relates to a pyridopyrimidine or pyrimidopyrimidine compound as represented by general formula (I), or an isomer thereof or a pharmaceutical acceptable salt, ester, prodrug or solvate thereof, a preparation method, a pharmaceutical composition and uses thereof in preparing a mTOR inhibitor. As a mTOR inhibitor, the compound or the pharmaceutical composition thereof can be used for treating a disease or condition due to PI3K-AKT-mTOR signalling pathway malfunction.

摘要翻译： 本发明属于药物化学领域。 具体地说，本发明涉及由通式（I）表示的吡啶并嘧啶或嘧啶并嘧啶化合物或其异构体或其药学上可接受的盐，酯，前药或溶剂化物，其制备方法，药物组合物及其用途 制备mTOR抑制剂。 作为mTOR抑制剂，该化合物或其药物组合物可用于治疗由PI3K-AKT-mTOR信号传导途径故障引起的疾病或病症。

公开(公告)号：EP3501548A1

公开(公告)日：2019-06-26

申请号：EP17842668.0

申请日：2017-06-09

申请人： Fudan University ,  Shanghai Institute Of Materia Medica Chinese Academy of Sciences ,  Shanghai Miracogen Inc.

发明人： YU, Ke ,  SHEN, Jingkang ,  MENG, Tao ,  MA, Lanping ,  ZHANG, Xuesai ,  LI, Qingrou

IPC分类号： A61K47/68 ,  A61K31/537 ,  A61P35/00 ,  C07K16/36

摘要： A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.

公开(公告)号：EP2383262A1

公开(公告)日：2011-11-02

申请号：EP09831388.5

申请日：2009-12-10

申请人： Topharman Shanghai Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Topharman Shandong Co., Ltd.

发明人： LIU, Zheng ,  LI, Jianfeng ,  YANG, Xiaojun ,  WANG, Zhen ,  ZHANG, Jinfeng ,  ZHU, Yi ,  TIAN, Guanghui ,  JIN, Qing ,  SHEN, Jingkang ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D239/36 ,  A61K31/505 ,  A61P15/10

CPC分类号： A61K31/505 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07H15/26

摘要： The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof; and to the pharmaceutical composition as well as the preparation method of the said compounds. The said compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.

摘要翻译： 本发明涉及一类苯基嘧啶酮化合物，药物组合物，其制备方法及用途。 更具体地，本发明涉及一种下式I的苯基嘧啶酮化合物，其药学上可接受的盐或溶剂合物; 和药物组合物以及所述化合物的制备方法。 所述根据本发明的式I化合物可有效抑制V型磷酸二酯酶（PDE5），因此可用于治疗各种血管疾病，如男性勃起功能障碍，肺动脉高压等。

公开(公告)号：EP0806416B1

公开(公告)日：2003-05-07

申请号：EP95941572.0

申请日：1995-12-26

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： ZHU, Dayuan ,  TANG, Xican ,  LIN, Jinlai ,  ZHU, Cheng ,  SHEN, Jingkang ,  WU, Guansong ,  JIANG, Shanhao ,  YAMAGUCHI, Takuji c/o Tsumura & Co. ,  TANAKA, Kazuhiro ,  WAKANATSU, Takeshi c/o Tsumura & Co. ,  NISHIMURA, Hiroaki c/o Tsumura & Co.

IPC分类号： C07D221/22 ,  C07D401/06 ,  C07D401/12 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D221/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is (a), or R' and Y together form =CH; R is (C1-C5)alkyl, (b), (c), (d), wherein n is 0 or 1, X is H, (C1-C5)alkyl; (C1-C5)alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis -(C1-C5)alkyl; -(CH2mCOOZ, wherein m=0∩5, Z is H or (C1-C5)alkyl; -CH=CH-G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl1 substituted by (C1-C5)alkyl at the nitrogen atom; R' is H, (C1-C5)alkyl, pyridoyl, benzoyl substituted by (C1-C5)alkyloxy; R' is H or (C1-C5)alkyl; processes for their manufacture and their use as acetyl cholinesterase inhibitor.

公开(公告)号：EP4001267A1

公开(公告)日：2022-05-25

申请号：EP20844824.1

申请日：2020-07-17

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

发明人： XIONG, Bing ,  LI, Jia ,  GENG, Meiyu ,  SHEN, Jingkang ,  ZANG, Yi ,  AI, Jing ,  CHEN, Danqi ,  WANG, Qi ,  DONG, Ying ,  PENG, Xia ,  JI, Yinchun ,  TAN, Qian

IPC分类号： C07D239/84 ,  A61K31/517 ,  A61P35/00

摘要： The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof.

公开(公告)号：EP3808773A2

公开(公告)日：2021-04-21

申请号：EP19803867.1

申请日：2019-05-10

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

发明人： YU, Ke ,  SHEN, Jingkang ,  MENG, Tao ,  PEI, Jinpeng ,  MA, Lanping ,  WANG, Xin ,  JIN, Rui ,  DU, Zhiyan ,  CHEN, Lin ,  YU, Ting ,  ZHANG, Yongliang

IPC分类号： C07K16/28 ,  C07K19/00 ,  A61K39/395 ,  A61K47/68 ,  A61P35/00

摘要： Disclosed are a new AXL-targeting monoclonal antibody and antibody-drug conjugate. Also disclosed is a method for preparing said antibody and antibody-drug conjugate. The AXL antibody of the present invention can bind with purified humanAXL protein and multiple AXL on tumor cell surface with high effectiveness and high specificity. Said humanized antibody also has high affinity and low immunogenicity. Said AXL antibody-drug conjugate has markable performance against tumors having high AXL expression.

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：EP3275882A1

公开(公告)日：2018-01-31

申请号：EP16767773.1

申请日：2016-03-24

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.

发明人： SHEN, Jingkang ,  MENG, Tao ,  YU, Ting ,  MA, Lanping ,  WANG, Xin ,  CHEN, Lin

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II', wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.

摘要翻译： 提供了合成取代的吡啶和嘧啶化合物的方法。 特别地，提供了通过式II'化合物制备式III化合物的方法，其中每个基团的定义如说明书所述。 与其他方法化合物相比，本发明方法具有收率高，结果产物易于分离的特点。

公开(公告)号：EP2383262B1

公开(公告)日：2016-07-06

申请号：EP09831388.5

申请日：2009-12-10

申请人： Topharman Shanghai Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Topharman Shandong Co., Ltd.

发明人： LIU, Zheng ,  LI, Jianfeng ,  YANG, Xiaojun ,  WANG, Zhen ,  ZHANG, Jinfeng ,  ZHU, Yi ,  TIAN, Guanghui ,  JIN, Qing ,  SHEN, Jingkang ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D239/36 ,  A61K31/505 ,  A61P15/10

CPC分类号： A61K31/505 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07H15/26