公开(公告)号：EP3812384A1

公开(公告)日：2021-04-28

申请号：EP19822932.0

申请日：2019-06-21

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

发明人： SHEN, Jingshan ,  HE, Yang ,  WANG, Zhen ,  LI, Jianfeng ,  LIU, Yongjian ,  SUO, Jin ,  TIAN, Guanghui ,  CHEN, Weiming ,  YANG, Feipu ,  WANG, Yu ,  JIANG, Xiangrui ,  ZHANG, Rongxia ,  JIANG, Hualiang

IPC分类号： C07D409/14 ,  C07D409/12

摘要： The present invention relates to a maleate salt of a benzothiophene compound, a crystalline form and use thereof. Specifically, the present invention relates to a compound of formula (I-A), a crystalline form A, a preparation method thereof and a pharmaceutical composition comprising the same, and a use thereof in the preparation of drugs for preventing or treating the central nervous system diseases. The compound of formula (I-A) and the crystalline form A thereof in the present invention have excellent physical and chemical properties, high oral bioavailability, and the best comprehensive properties for preparing into drugs and they are more suitable for making pharmaceutical preparations and more suitable for storage.

公开(公告)号：EP3115361A1

公开(公告)日：2017-01-11

申请号：EP15757771.9

申请日：2015-03-09

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

发明人： JIANG, Hualiang ,  WANG, Zhen ,  LI, Jianfeng ,  ZHANG, Rongxia ,  HE, Yang ,  LIU, Yongjian ,  BI, Minghao ,  LIU, Zheng ,  TIAN, Guanghui ,  CHEN, Weiming ,  YANG, Feipu ,  WU, Chunhui ,  WANG, Yu ,  JIANG, Xiangrui ,  YIN, Jingjing ,  WANG, Guan ,  SHEN, Jingshan

IPC分类号： C07D409/12 ,  C07D471/04 ,  C07D409/14 ,  C07D519/00 ,  C07D495/04 ,  C07D417/12 ,  C07D413/12 ,  A61K31/496 ,  A61K31/519 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

摘要： Provided are heterocyclic compounds represented by formula (I), stereoisomers or pharmaceutically acceptable salts of said compounds, a pharmaceutical composition of said compounds, and an application of said compounds in the preparation of a drug for the prevention and/or treatment of a central nervous system disease.

公开(公告)号：EP3670511A1

公开(公告)日：2020-06-24

申请号：EP18846464.8

申请日：2018-08-14

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

发明人： HE, Yang ,  JIANG, Xiangrui ,  LI, Jianfeng ,  WANG, Yu ,  WANG, Zhen ,  CHEN, Weiming ,  ZHU, Fuqiang ,  WU, Chunhui ,  ZHANG, Rongxia ,  SHEN, Jingshan ,  JIANG, Hualiang

IPC分类号： C07D455/03 ,  A61K31/4375 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/30

摘要： The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.

公开(公告)号：EP2746284B1

公开(公告)日：2017-04-12

申请号：EP12823704.7

申请日：2012-08-14

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

发明人： LI, Jianfeng ,  TIAN, Guanghui ,  WANG, Zhen ,  SUO, Jin ,  JIANG, Xiangrui ,  LIU, Zheng ,  YANG, Xiaojun ,  XIE, Zhu ,  ZHAO, Xianguo ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P15/10 ,  A61P9/12 ,  A61P15/00 ,  A61P15/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/00 ,  A61P9/10 ,  A61P9/04 ,  A61P13/12 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06 ,  A61P11/02 ,  A61P37/08 ,  A61P27/06 ,  A61P1/00 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.

公开(公告)号：EP3971158A1

公开(公告)日：2022-03-23

申请号：EP20809416.9

申请日：2020-05-15

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

发明人： SHEN, Jingshan ,  GONG, Xudong ,  ZHU, Fuqiang ,  JIANG, Xiangrui ,  ZHANG, Yan ,  SUN, Changliang

IPC分类号： C07C37/52 ,  C07C37/11 ,  C07C39/23 ,  C07C67/343 ,  C07C69/94 ,  C07C51/353 ,  C07C65/19

摘要： Disclosed is a method for preparing cannabidiol and analogues thereof; the method is implemented by means of reacting a resorcinol derivative with menthyl-2,8-dien-1-ol or a derivative thereof. The method of the present invention has advantages of such as high chemical reaction selectivity and simple operation.

公开(公告)号：EP2746284A1

公开(公告)日：2014-06-25

申请号：EP12823704.7

申请日：2012-08-14

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

发明人： LI, Jianfeng ,  TIAN, Guanghui ,  WANG, Zhen ,  SUO, Jin ,  JIANG, Xiangrui ,  LIU, Zheng ,  YANG, Xiaojun ,  XIE, Zhu ,  ZHAO, Xianguo ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P15/10 ,  A61P9/12 ,  A61P15/00 ,  A61P15/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/00 ,  A61P9/10 ,  A61P9/04 ,  A61P13/12 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06 ,  A61P11/02 ,  A61P37/08 ,  A61P27/06 ,  A61P1/00 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.

摘要翻译： 本发明涉及由式（I），和药学上可接受的多晶型物，溶剂化物，水合物，脱水物，共结晶，无水，或其无定形形式，所述药物组合物和药物单位剂量形式含在代表pyrazolopyrimidinones的新的盐 同样，worin X darstellt有机或无机酸，马来酸优选，琥珀酸，甲磺酸，盐酸，等等。本发明还涉及pyrazolopyrimidinones和含有相同的药物组合物的化合物的共结晶或络合物。 因此，本发明涉及一种用于制备，使用其和含有盐或结晶形式的药物制剂。

公开(公告)号：EP4410788A1

公开(公告)日：2024-08-07

申请号：EP22875040.2

申请日：2022-09-29

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Wuhan Institute Of Virology, Chinese Academy of Sciences ,  Hainan Simcere Pharmaceutical Co., Ltd.

发明人： JIANG, Xiangrui ,  XU, Yechun ,  ZHANG, Leike ,  SU, Haixia ,  ZHANG, Qiumeng ,  ZHAO, Wenfeng ,  SHANG, Weijuan ,  SHEN, Jingshan ,  XIAO, Gengfu ,  JIANG, Hualiang

IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D207/26 ,  C07D307/02 ,  C07D309/02 ,  C07D335/02 ,  A61K31/38 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18

CPC分类号： A61K31/38 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18 ,  C07D207/26 ,  C07D307/02 ,  C07D309/02 ,  C07D335/02 ,  C07D403/12 ,  C07D403/14

摘要： The present invention provides a compound represented by formula I, a racemate, an enantiomer, a diastereoisomer and a pharmaceutically acceptable salt thereof, and their use in preventing or treating a related disease caused by coronavirus and/or picornavirus infection.

公开(公告)号：EP4446326A1

公开(公告)日：2024-10-16

申请号：EP22903630.6

申请日：2022-12-12

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

发明人： SHEN, Jingshan ,  GAO, Zhaobing ,  XIAO, Gengfu ,  LI, Jia ,  YANG, Feipu ,  ZHANG, Leike ,  XIA, Bingqing ,  JIANG, Xiangrui ,  HE, Yang ,  JIANG, Hualiang

IPC分类号： C07D491/18 ,  A61K31/4748 ,  A61P31/12 ,  A61P31/14 ,  A61P19/10 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P25/00 ,  A61P27/00 ,  A61P43/00

摘要： The present invention provides a cyclic bisbenzyl tetrahydroisoquinoline compound as represented by formula (I), and a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, a racemate, a crystalline hydrate, and a solvate thereof, wherein R 1 and R 2 are as defined in the description. The present invention further provides a method for preparing the compound and the use of the compound for the preparation of an inhibitor for inhibiting viruses, inflammation, fibrosis and abnormal differentiation of T cells and/or for the preparation of a drug for preventing and/or treating related diseases caused by viruses, such as respiratory tract infections and pneumonia, inflanmmation-related diseases, fibrosis-related diseases and autoimmune diseases.

公开(公告)号：EP2671878A1

公开(公告)日：2013-12-11

申请号：EP12742093.3

申请日：2012-01-31

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

发明人： ZHANG, Qiang ,  ZHANG, Rongxia ,  TIAN, Guanghui ,  LI, Jianfeng ,  ZHU, Fuqiang ,  JIANG, Xiangrui ,  SHEN, Jingshan

IPC分类号： C07D263/26 ,  C07D263/62 ,  C07C17/16 ,  C07C22/04 ,  C07C29/159 ,  C07C33/20 ,  C07C51/06 ,  C07C57/30 ,  C07C209/08 ,  C07C209/50 ,  C07C209/62 ,  C07C231/02 ,  C07C231/08 ,  C07C231/12 ,  C07C303/28 ,  C07C309/66

CPC分类号： C07C235/34 ,  C07C17/16 ,  C07C41/26 ,  C07C43/225 ,  C07C43/23 ,  C07C59/64 ,  C07C59/68 ,  C07C213/02 ,  C07C215/54 ,  C07C217/62 ,  C07C309/66 ,  C07C309/73 ,  C07C309/75 ,  C07D263/26 ,  C07D263/52 ,  Y02P20/582 ,  C07C22/04

摘要： The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.