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.

公开(公告)号：EP2163538B1

公开(公告)日：2012-01-25

申请号：EP08748526.4

申请日：2008-05-22

申请人： Topharman Shanghai Co., Ltd. ,  Weifang Tehua Chemical Co., Ltd.

发明人： ZHU, Fuqiang ,  LI, Haihong ,  WANG, Wenzhong ,  ZHANG, Hui ,  SHEN, Jingshan

IPC分类号： C07C209/52 ,  C07C211/29 ,  C07C233/13 ,  C07C251/24 ,  C07D243/14

CPC分类号： C07C211/29 ,  C07C209/52 ,  C07C233/13 ,  C07C251/24 ,  C07D243/14

摘要： Preparation methods of 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and their intermediates. Compounds represented by the formula I and II. The preparation methods of 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine in which compounds represented by the formula I and II and o-nitrobenzaldehyde are used. These methods are absolutely novel synthetic routes for preparation of 4-acetyl-2,3,4,5-tetrahydro -benzo[1,4] diazepine. The routes are short and easy to operate and raw materials are readily available. The routes are economical and safe without using costly and unsafe lithium aluminium hydride.

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：EP3978497A1

公开(公告)日：2022-04-06

申请号：EP20813589.7

申请日：2020-05-29

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

发明人： SHEN, Jingshan ,  HE, Yang ,  WU, Chunhui ,  YANG, Feipu ,  WANG, Zhen ,  ZHANG, Junchi ,  ZHU, Fuqiang ,  QIN, Hongjian

IPC分类号： C07D487/04 ,  C07D409/04 ,  C07D209/52 ,  C07D405/04 ,  A61K31/407 ,  A61K31/55 ,  A61K31/403 ,  A61K31/4709 ,  A61P25/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/00

摘要： The present invention relates to a fused ring compound represented by general formula (I), a stereoisomer or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and use thereof. The compound provided in the present invention is useful for treating, preventing and/or controlling various nervous system disorders. The compound provided in the present invention modulates one or more monoamine transporters, inhibits the reuptake of endogenous monoamines such as dopamine, 5-hydroxytryptamine, and norepinephrine (e.g., from the synaptic cleft), and/or modulates the 5-HT 3 receptor.

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：EP2163538A1

公开(公告)日：2010-03-17

申请号：EP08748526.4

申请日：2008-05-22

申请人： Topharman Shanghai Co., Ltd. ,  Weifang Tehua Chemical Co., Ltd.

发明人： ZHU, Fuqiang ,  LI, Haihong ,  WANG, Wenzhong ,  ZHANG, Hui ,  SHEN, Jingshan

IPC分类号： C07C205/06 ,  C07D243/14

CPC分类号： C07C211/29 ,  C07C209/52 ,  C07C233/13 ,  C07C251/24 ,  C07D243/14

摘要： The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydrobenzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o- nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminium hydride.

摘要翻译： 本发明涉及一种制备4-乙酰基-2,3,4,5-四氢苯并[1,4]二氮杂的方法及其中间体。 本发明提供由式I表示的化合物和由式II表示的化合物，以及通过使用式（I）表示的化合物制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂 I，由式II表示的化合物和邻硝基苯甲醛。 本发明具有合成步骤较短，原料容易，操作简单等优点。 而且，通过避免使用昂贵且危险的氢化铝锂，该方法是经济和安全的。