公开(公告)号：US20160272624A1

公开(公告)日：2016-09-22

申请号：US15030331

申请日：2014-10-20

申请人： SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. ,  TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Zheng LIU ,  Chunhui WU ,  Yongjian LIU ,  Rongxia ZHANG ,  Yang HE ,  Guanghui TIAN ,  Jingshan SHEN

IPC分类号： C07D409/12 ,  C07D333/70 ,  C07D333/54

CPC分类号： C07D409/12 ,  C07D333/54 ,  C07D333/70

摘要： The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

摘要翻译： 本发明涉及制备布立乐拉唑类似物，关键中间体及其盐的方法，具体地说，本发明涉及一种制备布立乐拉唑的新方法，其类似物，关键中间体及其盐，以及关键中间体， 及其盐在制备过程中提供。 制备方法反应条件温和，中间体稳定，操作方便，使用便宜，易于使用的试剂，节省了合成成本，缩短了生产周期，提高了产量和产品质量，适用于质量 生产。

公开(公告)号：US20170158680A1

公开(公告)日：2017-06-08

申请号：US15124264

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

IPC分类号： C07D409/12 ,  C07D495/04 ,  C07D471/04

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

摘要： The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.

公开(公告)号：US20160102047A1

公开(公告)日：2016-04-14

申请号：US14975427

申请日：2015-12-18

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  TOPHARMAN SHANGHAI CO., LTD.

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

IPC分类号： C07C235/34 ,  C07C59/64 ,  C07C59/68

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

摘要翻译： 本发明涉及式I所示的（2R，3R）-3-（3-取代苯基）-2-甲基正戊酰胺化合物及其制备方法，其中取代基如本说明书中所定义 ，本发明还涉及上述化合物用于制备他喷他多II或其药学上可接受的盐的用途，以及参与制备方法的中间体

公开(公告)号：US20200255421A1

公开(公告)日：2020-08-13

申请号：US16639394

申请日：2018-08-14

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMYOF SCIENCES ,  TOPHARMAN SHANGHAI CO., LTD.

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

IPC分类号： C07D455/03 ,  A61P25/20 ,  C07D498/14

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.