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公开(公告)号:US11384073B2
公开(公告)日:2022-07-12
申请号:US17127350
申请日:2020-12-18
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: Jingshan Shen , Yang He , Zhen Wang , Jianfeng Li , Yongjian Liu , Jin Suo , Guanghui Tian , Weiming Chen , Feipu Yang , Yu Wang , Xiangrui Jiang , Rongxia Zhang , Hualiang Jiang
IPC分类号: C07D409/12
摘要: The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation.
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公开(公告)号:US10100044B2
公开(公告)日:2018-10-16
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: C07D333/70 , C07D409/12 , C07D333/54
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.
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公开(公告)号:US20210309648A1
公开(公告)日:2021-10-07
申请号:US17127350
申请日:2020-12-18
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: Jingshan Shen , Yang He , Zhen Wang , Jianfeng Li , Yongjian Liu , Jin Suo , Guanghui Tian , Weiming Chen , Feipu Yang , Yu Wang , Xiangrui Jiang , Rongxia Zhang , Hualiang Jiang
IPC分类号: C07D409/12
摘要: The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation.
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4.
公开(公告)号:US11434226B2
公开(公告)日:2022-09-06
申请号:US16736300
申请日:2020-01-07
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: Jingshan Shen , Yang He , Weiming Chen , Jianfeng Li , Guanghui Tian , Xudong Gong , Zhen Wang , Rongxia Zhang , Yongjian Liu , Hualiang Jiang
IPC分类号: C07D403/12 , A61K45/06
摘要: The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof.
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公开(公告)号:US10174011B2
公开(公告)日:2019-01-08
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 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D519/00 , A61K31/496 , A61K31/519 , A61K31/4709 , A61K31/517 , A61K31/538 , A61K31/5415 , A61K31/55
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.
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