公开(公告)号：US20170298080A1

公开(公告)日：2017-10-19

申请号：US15509796

申请日：2015-09-11

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

发明人： Jingshan SHEN ,  Zheng LIU ,  Zhen WANG ,  Guanghui TIAN ,  Jianfeng LI ,  Xiaojun YANG

IPC分类号： C07D495/04 ,  C07D275/04 ,  C07D261/20 ,  C07D333/20 ,  C07D231/56

CPC分类号： C07D495/04 ,  A61K31/33 ,  A61K31/381 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D209/14 ,  C07D231/56 ,  C07D261/20 ,  C07D275/04 ,  C07D307/77 ,  C07D333/20 ,  C07D333/46

摘要： Disclosed are aminosulfonyl-based compounds represented by the general formula I or tautomers, enantiomers, racemates or pharmaceutically acceptable salts thereof, a method for preparing the same, pharmaceutical compositions and uses thereof. The compounds can be used to treat epilepsy, convulsions, obesity and the like.

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：US20220227773A1

公开(公告)日：2022-07-21

申请号：US17615300

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

IPC分类号： C07D487/04 ,  C07D409/04 ,  C07D405/04 ,  C07D209/52

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-HT3 receptor.

公开(公告)号：US20220204431A1

公开(公告)日：2022-06-30

申请号：US17611348

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

IPC分类号： C07C37/16 ,  C07C35/21

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：US20230219993A1

公开(公告)日：2023-07-13

申请号：US17996430

申请日：2021-04-16

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  WUHAN INSTITUTE OF VIROLOGY, CHINESE ACADEMY OF SCIENCE ,  XINJIANG TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY, CHINESE ACADEMIY OF SCIENCES ,  VIGONVITA LIFE SCIENCES CO., LTD.

发明人： Yuanchao XIE ,  Gengfu XIAO ,  Yang HE ,  Leike ZHANG ,  Heji Akber AISA ,  Hualiang JIANG ,  Jingshan SHEN

IPC分类号： C07H7/06 ,  A61P31/14 ,  A61P31/16

CPC分类号： C07H7/06 ,  A61P31/14 ,  A61P31/16 ,  C07B2200/05

摘要： The present invention relates to an antiviral application of nucleoside analogs. Specifically, the present invention relates to uses of nucleoside analogs and a pharmaceutical composition thereof as: (a) inhibitors for inhibiting the replication of coronaviruses, influenza viruses, respiratory syncytial viruses, flaviviridae viruses, filoviridae viruses and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and mitigating diseases caused by coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV) infections. The nucleoside analogs according to the invention may treat and/or prevent and mitigate respiratory infection, pneumonia
(COVID-19) and other related diseases caused by 2019 novel coronavirus infection.

公开(公告)号：US20240309012A1

公开(公告)日：2024-09-19

申请号：US18009981

申请日：2021-01-11

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

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

IPC分类号： C07D491/18 ,  A61K31/4748 ,  A61P31/14 ,  C07D491/22 ,  C07D498/22 ,  C07D519/00

CPC分类号： C07D491/18 ,  A61K31/4748 ,  A61P31/14 ,  C07D491/22 ,  C07D498/22 ,  C07D519/00

摘要： Provided are an isoquinoline compound represented by formula (I), a pharmaceutically acceptable salt thereof, an enantiomer thereof, a diastereomer, a racemate, a crystalline hydrate, and a solvate, as well as an application of a composition thereof in fighting a virus. R1, R2, R3, and R4 are as defined in the description. Further provided are a preparation method for the compound and uses thereof for preparing an inhibitor that inhibits a virus and/or a drug for prophylaxis and/or treatment of an illness related to a respiratory tract infection, pneumonia, etc. caused by a virus.

公开(公告)号：US20230312584A1

公开(公告)日：2023-10-05

申请号：US18033673

申请日：2021-10-21

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

发明人： Jingshan SHEN ,  Yuanchao XIE ,  Leike ZHANG ,  Gengfu XIAO ,  Zhen WANG ,  Hualiang JIANG ,  Huaqiang XU ,  Tianwen HU ,  Guanghui TIAN

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： A salt of nucleoside analog, and crystal form, pharmaceutical composition and use thereof. The salt of nucleoside analog has a structure shown in formula I, wherein X is hydrogen or deuterium; Y is an acid, n is 0.5 to 2, or n is 1. When X is hydrogen or deuterium, Y is hydrogen bromide, and n is 1, the salt of the nucleoside analog exists in the form of a crystal with crystal form I or crystal form A or exists in an amorphous form.

公开(公告)号：US20220289684A1

公开(公告)日：2022-09-15

申请号：US17637637

申请日：2020-08-27

申请人： TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIAMEDICA,CHINESE ACADEMY OF SCIENCES ,  TOPHARMAN TANCHENG CO.,LTD.

发明人： Jingshan SHEN ,  Changliang SUN ,  Fuqiang ZHU ,  Junchi ZHANG ,  Rui LI

IPC分类号： C07D235/18 ,  C07C237/34

摘要： The present disclosure relates to a benzimidazole-substituted phenyl-n-butyramide-based compound and the preparation method thereof. The method of the present disclosure avoids nitration reaction and polyphosphoric acid cyclization reaction, and avoids the generation of a large amount of waste acid reaction solution from the source. The synthesis method embodied in the invention has the advantages of simplicity and high efficiency, mild conditions and few pollutants, etc., and is suitable to be developed as a green and sustainable production process.

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.