公开(公告)号：US20160272624A1

公开(公告)日：2016-09-22

申请号：US15030331

申请日：2014-10-20

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

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

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

CPC classification number: C07D409/12 ,  C07D333/54 ,  C07D333/70

Abstract: 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.

Abstract translation: 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：US20230312584A1

公开(公告)日：2023-10-05

申请号：US18033673

申请日：2021-10-21

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

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

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07B2200/13

Abstract: 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：US11434226B2

公开(公告)日：2022-09-06

申请号：US16736300

申请日：2020-01-07

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

Inventor： Jingshan Shen ,  Yang He ,  Weiming Chen ,  Jianfeng Li ,  Guanghui Tian ,  Xudong Gong ,  Zhen Wang ,  Rongxia Zhang ,  Yongjian Liu ,  Hualiang Jiang

IPC: C07D403/12 ,  A61K45/06

Abstract: 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.

公开(公告)号：US20170158680A1

公开(公告)日：2017-06-08

申请号：US15124264

申请日：2015-03-09

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

Inventor： 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: C07D409/12 ,  C07D495/04 ,  C07D471/04

CPC classification number: C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

Abstract: 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.