公开(公告)号：EP4234557A1

公开(公告)日：2023-08-30

申请号：EP21885029.5

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

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P31/14

摘要： The present disclosure pertains to the technical field of medicine, and relates to salt of nucleoside analog, and crystal form, pharmaceutical composition and use thereof. Specifically, the salt of nucleoside analog has a structure shown in formula I, wherein X is hydrogen or deuterium; Y is an acid, preferably hydrogen bromide, hydrogen chloride, nitric acid, methanesulfonic acid or maleic acid, n is 0.5 to 2, preferably 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, which has good appearance as solid material, high stability, good solubility, low hygroscopicity, etc., and can be used in the preparation of medicaments for the treatment and/or alleviation of related diseases caused by viruses (especially SARS-CoV-2).

公开(公告)号：EP3957640A1

公开(公告)日：2022-02-23

申请号：EP20791301.3

申请日：2020-04-20

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

发明人： XU, Huaqiang ,  LI, Jia ,  SHI, Jingjing ,  ZANG, Yi ,  SUN, Dandan ,  LIU, Mingliang ,  XIE, Rongrong ,  YOU, Erli ,  GAO, Lixin ,  TAN, Qian

IPC分类号： C07D487/08 ,  A61P3/00 ,  A61P29/00 ,  A61P1/16 ,  A61P3/06 ,  A61P3/10 ,  A61K31/454 ,  A61K31/4245 ,  A61K31/439 ,  A61K31/55

摘要： An FXR small molecule agonist and a preparation method therefor and a use thereof, having a structure as shown in formula (I). The compound represented by formula (I) has FXR agonistic activity and is capable of preparing drugs for treatment of FXR-related diseases.

公开(公告)号：EP4223757A1

公开(公告)日：2023-08-09

申请号：EP21874475.3

申请日：2021-09-28

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

发明人： XU, Huaqiang ,  LI, Jia ,  SHI, Jingjing ,  ZANG, Yi ,  SUN, Dandan ,  LIU, Mingliang ,  XIE, Rongrong ,  YOU, Erli ,  GAO, Lixin ,  TAN, Qian

IPC分类号： C07D471/08 ,  A61K31/46

摘要： A strong FXR small-molecule agonist, and a preparation method therefor and use thereof, the structure of the agonist being represented by formula (I). In the formula, each substituent is as defined in the description and the claims. The compound provided by the present invention has the advantages of high FXR agonist activity, simple synthesis, easily available raw materials and the like, and can be used for preparing medicines for treating FXR related diseases.