公开(公告)号：EP4410788A1

公开(公告)日：2024-08-07

申请号：EP22875040.2

申请日：2022-09-29

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Wuhan Institute Of Virology, Chinese Academy of Sciences ,  Hainan Simcere Pharmaceutical Co., Ltd.

发明人： JIANG, Xiangrui ,  XU, Yechun ,  ZHANG, Leike ,  SU, Haixia ,  ZHANG, Qiumeng ,  ZHAO, Wenfeng ,  SHANG, Weijuan ,  SHEN, Jingshan ,  XIAO, Gengfu ,  JIANG, Hualiang

IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D207/26 ,  C07D307/02 ,  C07D309/02 ,  C07D335/02 ,  A61K31/38 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18

CPC分类号： A61K31/38 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18 ,  C07D207/26 ,  C07D307/02 ,  C07D309/02 ,  C07D335/02 ,  C07D403/12 ,  C07D403/14

摘要： The present invention provides a compound represented by formula I, a racemate, an enantiomer, a diastereoisomer and a pharmaceutically acceptable salt thereof, and their use in preventing or treating a related disease caused by coronavirus and/or picornavirus infection.

公开(公告)号：EP4141007A1

公开(公告)日：2023-03-01

申请号：EP21792567.6

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 Sciences ,  XINJIANG TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY, CHINESE ACADEMY OF SCIENCES ,  Vigonvita Life Sciences Co., Ltd.

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

IPC分类号： C07D487/04 ,  C07F9/6561 ,  A61P31/14 ,  A61P31/16 ,  A61K31/53 ,  A61K31/685 ,  A61K31/675

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：EP4446326A1

公开(公告)日：2024-10-16

申请号：EP22903630.6

申请日：2022-12-12

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

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

IPC分类号： C07D491/18 ,  A61K31/4748 ,  A61P31/12 ,  A61P31/14 ,  A61P19/10 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P25/00 ,  A61P27/00 ,  A61P43/00

摘要： The present invention provides a cyclic bisbenzyl tetrahydroisoquinoline compound as represented by formula (I), and a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, a racemate, a crystalline hydrate, and a solvate thereof, wherein R 1 and R 2 are as defined in the description. The present invention further provides a method for preparing the compound and the use of the compound for the preparation of an inhibitor for inhibiting viruses, inflammation, fibrosis and abnormal differentiation of T cells and/or for the preparation of a drug for preventing and/or treating related diseases caused by viruses, such as respiratory tract infections and pneumonia, inflanmmation-related diseases, fibrosis-related diseases and autoimmune diseases.

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：EP3782995A1

公开(公告)日：2021-02-24

申请号：EP19788657.5

申请日：2019-04-18

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

发明人： ZHOU, Bing ,  LUO, Cheng ,  JIANG, Hualiang ,  YANG, Yaxi ,  MEI, Lianghe ,  LU, Wenchao ,  XIAO, Senhao ,  CHEN, Shijie ,  WAN, Shili ,  QIAO, Gang ,  ZHANG, Rukang

IPC分类号： C07D413/06 ,  C07D417/06 ,  C07D413/14 ,  A61K31/4725 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61K31/5513 ,  A61P35/00 ,  A61P35/02 ,  A61P3/00 ,  A61P25/28 ,  A61P29/00

摘要： The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.

公开(公告)号：EP4098653A1

公开(公告)日：2022-12-07

申请号：EP20916984.6

申请日：2020-03-26

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Frontier Biotechnologies Inc.

发明人： LIU, Hong ,  LI, Jian ,  DAI, Wenhao ,  PENG, Jingjing ,  XIE, Xiong ,  HU, Shulei ,  LI, Chunpu ,  XU, Yechun ,  YANG, Haitao ,  ZHANG, Leike ,  SU, Haixia ,  JIANG, Hualiang ,  JIN, Zhenming ,  XIAO, Gengfu ,  CHEN, Kaixian

IPC分类号： C07D405/12 ,  A61K31/437

摘要： Use of an aldehyde-based compound as represented by general formula I, a pharmaceutical composition, a pharmaceutical salt, an enantiomer, a diastereomer and a racemic compound thereof as a novel coronavims 2019 (2019-nCov) 3CL protease inhibitor in preparation of a medicament for treating and/or preventing and relieving respiratory tract infections, pneumonia and other related diseases caused by the novel coronavims infection 2019.

公开(公告)号：EP4067345A1

公开(公告)日：2022-10-05

申请号：EP20893986.8

申请日：2020-11-24

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Jiangsu Kanion Pharmaceutical Co., Ltd.

发明人： LIU, Hong ,  ZHOU, Yu ,  ZHANG, Haiyan ,  FU, Yan ,  LI, Jian ,  JIANG, Hualiang ,  TANG, Xican ,  CHEN, Kaixian

IPC分类号： C07D211/38 ,  A61K31/445

摘要： The present invention provides a crystalline form of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B and crystalline form C of 2-((1-(2-fluorobenzyl)-4-fluoropiperidin-4-yl) methylene)-5, 6-dimethoxy-2, 3-dihydro-1-indanone.The crystalline form of the present invention does not contain water and solvent, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.

公开(公告)号：EP3521274A1

公开(公告)日：2019-08-07

申请号：EP17854729.5

申请日：2017-09-19

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

发明人： LIU, Hong ,  WANG, Jiang ,  ZHOU, Shengbin ,  PENG, Panfeng ,  NIAN, Yong ,  WANG, Shuni ,  SHU, Shuangjie ,  SHEN, Hao ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D207/16 ,  C07D409/12 ,  C07F15/04 ,  C07C227/34 ,  C07C229/34 ,  C07D401/04

摘要： Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β 3 -amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.

公开(公告)号：EP3470415A1

公开(公告)日：2019-04-17

申请号：EP17802189.5

申请日：2017-05-24

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

发明人： JIANG, Hualiang ,  LIU, Hong ,  GENG, Meiyu ,  ZHENG, Mingyue ,  AI, Jing ,  WANG, Yulan ,  WU, Xiaowei ,  LI, Shuangjie ,  PENG, Xia ,  LI, Chunpu ,  CHEN, Kaixian ,  WANG, Bao

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541

摘要： The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a compound as represented by formula (I). Various radicals are as defined in the specification. The compound provided by the invention effectively inhibits an activity of an FGFR kinase, and can be used to manufacture a pharmaceutical product for treating a disease related to the activity of the FGFR kinase.

公开(公告)号：EP3459948A1

公开(公告)日：2019-03-27

申请号：EP17798743.5

申请日：2017-05-17

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

发明人： LIU, Hong ,  ZHOU, Yu ,  XIA, Wenjing ,  ZHANG, Dong ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D471/04 ,  A61K31/4545 ,  A61K31/437 ,  A61K31/496 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/04

摘要： The present invention provides a fluorine-containing triazolopyridine represented by formula (I) and a racemate, R-stereoisomer, S-stereoisomer, pharmaceutically acceptable salt, or mixture thereof. The triazolopyridine can be used as a positive allosteric modulator of an mGluR2, and is highly selective in activating the mGluR2, exerting no activation or very limited activation of other homologous metabotropic glutamate receptor. The triazolopyridine can thus be used to prepare a product for treating an mGluR2-related disease, such as a central nervous system disease or neurological disease.