公开(公告)号：EP3835296A1

公开(公告)日：2021-06-16

申请号：EP19847084.1

申请日：2019-08-09

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

发明人： LIU, Hong ,  JIANG, Shibo ,  DAI, Wenhao ,  LU, Lu ,  PENG, Jingjing ,  XIA, Shuai ,  WANG, Jiang ,  LI, Jian ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D241/44 ,  C07D209/42 ,  A61K31/498 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4025 ,  A61K31/4525 ,  A61K31/4709 ,  A61P31/14

摘要： A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.

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：EP3546454A1

公开(公告)日：2019-10-02

申请号：EP17874582.4

申请日：2017-11-17

申请人： East China University of Science and Technology ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： LI, Jian ,  LAN, Lefu ,  LI, Baoli ,  CHEN, Feifei ,  NI, Shuaishuai ,  LIU, Yifu ,  WEI, Hanwen ,  MAO, Fei ,  ZHU, Jin

IPC分类号： C07D307/82 ,  C07D333/66 ,  A61K31/343 ,  A61K31/381 ,  A61P31/04 ,  A61P31/10

摘要： Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.

公开(公告)号：EP3434677A1

公开(公告)日：2019-01-30

申请号：EP17769393.4

申请日：2017-03-20

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

发明人： LIU, Hong ,  WANG, Jiang ,  LI, Jian ,  LI, Jia ,  LI, Jingya ,  JIANG, Hualiang ,  LUO, Xiaomin ,  CHEN, Kaixian

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P3/10

摘要： A polymorph of (R) methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothioph ene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.

公开(公告)号：EP3315502A1

公开(公告)日：2018-05-02

申请号：EP16813720.6

申请日：2016-06-23

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

发明人： LIU, Hong ,  LI, Jia ,  WANG, Jiang ,  LI, Jingya ,  CHEN, Hui ,  LI, Dan ,  LI, Jian ,  WANG, Yibing ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D493/10 ,  A61K31/35 ,  A61K31/381 ,  A61K31/427 ,  A61K31/4436 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10

CPC分类号： C07H19/01 ,  A61K31/35 ,  A61K31/381 ,  A61K31/427 ,  A61K31/4436 ,  A61P3/08 ,  C07D493/10

摘要： The present invention provides C, O-spiro aryl glycoside compounds, preparation therefor and use thereof. Specifically provided are the compounds represented by the formula (I), wherein the definitions of each group are described in the specification. The compound can be used as SGLT2 inhibitors in preparing the pharmaceutical compositions for treating diseases such as diabetes, atherosclerosis, adiposity and etc.

摘要翻译： 本发明提供C，O-螺芳基糖苷化合物，其制备方法及其用途。 具体提供了由式（I）表示的化合物，其中每个基团的定义在说明书中描述。 该化合物可以作为SGLT2抑制剂用于制备治疗糖尿病，动脉粥样硬化，肥胖症等疾病的药物组合物。

公开(公告)号：EP3091013A1

公开(公告)日：2016-11-09

申请号：EP14877091.0

申请日：2014-12-29

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

发明人： LIU, Hong ,  WU, Beili ,  ZHENG, Yongtang ,  XIE, Xin ,  JIANG, Hualiang ,  PENG, Panfeng ,  LUO, Ronghua ,  LI, Jing ,  LI, Jian ,  ZHU, Ya ,  CHEN, Ying ,  ZHANG, Haonan ,  YANG, Liumeng ,  ZHOU, Yu ,  CHEN, Kaixian

IPC分类号： C07D409/14 ,  C07D451/04 ,  C07D401/14 ,  C07D519/00 ,  A61K31/454 ,  A61K31/46 ,  A61K31/4545 ,  A61P31/18

CPC分类号： C07D519/00 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  C07D451/04 ,  A61K2300/00

摘要： Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

摘要翻译： 提供的是1-（3-氨基丙基）substituiertem环状胺化合物由式（I），其药学上可接受的盐，对映异构体，非对映体，种族匹配和混合物作为代表，以及它们的合成的方法，所述1-（3-氨基丙基）substituiertem环状胺 通过使用芳族杂环甲醛作为原料化合物。 所述化合物可被用作CCR5拮抗剂为HIV感染症的治疗。

公开(公告)号：EP3798218A1

公开(公告)日：2021-03-31

申请号：EP19806732.4

申请日：2019-05-21

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

发明人： LIU, Hong ,  GENG, Meiyu ,  ZHOU, Yu ,  DING, Jian ,  FANG, Feifei ,  AI, Jing ,  LI, Jian ,  PENG, Xia ,  JIANG, Hualiang ,  JI, Yinchun ,  CHEN, Kaixian

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D453/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5025 ,  A61K31/4985 ,  A61K31/4709 ,  A61P35/00

摘要： Provided are a class of fused-cyclic pyrazolone formamide compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided is a compound having the structure as shown in formula (I) (with each group defined in the description). The compound can be used as an AXL inhibitor in the preparation of a pharmaceutical composition for treating tumors.

公开(公告)号：EP3284738A1

公开(公告)日：2018-02-21

申请号：EP16779633.3

申请日：2016-04-15

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

发明人： LIU, Hong ,  ZHOU, Yu ,  ZHANG, Dong ,  LI, Jian ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D213/56 ,  C07D401/12 ,  C07D277/30 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D417/06 ,  C07D213/82 ,  C07D213/75 ,  C07D239/26

CPC分类号： C07D487/04 ,  C07D213/56 ,  C07D213/75 ,  C07D213/82 ,  C07D231/56 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D277/30 ,  C07D277/32 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D491/10

摘要： The present invention relates to the fields of pharmaceutical chemistry and drug therapy, and particularly relates to a compound of formula I, and a preparation method and use thereof as a negative allosteric modulator of a metabotropic glutamate receptor (mG1uR) subtype 5.

摘要翻译： 本发明涉及药物化学和药物治疗领域，具体涉及作为代谢型谷氨酸受体（mG1uR）亚型5的负变构调节剂的式I化合物及其制备方法和用途。

公开(公告)号：EP3284738B1

公开(公告)日：2020-11-25

申请号：EP16779633.3

申请日：2016-04-15

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

发明人： LIU, Hong ,  ZHOU, Yu ,  ZHANG, Dong ,  LI, Jian ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D213/56 ,  C07D401/12 ,  C07D277/30 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D417/06 ,  C07D213/82 ,  C07D213/75 ,  C07D239/26 ,  C07D401/10 ,  C07D277/32