公开(公告)号：EP2786998B1

公开(公告)日：2018-07-25

申请号：EP12853993.9

申请日：2012-10-23

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

发明人： LIU, Hong ,  LI, Jia ,  LI, Jian ,  LI, Jingya ,  WANG, Jiang ,  SU, Mingbo ,  LIAN, Jie ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61K31/55 ,  A61P3/10

CPC分类号： C07D495/04

摘要： Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

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.

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：EP3438108A1

公开(公告)日：2019-02-06

申请号：EP17773232.8

申请日：2017-03-29

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

发明人： LIU, Hong ,  WANG, Yiping ,  ZHAO, Fei ,  ZHAO, Jing ,  WANG, Jiang ,  XI, Cong ,  WU, Chenglin ,  SHEN, Hao ,  HAN, Xu ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D471/14 ,  C07D491/22 ,  C07D495/22 ,  A61K31/4745 ,  A61P3/06 ,  A61P3/00 ,  A61P1/16 ,  A61P9/10 ,  A61P3/04

摘要： The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.