公开(公告)号：EP2772481A8

公开(公告)日：2014-11-26

申请号：EP12843367.9

申请日：2012-10-23

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

发明人： NAN, Fajun ,  LI, Min ,  GAO, Zhaobing ,  CHEN, Fei ,  ZHANG, Yangming ,  ZHOU, Pingzheng ,  HU, Haining ,  XU, Haiyan ,  LIU, Sheng

IPC分类号： C07C271/28 ,  C07C269/04 ,  C07C233/43 ,  C07C231/02 ,  C07D235/26 ,  A61K31/27 ,  A61K31/167 ,  A61K31/4184 ,  A61P25/08 ,  A61P25/04 ,  A61P25/28 ,  A61P25/00 ,  A61P9/10

CPC分类号： C07C271/28 ,  C07C231/00 ,  C07C233/43 ,  C07C233/44 ,  C07C269/04 ,  C07C2601/16 ,  C07D235/26

摘要： The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medcine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.

摘要翻译： 本发明提供具有通式I所示结构的化合物，其药学上可接受的盐，其制备方法及其在制备用于治疗神经系统疾病的药物中的用途。 该化合物或其药物组合物可以用作治疗神经系统疾病的KCNQ钾通道激动剂。 与瑞替加滨相比，现有技术中的化合物，本发明化合物具有相同或更好的治疗效果，更容易合成和储存，且不易氧化变质。

公开(公告)号：EP2772481B1

公开(公告)日：2017-01-18

申请号：EP12843367.9

申请日：2012-10-23

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

发明人： NAN, Fajun ,  LI, Min ,  GAO, Zhaobing ,  CHEN, Fei ,  ZHANG, Yangming ,  ZHOU, Pingzheng ,  HU, Haining ,  XU, Haiyan ,  LIU, Sheng

IPC分类号： C07C271/28 ,  C07C269/04 ,  C07C233/43 ,  C07C231/02 ,  C07D235/26 ,  A61K31/27 ,  A61K31/167 ,  A61K31/4184 ,  A61P25/08 ,  A61P25/04 ,  A61P25/28 ,  A61P25/00 ,  A61P9/10

CPC分类号： C07C271/28 ,  C07C231/00 ,  C07C233/43 ,  C07C233/44 ,  C07C269/04 ,  C07C2601/16 ,  C07D235/26

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：EP3138833A1

公开(公告)日：2017-03-08

申请号：EP15786771.4

申请日：2015-04-22

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

发明人： NAN, Fajun ,  LI, Min ,  GAO, Zhaobing ,  ZHANG, Yangming ,  HU, Haining ,  XU, Haiyan ,  LIU, Huanan ,  PI, Xiaoping

IPC分类号： C07C271/28 ,  C07C269/04 ,  C07C269/06 ,  C07C333/08 ,  C07C275/64 ,  C07C273/18 ,  C07C231/02 ,  C07C235/16 ,  C07C237/04 ,  C07C237/22 ,  C07C233/62 ,  C07C235/74 ,  C07D307/24 ,  A61K31/27 ,  A61K31/277 ,  A61K31/17 ,  A61K31/167 ,  A61K31/341 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28

CPC分类号： C07D307/24 ,  A61K31/167 ,  A61K31/17 ,  A61K31/27 ,  A61K31/277 ,  A61K31/341 ,  C07C231/02 ,  C07C233/62 ,  C07C235/16 ,  C07C235/74 ,  C07C237/04 ,  C07C237/22 ,  C07C237/48 ,  C07C269/04 ,  C07C269/06 ,  C07C271/28 ,  C07C273/18 ,  C07C275/64 ,  C07C333/08 ,  C07C2601/02 ,  C07C2601/14

摘要： The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.