公开(公告)号：US20140336252A1

公开(公告)日：2014-11-13

申请号：US14353842

申请日：2012-10-23

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Fei Chen ,  Yangming Zhang ,  Pingzheng Zhou ,  Haining Hu ,  Haiyan Xu ,  Sheng Liu

IPC: C07C271/28 ,  C07C233/44 ,  C07C231/00 ,  C07C269/04

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

Abstract: 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 medicine 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.

Abstract translation: 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。 其化合物或其药物组合物可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，本发明的化合物具有相同或更好的治疗效果，更易于合成和储存，并且不易氧化劣化。

公开(公告)号：US10316008B2

公开(公告)日：2019-06-11

申请号：US15870276

申请日：2018-01-12

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Yangming Zhang ,  Haining Hu ,  Haiyan Xu ,  Huanan Liu ,  Xiaoping Pi

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

Abstract: 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.

公开(公告)号：US20180134677A1

公开(公告)日：2018-05-17

申请号：US15870276

申请日：2018-01-12

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Yangming Zhang ,  Haining Hu ,  Haiyan Xu ,  Huanan Liu ,  Xiaoping Pi

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

CPC classification number: 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

Abstract: 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.

公开(公告)号：US09353048B2

公开(公告)日：2016-05-31

申请号：US14353842

申请日：2012-10-23

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Fei Chen ,  Yangming Zhang ,  Pingzheng Zhou ,  Haining Hu ,  Haiyan Xu ,  Sheng Liu

IPC: C07C261/00 ,  C07C271/28 ,  C07D235/26 ,  C07C233/43 ,  C07C231/00 ,  C07C233/44 ,  C07C269/04

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

Abstract: 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 medicine 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.

Abstract translation: 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。 其化合物或其药物组合物可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，本发明的化合物具有相同或更好的治疗效果，更易于合成和储存，并且不易氧化劣化。

公开(公告)号：US10077245B2

公开(公告)日：2018-09-18

申请号：US15306971

申请日：2015-04-22

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Yangming Zhang ,  Haining Hu ,  Haiyan Xu ,  Huanan Liu ,  Xiaoping Pi

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

CPC classification number: 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

Abstract: 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.