公开(公告)号：US20250122148A1

公开(公告)日：2025-04-17

申请号：US18728641

申请日：2023-01-10

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

Inventor： Fajun NAN ,  Zhaobing GAO ,  Wuheng DONG ,  Yueming ZHENG ,  Jintao WANG ,  Xiaoyu ZHOU ,  Huanan LIU ,  Haiyan XU

IPC: C07C269/04 ,  A61K31/27 ,  A61P21/00

Abstract: Disclosed are a high-selectivity KCNQ4 potassium channel agonist of formula I, a preparation method therefor and the use thereof. The compound further improves the KCNQ4 agonistic activity, and is still free of KCNQ2 agonistic activity, thus having excellent KCNQ4/KCNQ2 selectivity. The high-selectivity KCNQ4 agonist overcomes the defect of poor selectivity of existing potassium channel agonists, the activity is relatively increased, and the toxicity is remarkably reduced. The agonist also has a simpler structure and lower product cost, thereby having a better development prospect.

公开(公告)号：US20170081301A1

公开(公告)日：2017-03-23

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: C07D307/24 ,  C07C237/48 ,  C07C275/64 ,  C07C235/16 ,  C07C271/28 ,  C07C333/08

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.