Title:
MEMANTINE UREA DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN PREPARATION OF MEDICAMENT FOR TREATING SOLUBLE EPOXIDE ENZYME-MEDIATED DISEASES
Document Type and Number:
WIPO Patent Application WO/2024/104411
Kind Code:
A1
Abstract:
The present application provides a memantine urea derivative, a preparation method therefor, and use thereof, which relate to the technical field of pharmaceutics. The memantine urea derivative provided by the present application has a typical urea structure as a primary pharmacophore of sEH. Molecular docking shows that the memantine moiety acts as a hydrophobic fragment to generate hydrophobic interactions with a receptor. Notably, when R1 and R2 are all methyl groups (i.e., 3,5-dimethyl substitution), the van der Waals force can be enhanced. Therefore, the memantine urea derivative provided by the present application has high inhibitory activity against human sEH (HsEH) and murine sEH (MsEH), and can be used as an sEH inhibitor for preparing a medicament for treating a soluble epoxide enzyme-mediated disease.
Inventors:
CHEN GUOLIANG (CN)
WANG GAOHUA (CN)
CHEN YUANGUANG (CN)
LIU ZHONGBO (CN)
CAO RUOLIN (CN)
XU HUASHEN (CN)
CHEN LU (CN)
WANG GAOHUA (CN)
CHEN YUANGUANG (CN)
LIU ZHONGBO (CN)
CAO RUOLIN (CN)
XU HUASHEN (CN)
CHEN LU (CN)
Application Number:
PCT/CN2023/131933
Publication Date:
May 23, 2024
Filing Date:
November 16, 2023
Export Citation:
Assignee:
UNIV SHENYANG PHARMACEUTICAL (CN)
WANG GAOHUA (CN)
WANG GAOHUA (CN)
International Classes:
C07D211/60; A61K31/445; A61K31/495; A61P3/10; A61P9/00; A61P11/00; A61P13/12; A61P25/00; A61P29/00; C07C273/18; C07C275/42; C07D243/08; C07D295/205; C07D401/06
Foreign References:
| CN115819328A | 2023-03-21 | |||
| CN116217511A | 2023-06-06 | |||
| CN116947740A | 2023-10-27 | |||
| CN113185451A | 2021-07-30 | |||
| CN115141123A | 2022-10-04 | |||
| CN113402447A | 2021-09-17 | |||
| CN101495119A | 2009-07-29 | |||
| CN111423396A | 2020-07-17 | |||
| CN102464631A | 2012-05-23 |
Other References:
DU FANGYU, CAO RUOLIN; CHEN U.; SUN JIANWEN; SHI YAJIE; FU YANG; HAMMOCK BRUCE D.; ZHENG ZHONGHUI; LIU ZHONGBO; CHEN GUOLIANG: "Structure-guided discovery of potent and oral soluble epoxide hydrolase inhibitors for the treatment of neuropathic pain", ACTA PHARMACEUTICA SINICA B, ELSEVIER, vol. 12, no. 3, 1 March 2022 (2022-03-01), pages 1377 - 1389, XP093170613, ISSN: 2211-3835, DOI: 10.1016/j.apsb.2021.09.018
DATABASE Registry 8 April 2018 (2018-04-08), ANONYMOUS: "STNext", XP093170614, Database accession no. 2207978-09-2
DATABASE Registry 8 April 2018 (2018-04-08), ANONYMOUS: "STNext", XP093170614, Database accession no. 2207978-09-2
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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