Title:
STILBENE DERIVATIVES AS WELL AS PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2024/061187
Kind Code:
A1
Abstract:
Provided in the present disclosure are stilbene derivatives, a preparation method therefor and the use thereof. Specifically, provided in the present disclosure is the use of compounds represented by formula (I-1), and stereoisomers, pharmaceutically acceptable salts or prodrugs thereof as an aryl hydrocarbon receptor (AHR) regulator. Compared with marketed drug tapinarof, the compounds represented by formula I-1 have greatly improved molecular structure stability under illumination, thus overcoming photoinstability of tapinarof, and solving the problem of tapinarof being liable to degrade under illumination; in addition, the compounds have remarkably improved activity on AHR protein; and finally, the preparation method for the compounds represented by formula I-1 is simple, and can achieve gram-level or kilogram-level preparation. Therefore, the compounds have better prospects in subsequent preparation development, safety and clinical use.
Inventors:
CAI YAXIAN (CN)
JIA JIANMIN (CN)
HAN ZISHENG (CN)
CAI KAIMING (CN)
SUN HUANLIANG (CN)
TANG MENGJIE (CN)
JIA JIANMIN (CN)
HAN ZISHENG (CN)
CAI KAIMING (CN)
SUN HUANLIANG (CN)
TANG MENGJIE (CN)
Application Number:
PCT/CN2023/119575
Publication Date:
March 28, 2024
Filing Date:
September 19, 2023
Export Citation:
Assignee:
THEDERMA SHANGHAI CO LTD (CN)
International Classes:
C07C39/373; C07C37/055; C07C39/21; A61K31/05; A61P17/00; A61P35/00; A61P37/00
Foreign References:
| CN113024357A | 2021-06-25 | |||
| US20210220481A1 | 2021-07-22 | |||
| CN101648851A | 2010-02-17 |
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