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1. (WO2017148417) 2,3-EPOXY SUCCINYL DERIVATIVE, PREPARATION METHOD THEREFOR, AND USES THEREOF

Pub. No.:    WO/2017/148417    International Application No.:    PCT/CN2017/075453
Publication Date: Sat Sep 09 01:59:59 CEST 2017 International Filing Date: Fri Mar 03 00:59:59 CET 2017
IPC: C07D 303/48
C07D 301/00
C07D 405/12
A61K 31/336
A61K 31/4523
A61K 31/4025
A61K 31/5377
A61K 31/541
A61K 31/427
A61P 35/00
Applicants: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA
中国人民解放军军事医学科学院毒物药物研究所
Inventors: LI, Song
李松
XIAO, Junhai
肖军海
ZHANG, Xiaoye
张晓叶
WANG, Hongliang
王宏亮
ZHONG, Wu
钟武
ZHENG, Zhibing
郑志兵
XIE, Yunde
谢云德
LI, Xingzhou
李行舟
ZHOU, Xinbo
周辛波
WANG, Xiaokui
王晓奎
Title: 2,3-EPOXY SUCCINYL DERIVATIVE, PREPARATION METHOD THEREFOR, AND USES THEREOF
Abstract:
Disclosed in the present invention are a 2,3-epoxy succinyl derivative, a preparation method therefor, and uses thereof. Specifically, disclosed in the present invention are a compound represented by formula (1), a raceme thereof, an optical isomer thereof, a solvate thereof or a pharmaceutical acceptable salt thereof. The compound in the present invention has good inhibitory activity and/or selectivity on cathepsins and especially on cathepsin B, and can be used for treating multiple kinds of diseases related to cathepsins, such as osteoporosis, rheumatoid arthritis and osteoarthritis related to cathepsin K, Ebola virus infection, degenerative diseases and autoimmune diseases related to cathepsins L and S, especially tumor diseases related to cathepsin B, such as stomach cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, glioma and melanoma.