The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 12, 2020

Filed:

Mar. 02, 2017
Applicant:

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.l.a. China, Beijing, CN;

Inventors:

Song Li, Beijing, CN;

Junhai Xiao, Beijing, CN;

Xiaoye Zhang, Beijing, CN;

Hongliang Wang, Beijing, CN;

Wu Zhong, Beijing, CN;

Zhibing Zheng, Beijing, CN;

Yunde Xie, Beijing, CN;

Xingzhou Li, Beijing, CN;

Xinbo Zhou, Beijing, CN;

Xiaokui Wang, Beijing, CN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 303/48 (2006.01); C07D 405/12 (2006.01); A61K 31/5377 (2006.01); A61K 31/541 (2006.01); A61K 31/336 (2006.01); A61K 31/4025 (2006.01); A61K 31/4523 (2006.01); A61K 31/427 (2006.01); C07D 417/12 (2006.01); A61P 19/00 (2006.01); A61P 37/02 (2006.01); A61P 35/00 (2006.01); C07D 301/27 (2006.01);
U.S. Cl.
CPC ...
C07D 303/48 (2013.01); A61K 31/336 (2013.01); A61K 31/4025 (2013.01); A61K 31/427 (2013.01); A61K 31/4523 (2013.01); A61K 31/5377 (2013.01); A61K 31/541 (2013.01); A61P 19/00 (2018.01); A61P 35/00 (2018.01); A61P 37/02 (2018.01); C07D 301/27 (2013.01); C07D 405/12 (2013.01); C07D 417/12 (2013.01);
Abstract

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma.


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