Novel compounds

By developing a new compound with a specific structure, we solved the problem of existing DUB inhibitors that have not successfully entered clinical application, achieved effective inhibition of UCHL1, provided a new DUB inhibitor for cancer treatment, and reduced the cost of drugs. Risk of drug resistance and toxicity.

CN111592534AActive Publication Date: 2020-08-28MISSION THERAPEUTICS LTD
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Patent Information

Application Number
CN202010193668.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2014-09-23
Filing Date
2015-09-22
Publication Date
2020-08-28
Estimated Expiration
2035-09-22

AI Technical Summary

Technical Problem

Existing DUB inhibitors have not yet successfully entered clinical application, and existing cancer treatment targeted drugs such as bortezomib have drug resistance and toxicity problems. New DUB inhibitors need to be developed to replace traditional targeting strategies.

Method used

Provide a new compound, the specific structure is a 5-10 membered heteroaryl ring compound with specific substituents, used to inhibit ubiquitin C-terminal hydrolase UCHL1, through the pharmaceutical form of the compound or its pharmaceutically acceptable salt form , as a DUB inhibitor for the treatment of cancer and other indications.

Benefits of technology

This compound effectively inhibits the activity of UCHL1 and has potential benefits in the treatment of cancer and other diseases, especially in reducing drug resistance and toxicity while improving therapeutic efficacy.

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Abstract

The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
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