USP7 Inhibitor Compounds for Cancer Treatment

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Solution Overview

Problem

Current treatments for cancers and other disorders, such as neurodegenerative diseases and immunological disorders, are limited in effectively targeting Ubiquitin-Specific Protease 7 (USP7) due to its role in regulating protein stability and cellular pathways, including the p53 signaling pathway, which is often upregulated in cancer cells.

Innovation Solution

Development of a compound of Formula (I) or its pharmaceutically acceptable salt, solvate, N-oxide, or stereoisomer, which inhibits USP7, potentially used in pharmaceutical compositions to treat cancers by modulating USP7 activity, thereby affecting protein stability and cellular pathways.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for cancers and other disorders, then existing therapeutic options are available, but they are limited in effectively targeting USP7 due to its role in regulating protein stability and cellular pathways

Engineering Contradiction:

Improveeffectiveness of targeting USP7VSAvoidlimitation of current treatments

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops novel small molecule compounds with specific chemical structures (Formula I) that bind to and inhibit USP7 enzyme activity. This represents a parameter change from existing treatments to new chemical entities with targeted USP7 inhibition capability, thereby improving the reliability of USP7 targeting while overcoming the limitations of current therapies

Inventive Principle:

Principle #35Parameter changes

2Stability of the object's composition

If USP7 is upregulated in cancer cells leading to suppression of p53, then protein stability is maintained, but this suppresses tumor suppressor function

Engineering Contradiction:

Improveprotein stabilityVSAvoidsuppression of tumor suppressor

Core Design Contradiction:

Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful effect of USP7-mediated protein stabilization into a beneficial therapeutic outcome by using small molecule inhibitors to block USP7 activity. This inhibition restores normal protein degradation pathways, activates p53 tumor suppressor function, and eliminates the harmful suppression caused by USP7 upregulation in cancer cells

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentUS20240158412A1Ubiquitin-specific protease 7 (USP7) inhibitors and uses thereof

Publication Date: 2024.05.16 FAXIAN THERAPEUTICS LLC

AI summary

Described herein are compounds that are useful in treating a USP7-mediated disorder. In some embodiments, the USP7-mediated disorder is cancer.