USP9X INHIBITORS

The invention relates to macrocyclic polyamide and linear polyamide compounds that inhibit deubiquitinating enzymes (DUBs), including ubiquitin C-terminal hydrolases (UCHs) and the ubiquitin-specific proteases (USPs), particularly USP9X. Inhibition of DUBs, particularly USP9X, induces the targeted d...

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Bibliographic Details
Main Authors BOND, Julian F, MARTINELLI, Richard
Format Patent
LanguageEnglish
French
Published 10.08.2023
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The invention relates to macrocyclic polyamide and linear polyamide compounds that inhibit deubiquitinating enzymes (DUBs), including ubiquitin C-terminal hydrolases (UCHs) and the ubiquitin-specific proteases (USPs), particularly USP9X. Inhibition of DUBs, particularly USP9X, induces the targeted degradation of the substrates of the deubiquitylase, including Mci-1, erbB2, beta-catenin and aldehyde dehydrogenase 1A3. The invention also includes methods of inhibiting DUBs, including USP9X, and methods of treating cancers. L'invention concerne des composés qui inhibent les DUB, en particulier USP9X. L'invention concerne également des procédés d'inhibition de DUB, y compris USP9X, et des procédés de traitement de cancers.
Bibliography:Application Number: WO2023IB50332