Degradation of IRAK4 by the binding of an E3 ligase ligand and an IRAK4 inhibitor and methods of use thereof

JP2025519417A5Pending Publication Date: 2026-06-03BEIGENE SWITZERLAND GMBH
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
BEIGENE SWITZERLAND GMBH
Filing Date
2023-06-08
Publication Date
2026-06-03

AI Technical Summary

Technical Problem

Current therapies for autoimmune diseases, inflammatory diseases, and neoplastic diseases often struggle to effectively target and modulate the activity of IRAK4, a key regulator of inflammatory responses, beyond just inhibiting its kinase activity.

Method used

Development of novel bifunctional compounds that selectively degrade IRAK4 by linking an IRAK4 inhibitor moiety with an E3 ligase ligand moiety, utilizing the ubiquitin-proteasome pathway to recruit and degrade IRAK4.

Benefits of technology

These compounds demonstrate enhanced potency in inhibiting inflammatory cytokine production compared to traditional small molecule IRAK4 inhibitors, offering potential therapeutic benefits for autoimmune, inflammatory, and neoplastic diseases.

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Abstract

Disclosed herein are novel bifunctional compounds formed by linking an IRAK4 inhibitor moiety and an E3 ligase ligand moiety, compounds that function to recruit and degrade a target protein to an E3 ubiquitin ligase, as well as methods for their preparation and use.
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