Crystals of naphthofuran-substituted glutarimide compounds, production method and use thereof

Naphthofuran-substituted glutarimide crystals are developed to target androgen receptors for degradation via PROTAC compounds, addressing the ineffectiveness of current CRPC treatments and providing a stable therapeutic option for prostate cancer.

JP2025531599APending Publication Date: 2025-09-22SHANGHAI QILU PHARMACEUTICAL RESEARCH & DEVELOPMENT CENTRE LTD
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Patent Information

Application Number
JP2025514650
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-08-29
Filing Date
2023-09-13
Publication Date
2025-09-22

AI Technical Summary

Technical Problem

Current treatments for castration-resistant prostate cancer (CRPC) are ineffective in the long term, and there is a need for more targeted approaches to degrade androgen receptors to manage prostate cancer progression.

Method used

Development of bifunctional proteolysis-targeting chimera (PROTAC) compounds that recruit endogenous proteins to E3 ubiquitin ligases like cereblon for ubiquitination and subsequent degradation of androgen receptors, utilizing specific crystal forms of naphthofuran-substituted glutarimide compounds.

Benefits of technology

The crystal forms of naphthofuran-substituted glutarimide compounds demonstrate stable properties and potential for effective drug discovery, offering a therapeutic approach to treat diseases associated with androgen protein degradation, such as prostate cancer.

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Abstract

The present invention discloses crystals of naphthofuran-substituted glutarimide compounds, a method for producing the same, and uses thereof, and more specifically, the present invention discloses crystals of compound (1) and the production thereof. JPEG2025531599000016.jpg3499
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