Coumarin-modified androgen for treating prostate cancer

JP2025098059A5Inactive Publication Date: 2025-10-03HEALTH RESEARCH INC +1
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Patent Information

Application Number
JP2025035100
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2019-08-22
Filing Date
2025-03-06
Publication Date
2025-10-03
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Current treatments for castration-resistant prostate cancer (CRPC) are limited in efficacy due to the persistence of androgen biosynthesis pathways, particularly the backdoor pathways that produce dihydrotestosterone (DHT), and the development of resistance mechanisms such as AR-V7, rendering existing anti-androgens ineffective.

Method used

Development of androstane and dihydrotestosterone compounds functionalized with carbocyclic or heterocyclic groups, including coumarin-containing rings, that inhibit redox enzymes in the backdoor pathway, compete with AR-LBD binding, and disrupt AR function, potentially degrading AR to overcome resistance.

Benefits of technology

These compounds effectively inhibit DHT biosynthesis, suppress AR-V7-expressing cell lines, and degrade AR, offering a more significant clinical impact than existing treatments by impairing AR transactivation and dimerization, thereby reducing prostate cancer cell proliferation.

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Abstract

To provide novel therapeutic methods for prostate cancer.SOLUTION: Provided are androstane and dihydrotestosterone compounds functionalized with carbocyclic groups or heterocyclic groups that may be saturated or unsaturated. The compounds may be used in methods of inhibiting cell growth of malignant cells and / or hyperplastic cells and / or treating individuals having diseases associated with malignant cell growth (e.g., cancer, such as, for example, prostate cancer) and / or hyperplastic cell growth and / or molecular imaging of malignant cells and / or hyperplastic cells and / or inducing degradation of a target protein. Also provided are compositions.SELECTED DRAWING: Figure 2
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