Fused heterocyclic compound

Small organic compounds targeting USP1 inhibit its activity, addressing the need for therapeutic agents in cancer and metabolic disorders by leveraging USP1's role in DNA repair and metabolic regulation.

WO2026127574A1PCT designated stage Publication Date: 2026-06-18AIGEN SCIENCES INC

Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
AIGEN SCIENCES INC
Filing Date
2025-12-09
Publication Date
2026-06-18

AI Technical Summary

Technical Problem

There is a need for a novel small organic molecule compound capable of inhibiting the activity of the deubiquitination enzyme USP1, which is overexpressed in various cancer cells and plays a crucial role in DNA damage repair, offering potential therapeutic targets for cancer and metabolic disorders.

Method used

Development of small organic compounds defined by specific chemical formulas (e.g., Formula 1, Formula 2, Formula 3) that inhibit USP1 activity, including their tautomers, stereoisomers, and pharmaceutically acceptable salts, targeting USP1 for selective inhibition in cancer treatment and metabolic diseases.

🎯Benefits of technology

The compounds effectively inhibit USP1 activity, demonstrating synthetic lethality with BRCA activity, providing therapeutic potential for treating BRCA-mutated cancers and metabolic disorders such as diabetes and obesity.

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Abstract

Provided is a compound represented by chemical formula (1) or a tautomer thereof or a stereoisomer thereof, and a pharmaceutically acceptable salt thereof. The compound according to the present invention can inhibit the activity of ubiquitin-specific protease 1. In formula 1, X1 to X4, R1, L, Z, (I), (II), and (III) are as defined in the present specification.
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