一种DNA聚合酶theta抑制剂及其应用

By providing a novel DNA polymerase theta inhibitor, the problem of the single structure of existing inhibitors is solved, and effective inhibition of Polθ is achieved, which has the potential for anti-cancer therapy, especially in reducing the risk of cell death in the case of BRCA1 or BRCA2 mutations.

CN118451067BActive Publication Date: 2026-07-17SHANGHAI APEIRON THERAPEUTICS CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI APEIRON THERAPEUTICS CO LTD
Filing Date
2022-12-30
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing Polθ inhibitors have relatively simple structures and cannot effectively inhibit the activity of DNA polymerase theta.

Method used

A novel DNA polymerase theta inhibitor is provided, comprising compounds whose structures are represented by specific chemical formulas II or III, and their pharmaceutically acceptable salts or solvates, which can effectively inhibit the activity of Polθ.

Benefits of technology

This inhibitor can significantly suppress the activity of Polθ and has potential anti-cancer therapeutic effects, especially in the case of HR deficiency caused by BRCA1 or BRCA2 mutations, reducing the accumulation of toxic RAD51 intermediates and reducing the risk of cell death.

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Abstract

本发明公开了一种DNA聚合酶theta抑制剂及其应用。本发明具体提供了如式(I)或式(II)所示的化合物,或其互变异构体、其立体异构体、前述任一者的药学上可接受的盐或前述任一者的溶剂合物。其对Polθ有较好的抑制作用。
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