含氮稠合杂芳双环化合物作为USP1抑制剂及其应用

By developing nitrogen-containing fused heteroaromatic bicyclic compounds as USP1 inhibitors, the problem of poor efficacy of existing USP1 inhibitors in combination therapy has been solved. This has enabled the enhancement of cancer cell sensitivity to DNA cross-linking agents and PARP inhibitors, thereby improving the anti-cancer treatment effect.

CN117412973BActive Publication Date: 2026-07-17IMPACT THERAPEUTICS (SHANGHAI) INC +1

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
IMPACT THERAPEUTICS (SHANGHAI) INC
Filing Date
2022-05-30
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

In the existing technology, USP1 inhibitors have limited efficacy in treating drug-resistant tumors, especially when used in combination with DNA cross-linking agents, making it difficult to improve the sensitivity of cancer cells to DNA cross-linking agents and PARP inhibitors.

Method used

Develop nitrogen-containing fused heteroaromatic bicyclic compounds as USP1 inhibitors, and enhance their killing effect on cancer cells by combining them with DNA cross-linking agents.

Benefits of technology

It increased the sensitivity of cancer cells to DNA cross-linking agents and PARP inhibitors, thereby enhancing the efficacy of anti-cancer treatment.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明提供了由式I所示的含氮稠合杂芳双环化合物及其应用,其中A1、A2、A3、A4、B1、B2、B3、D1、D2、D3、D4、L、Cy1和Cy2如文中所定义。式I的化合物为USP1抑制剂。因此,本公开的化合物可用于治疗USP1调节相关的疾病、障碍和病症,如癌症。
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