Pyrazolo[1,5-a]pyrimidine derivatives, their preparation methods and uses

By developing pyrazolo[1,5-a]pyrimidine derivatives as PI3Kα inhibitors, the problems of drug resistance and toxicity of existing PI3Kα inhibitors in cancer treatment have been solved, and effective treatment of cancers with dysregulated PI3Kα signaling pathways has been achieved.

CN116987083BActive Publication Date: 2026-05-26杭州贝奥科瑞生物科技有限公司
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Patent Information

Application Number
CN202210442580.4
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2022-04-25
Publication Date
2026-05-26
Estimated Expiration
2042-04-25

AI Technical Summary

Technical Problem

Existing PI3Kα inhibitors exhibit drug resistance and lack specificity in cancer treatment, leading to intolerable toxicity and an inability to effectively inhibit cancers caused by dysregulation of the PI3Kα signaling pathway.

Method used

A pyrazolo[1,5-a]pyrimidine derivative and its tautomers, stereoisomers or pharmaceutically acceptable salts thereof have been developed as PI3Kα inhibitors for the treatment of cancers caused by dysregulation of the PI3Kα signaling pathway, such as breast cancer, lung cancer or rectal cancer.

Benefits of technology

This compound can effectively inhibit the PI3Kα signaling pathway, exhibiting high selectivity and novelty. It provides a new strategy for treating cancers caused by PI3Kα signaling pathway dysregulation and has promising application prospects.

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Abstract

This invention relates to the pyrazolo[1,5-a]pyrimidine derivative of Formula I, its preparation method, and its uses. It can be used as a PI3Kα inhibitor to treat cancers caused by dysregulation of the PI3Kα signaling pathway, such as breast cancer, lung cancer, or rectal cancer. Furthermore, the preparation method of this compound is simple and it has certain application prospects.
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