一种3位含氧基取代的6H-二苯并[b,d]吡喃类衍生物及其制备方法和应用

By designing a 6H-dibenzo[b,d]pyran derivative with an oxygen-substituted 3-position, the specific binding to PI3Kδ kinase is enhanced, providing a novel inhibitor with strong inhibitory activity and selectivity, thus solving the problems of single structure and large toxic side effects of existing PI3Kδ inhibitors.

CN117736199BActive Publication Date: 2026-07-17XI AN JIAOTONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
XI AN JIAOTONG UNIV
Filing Date
2023-12-18
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

The existing PI3Kδ inhibitors have a single core structure, resulting in significant toxic side effects and adverse reactions during clinical use, thus limiting their applicability.

Method used

A novel inhibitory core structure was developed by developing a 3-oxygen-substituted 6H-dibenzo[b,d]pyran derivative that enhances the interaction with the catalytic active and affinity regions of PI3Kδ kinases and binds to specific amino acids.

Benefits of technology

This has expanded the core structural types of PI3Kδ inhibitors, improved selectivity and reduced toxic side effects, and broadened the range of indications.

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Abstract

本发明公开一种3位含氧基取代的6H‑二苯并[b,d]吡喃类衍生物及其制备方法和应用，该3位含氧基取代的6H‑二苯并[b,d]吡喃类衍生物，包括通式(I)所示的化合物、通式(I)的立体异构体或其盐：其中，R1基为氮杂环基以及取代的氮杂环基；R2基为杂环基、取代的杂环基、杂芳基以及取代的杂芳基中的任意一个。
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