2-[(6H-二苯并[b,d]吡喃-3-基)氧]酰胺类衍生物及其制备方法和应用

By designing 2-[(6H-dibenzo[b,d]pyran-3-yl)oxy]amide derivatives, the binding ability with PI3Kδ kinase is enhanced, which solves the problems of single structure and large toxic side effects of existing PI3Kδ inhibitors, and achieves better inhibitory activity and safety.

CN117736200BActive Publication Date: 2026-07-17XI AN JIAOTONG UNIV

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 core structure of existing PI3Kδ inhibitors is of a single type, resulting in significant toxic side effects and a limited range of indications.

Method used

A 2-[(6H-dibenzo[b,d]pyran-3-yl)oxy]amide derivative was developed, which enhances inhibitory activity and expands the core structural types of inhibitors by interacting with the catalytic active and affinity regions of PI3Kδ kinase through a specific structure.

Benefits of technology

This derivative enhances the specific binding to PI3Kδ kinase, reduces toxic side effects, and expands the indications for the inhibitor.

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Abstract

本发明公开一种2‑[(6H‑二苯并[b,d]吡喃‑3‑基)氧]酰胺类衍生物及其制备方法和应用,该2‑[(6H‑二苯并[b,d]吡喃‑3‑基)氧]酰胺类衍生物包括通式(I)所示的化合物、通式(I)的立体异构体或其盐:其中,R1基为氢原子、甲基、乙基、苄基中的任意一个;R2基为氨基、取代的氨基、氮杂环基、取代的氮杂环基、吗啉基以及取代的吗啉基中的任意一个;R3基为取代的杂环基或取代嘧啶基;当所述R2基为氨基时,所述R1基为苄基。
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