一种N-(3-氟苄基)-1H-吲唑-5-胺衍生物及其用途

By designing and synthesizing N-(3-fluorobenzyl)-1H-indazole-5-amine derivatives, the problem of limited efficacy of existing TRK inhibitors against drug-resistant mutations has been solved, achieving effective inhibition of TRK kinases, especially for the treatment of NTRK gene fusion tumors.

CN118561776BActive Publication Date: 2026-07-17SHENYANG PHARMA UNIV
View PDF 0 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHENYANG PHARMA UNIV
Filing Date
2024-05-15
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing TRK inhibitors have limited efficacy against drug resistance mutations, and novel TRK inhibitors need to be designed to maintain efficacy against drug resistance mutations.

Method used

A series of N-(3-fluorobenzyl)-1H-indazole-5-amine derivatives were developed, and compounds with TRK kinase inhibitory activity were prepared through compound design and synthetic routes with specific structures.

Benefits of technology

These compounds exhibit good inhibitory activity against wild-type TRK kinase and various mutants, and can effectively treat NTRK gene fusion tumors, overcoming drug resistance caused by TRK mutations in clinical practice.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure CN118561776B_ABST
    Figure CN118561776B_ABST
Patent Text Reader

Abstract

本发明属于药物化学领域，具体涉及一种具有通式(I)所示结构的N‑(3‑氟苄基)‑1H‑吲唑‑5‑胺衍生物及其制备和应用。本发明提供的通式(I)所示结构的N‑(3‑氟苄基)‑1H‑吲唑‑5‑胺衍生物、其立体异构体、药学上可接受的盐、水合物、溶剂化物或前药具有作为蛋白激酶抑制剂，特别是对原肌球蛋白受体酪氨酸激酶(TRK)的抑制活性。
Need to check novelty before this filing date? Find Prior Art