CSF-1R Kinase Inhibitor Patent Grant

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Use of CSF-1R kinase inhibitor

Grant US12605375B2 Kind: B2 Apr 21, 2026

Assignee

Shanghai Runshi Medical Technology Co., Ltd

Inventors

Ao Zhang, Meiyu Geng, Jing Ai, Caixia Wang, Xia Peng, Yang Zhang, Jian Ding

Abstract

Use of a compound of general formula (A) which is a CFS-IR kinase inhibitor or a pharmaceutically acceptable salt thereof in the preparation of medicaments for treating diseases related to CSF-1R kinase signal transduction pathway or medicaments for regulating immunization. In vivo and in vitro studies show that the compound can significantly inhibit CSF-IR kinase activity; significantly inhibits the proliferation of a CSF-1/CSF-1R-driven mouse myeloid leukemia cell line, inhibits the survival of macrophages induced by CSF-1 and reverses M2 polarization phenotype of macrophages, and has an effect superior to that of the marketed medicament Pexidartinib. In a TAM enriched tumor model (MC38 model), the compound significantly antagonizes the tumor immunosuppressive microenvironment and exhibits significant anti-tumor efficacy. The compound has inhibitory effects on tumors that are not sensitive to immune checkpoint drugs, and can enhance the efficacy of immune checkpoint drugs, and has good clinical application prospects.

CPC Classifications

A61K 31/496 A61K 39/00 A61K 31/513 A61K 39/3955 A61K 45/06 A61K 2300/00 A61P 35/00 A61P 35/02 A61P 37/04 A61P 29/00 C07K 16/2818 C07K 16/2827 C07D 401/12

Filing Date

2021-02-26

Application No.

17802898

Claims

8

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