发明公开
- 专利标题: USE OF CSF-1R KINASE INHIBITOR
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申请号: EP21760664.9申请日: 2021-02-26
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公开(公告)号: EP4112054A1公开(公告)日: 2023-01-04
- 发明人: ZHANG, Ao , GENG, Meiyu , AI, Jing , WANG, Caixia , PENG, Xia , ZHANG, Yang , DING, Jian
- 申请人: Shanghai Runshi Medical Technology Co., Ltd , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- 申请人地址: CN Shanghai 200040 Room 5002-N, 1486 Nanjing West Road Jing'an District; CN Shanghai 201203 555 Zuchongzhi Road, Zhangjiang, Pudong
- 代理机构: Mewburn Ellis LLP
- 优先权: CN202010128115 20200228
- 国际公布: WO2021170078 20210902
- 主分类号: A61K31/4427
- IPC分类号: A61K31/4427 ; A61K31/44 ; A61K31/4439 ; A61K31/4545 ; A61K31/496 ; A61K31/5377 ; A61K31/506 ; A61K31/4433 ; C07D401/12 ; C07D213/75 ; C07D413/12 ; C07D417/12 ; C07D403/12 ; C07D405/12 ; A61P35/00
摘要:
Use of a compound of general formula (A) which is a CFS-1R 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-1R 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.
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