公开(公告)号：US20230382871A1

公开(公告)日：2023-11-30

申请号：US18027759

申请日：2021-09-22

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Jian DING ,  Wenhu DUAN ,  Hua XIE ,  Meiyu GENG ,  Caixia WANG ,  Zhengsheng ZHAN ,  Na GAO ,  Yang ZHANG

IPC: C07D231/56 ,  A61P35/00 ,  C07K16/28

CPC classification number: C07D231/56 ,  A61P35/00 ,  C07K16/2818 ,  C07K16/2827 ,  A61K2039/505

Abstract: Provided is the use of a CSF1R kinase inhibitor compound or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating diseases related to the CSF1R kinase signal transduction pathway or drugs for regulating immunization.

公开(公告)号：US20230285389A1

公开(公告)日：2023-09-14

申请号：US17802898

申请日：2021-02-26

Applicant: Shanghai Runshi Medical Technology Co., Ltd ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Ao ZHANG ,  Meiyu GENG ,  Jing AI ,  Caixia WANG ,  Xia PENG ,  Yang ZHANG ,  Jian DING

IPC: A61K31/496 ,  A61P35/00 ,  C07K16/28

CPC classification number: A61K31/496 ,  A61P35/00 ,  C07K16/2818 ,  C07K16/2827

Abstract: 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.