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High-selectivity CSF1R inhibitor, preparation method and pharmaceutical applications thereof

A pharmacy, drug technology, applied in the field of drug synthesis

Active Publication Date: 2020-02-28
ABBISKO THERAPEUTICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Small-molecule kinase inhibitors generally have selectivity issues, especially with respect to other members of the same kinase family

Method used

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  • High-selectivity CSF1R inhibitor, preparation method and pharmaceutical applications thereof
  • High-selectivity CSF1R inhibitor, preparation method and pharmaceutical applications thereof
  • High-selectivity CSF1R inhibitor, preparation method and pharmaceutical applications thereof

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Embodiment Construction

[0019] After extensive and in-depth research, the inventors of the present application have firstly developed a highly selective CSF1R inhibitor with the structure of formula (I), its preparation method and pharmaceutical application. The compound of the present invention has a strong inhibitory effect on CSF1R kinase activity, and can be widely used in the preparation of medicines for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, especially for the treatment of ovarian cancer, pancreatic cancer and prostate cancer Drugs for breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic diseases, neurodegenerative diseases, metastasis of primary tumor site or bone metastatic cancer are expected to be developed into a new generation of CSF1R inhibitors drug. On this basis, the present invention has been accomplished.

[0020] "Pharmaceutical composition" means a mixture containing one or more compounds described herein, or a ph...

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PUM

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Abstract

The invention relates to a high-selectivity CSF1R inhibitor with a structure represented by a formula (I), a preparation method and pharmaceutical applications thereof. According to the invention, thecompound can be widely applied to preparation of medicines for treating cancers, tumors, autoimmune diseases, metabolic diseases or metastatic diseases, especially for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic diseases, neurodegenerative diseases, primary tumor site metastasis or bone metastatic cancer, and is expected to be developed into a new generation of CSF1R inhibitor drugs.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a highly selective CSF1R inhibitor, its preparation method and its application in pharmacy. [0002] technical background [0003] The full name of CSF1R (cFMS) is colony stimulating factor 1 receptor. CSF1R and cKIT, FLT3, PDGFR-a&b belong to the same three types of growth hormone receptor family. The receptor is a membrane protein expressed on the surface of macrophages and monocytes. Its extracellular segment can bind to macrophage colony-stimulating factor, and its intracellular segment tyrosine kinase can activate macrophages and monocytes downstream Cell growth and reproduction signaling pathways, including MAPK, PI3K, etc. Therefore, the CSF1R signaling pathway has an important impact on the development and differentiation of macrophages, monocytes, and the physiological functions of tumor-associated macrophages (Tumor-Associated Macrophage, TAM). [0004] Tumor...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61P35/00A61P35/02A61P19/02A61P29/00A61P19/08A61P13/12A61P37/06A61P1/00A61P11/06A61P11/00A61P19/10A61K31/444
CPCC07D401/14A61P35/00A61P35/02A61P19/02A61P29/00A61P19/08A61P13/12A61P37/06A61P1/00A61P11/06A61P11/00A61P19/10
Inventor 赵保卫张鸣鸣喻红平陈椎徐耀昌
Owner ABBISKO THERAPEUTICS CO LTD
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