Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Inhibitors of Bruton's tyrosine kinase

A technology of amino and compounds, applied in the field of compounds that inhibit the activity of Bruton's tyrosine kinase in a covalent and reversible manner, can solve the problem that reversible covalent inhibitors do not yet exist

Active Publication Date: 2020-10-30
BEIJING RECIPROCAPHARM
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Reversible covalent inhibitory drugs targeting Btk do not exist so far

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Inhibitors of Bruton's tyrosine kinase
  • Inhibitors of Bruton's tyrosine kinase
  • Inhibitors of Bruton's tyrosine kinase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0100] The following specific non-limiting examples are to be construed as merely illustrative and not restrictive of the invention in any way. While further elaboration is not required, it is believed that one skilled in the art can, based on the description herein, fully utilize the present invention.

[0101] compound synthesis

[0102] In the synthetic schemes below, the following abbreviations are used:

[0103] Boc: tert-butoxycarbonyl;

[0104] Et 3 N / TEA: Triethylamine;

[0105] Dioxane: 1,4-dioxane;

[0106] RT: room temperature;

[0107] CH 3 CN: acetonitrile;

[0108] K 2 CO 3 : potassium carbonate;

[0109] SOCl 2 : thionyl chloride;

[0110] DCM: dichloromethane;

[0111] DIEA: N,N-Diisopropylethylamine;

[0112] HATU: 2-(7-benzotriazole oxide)-N,N,N',N'-tetramethyluronium hexafluorophosphate;

[0113] DMF: dimethylformamide;

[0114] TFA: Trifluoroacetic acid

[0115] step 1:

[0116]

[0117] m-Phenylenediamine 1 (0.500g, 4.62mmol) and (Boc)...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a compound with a general formula (I), wherein the compound is capable of inhibiting Btk, and the groups are disclosed in the invention. The compound can be used for treating autoimmune diseases, heterologous immunization diseases, cancers, or thromboembolism diseases. The invention also discloses a pharmaceutical composition containing the compound represented by formula (I). The Bruton's tyrosine kinase inhibitor is capable of inhibiting the activity of Bruton's tyrosine kinas through covalent binding such as a covalent reversible mode.

Description

technical field [0001] The present invention relates to compounds that inhibit the activity of Bruton's tyrosine kinase (Btk), in particular, the present invention also relates to compounds that inhibit the activity of Bruton's tyrosine kinase in a covalently reversible manner. The compounds of the present invention can be used in the treatment of diseases related to B cells. Background technique [0002] "Molecular targeted therapy" is a method of treating cancer with some key enzymes involved in the differentiation and proliferation of tumor cells as drug screening targets, which has become an important field of anticancer drug research and development today. In recent years, the research on protein tyrosine kinase (PTK) signaling channel has become a hotspot. People have learned more about the relationship between PTKs and tumor cell proliferation, differentiation, migration and apoptosis. The strategy of breaking the tyrosine kinase pathway has been used in the treatmen...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/48C07D405/12C07D403/12C07D409/12A61K31/506A61K31/505A61P37/02A61P29/00A61P35/00A61P7/02
CPCC07D239/48C07D403/12C07D405/12C07D409/12
Inventor 李锡涛陶冠宇史艳霞潘峥婴
Owner BEIJING RECIPROCAPHARM
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com