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Bruton's tyrosine kinase inhibitor

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: 2019-03-05
BEIJING RECIPROCAPHARM
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  • 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

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Embodiment

[0100] The following specific non-limiting examples will be construed as merely illustrative and do not limit the present invention in any way. Although no further detailed description is required, it is believed that those skilled in the art can fully utilize the present invention based on the description herein.

[0101] Compound synthesis

[0102] In the following synthesis schemes, 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'-tetramethylurea hexafluorophosphate;

[0113] DMF: Dimethylformamide;

[0114] TFA: Trifluoroacetic acid

[0115] step 1:

[0116]

[0117] Combine m-phenylenediamine 1 (0.500g, 4.62mmol) and (Boc) 2 O (0.92mL, 4.0mmol)...

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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 covalent and reversible manner. The compounds of the present invention can be used to treat 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 targets for drug screening. It has become an important field in the research and development of anti-cancer drugs. In recent years, the research on protein tyrosine kinase (PTK) signal channels has become a hot spot. People have learned more about the relationship between PTKs and tumor cell proliferation, differentiation, migration and apoptosis, and interfere or hinder The strategy of breaking the tyrosine kinase pathway has been used in...

Claims

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Application Information

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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
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