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Diarylpyrimidine compound, composition and application

A compound and composition technology, applied in the field of medicine, can solve the problems of poor drug resistance and achieve the effect of great application value

Inactive Publication Date: 2016-09-28
DALIAN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs inevitably have the problem of poor drug resistance

Method used

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  • Diarylpyrimidine compound, composition and application
  • Diarylpyrimidine compound, composition and application
  • Diarylpyrimidine compound, composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The preparation of embodiment 1 target molecule

[0071] The thin-layer chromatography silica gel plate uses Yantai Huanghai HSGF254 or Qingdao GF254 silica gel plate, the specification of the silicon amine plate used in thin-layer chromatography (TLC) is 0.15mm-0.2mm, and the specification of thin-layer chromatography separation and purification product is 0.4 mm-0.5mm.

[0072] The raw materials used in the present invention are mainly purchased from Sinopharm Chemical Reagent Co., Ltd., Beijing Coup Technology Co., Ltd., Aladdin Chemical Reagent Co., Ltd., Darui Chemicals and other companies.

[0073] Unless otherwise specified in the examples, the solution refers to an aqueous solution.

[0074] Unless otherwise specified in the examples, the reaction temperature is room temperature, which is 20°C-30°C.

[0075] The technical scheme that the present invention adopts is as follows:

[0076]

[0077] Synthetic route of compound (Ⅰ). Reagents and conditions: (a) ...

Embodiment 2

[0183] Example 2 Evaluation of biological activity of target molecule

[0184] 1. In vitro test method for receptor tyrosine kinase inhibitory activity

[0185] Prepare Kinase Assay Buffer

[0186] ① Melt the Kinase Detection Buffer at room temperature and observe whether there is precipitation.

[0187] ②If precipitation occurs, incubate at 37°C (Kinase Detection Buffer) for 15 minutes and shake frequently to dissolve the precipitation. Alternatively, carefully aspirate the supernatant to remove the pellet.

[0188] Prepare Kinase Assay Reagents

[0189] ①Equilibrate Kinase Detection Buffer (Kinase Detection Buffer) and (Kinase Detection Substrate) at room temperature before use.

[0190] ② Pour all the Kinase Detection Buffer into the brown bottle containing the Kinase Detection Substrate to dissolve the lyophilized powder substrate, thus making the Kinase Detection Reagent.

[0191] ③Gently oscillate, vortex or invert to mix to form a homogeneous solution, and the subs...

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Abstract

The invention relates to a diarylpyrimidine compound, a composition and application. The diarylpyrimidine compound is particularly a compound as shown in a general formula (I), and all substituent groups of the general formula (I) are as defined in the description. The invention further relates to application of the compound as shown in the general formula (I) or a pharmaceutically acceptable salt or the pharmaceutical composition in treating tumor diseases, particularly treating a non-small cell lung cancer, a small cell lung cancer, squamous-cell carcinoma, a breast cancer and lymphocytic leukemia by inhibiting epidermal growth factor receptor (EGFR) protein tyrosine kinase (PTK). Please see the formula in the description.

Description

technical field [0001] The invention relates to diarylpyrimidine compounds, composition and application, and belongs to the technical field of medicine. Background technique [0002] Protein tyrosine kinases (PTKs) regulate a series of physiological and biochemical processes such as cell growth, differentiation, and apoptosis by controlling cell signal transduction pathways. Receptor-type tyrosine kinases are a relatively large class of kinases that span cell membranes, possess a ligand-binding extracellular domain, a transmembrane domain, and act as kinases—in phosphorylating specific tyrosine residues and by This affects the intracellular domain of cell proliferation. Aberrant expression of these kinases has been found in common human cancers (eg, lung cancer, breast cancer, gastric cancer, ovarian cancer, lymphoma). Protein tyrosine kinase has become one of the important targets in the research and development of anticancer drugs. [0003] Epidermal growth factor recep...

Claims

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Application Information

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IPC IPC(8): C07D239/48A61K31/506A61K31/5377A61P35/00A61P35/02
CPCC07D239/48
Inventor 马晓东宋振东葛阳张建斌王长远唐泽耀彭金咏刘克辛
Owner DALIAN MEDICAL UNIVERSITY
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