ALK inhibitor and applications thereof

A technology of inhibitors and uses, applied in the field of medicinal chemistry, can solve the problems of loss of curative effect and limited prognosis of patients with advanced NSCLC

Inactive Publication Date: 2016-08-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Large-scale clinical trial data show that conventional chemotherapy has very limited prognostic effect on patients with advanced NSCLC, and the survival time of patients is less than 12 months
However, the first generation of targeted drugs for ALK also has its own shortcomings. Taking crizotinib as an example, patients who are mainly effective for its treatment usually lose their efficacy due to drug resistance after 1 year of treatment

Method used

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  • ALK inhibitor and applications thereof
  • ALK inhibitor and applications thereof
  • ALK inhibitor and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0011] Experimental Study on the Inhibitory Activity of Compound 1~Compound 20 on ALK

[0012] 1) Experimental materials: DMSO, PBS, rabbit serum, ALK, dextran sulfate / MgCl 2 , centrifuge, scintillation fluid.

[0013] 2) Experimental method

[0014] · Dissolve all test compounds in DMSO.

[0015] · Prepare the reaction system (Mixture 1) according to the table below and incubate at 37°C for 10 minutes.

[0016]

[0017] The concentration of each substance is 100μM

[0018] · Prepare an appropriate amount of mixed solution with ALK and PBS in a ratio of 2:8, mix well, and add 50 μL of each tube to Mixture 1. Seal and mix well.

[0019] • Incubate at 37°C for 6 hours.

[0020] Add 10 μL ALK precipitant dextran sulfate / MgCl 2 , and the final concentrations were 0.05% and 50 mM, respectively. Mix well and let stand for 10 minutes.

[0021] · Centrifuge at 5000 rpm for 15 minutes. Let it stand for 10 minutes after taking it out.

[0022] · Pipette 50 μL supernatant i...

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Abstract

The invention relates to the field of medicinal chemistry, and in particular relates to medical applications of compounds (1-20) and medicinal compositions containing the compounds, especially the applications as an ALK inhibitor. The structural formulas of the 20 compounds are shown in the description.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to 20 compounds, pharmaceutical compositions containing these compounds and their medical application, especially the application as an inhibitor of anaplastic lymphoma kinase (ALK). Background technique [0002] In recent years, lung cancer, especially non-small cell lung cancer (NSCLC), has occurred frequently and is the cancer with the highest mortality rate. Data from large-scale clinical trials show that conventional chemotherapy has very limited prognostic effect on patients with advanced NSCLC, and the survival time of patients is less than 12 months. Therefore, according to the pathogenesis of NSCLC, it is particularly urgent to find new targeted small molecule inhibitors. [0003] Erlotinib and gefitinib targeting epidermal growth factor receptor (EGFR) mutations and crizotinib targeting anaplastic lymphoma kinase (ALK) produced by gene translocation The discovery broug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K31/519A61K31/55A61K31/404A61K31/4525A61K31/4453A61K31/427A61K31/4184A61K31/517A61K31/513A61K31/426A61K31/429A61K31/36A61K31/402A61P35/00A61P35/02
Inventor 李红玫
Owner CHINA PHARM UNIV
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