New use of quinazoline derivative tyrosine kinase inhibitor

A technology of uses and drugs, applied in the field of medicine, can solve problems such as uncontrolled cell reproduction and abnormality

Active Publication Date: 2018-05-29
SHANDONG XUANZHU PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, under certain conditions, these receptors are either mutated or overexpressed, becoming abnormal, causing cells to multiply uncontrollably, leading to tumor growth and ultimately the well-known disease known as cancer.

Method used

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  • New use of quinazoline derivative tyrosine kinase inhibitor
  • New use of quinazoline derivative tyrosine kinase inhibitor
  • New use of quinazoline derivative tyrosine kinase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0048] In vitro enzymatic activity test one of experimental example 1 formula (1) compound

[0049] Test product: dimaleate of the compound of formula (1), self-made.

[0050] Experimental method: Mobility Shift Assay was used to screen compounds on kinases EGFR_C797S, EGFR_C797S / L858R, EGFR_T790M / C797S and EGFR_T790M / C797S / L858R in the case of Km ATP.

[0051] 1. Reagent preparation

[0052] (1) 1x Kinase Buffer for Kinase Detection

[0053] 50mM HEPES (pH 7.5), 0.0015% Brij-35, 5mM MgCl 2 , 2mM DTT.

[0054] (2) Stop solution

[0055] 100 mM HEPES (pH 7.5), 0.015% Brij-35, 0.2% Coating Reagent #3, 50 mM EDTA.

[0056] 2. Compound preparation

[0057] (1) According to the highest concentration to be used, the compound was made into a 50× stock solution with 100% DMSO.

[0058] (2) Take a new 96-well plate, add 100 μL of compound master solution to the second well, and add 60 μL of 100% DMSO to the other wells. Take 20 μL of the compound from the second well and add i...

experiment example 2

[0082] In vitro enzymatic activity experiment two of experimental example 2 formula (1) compound

[0083] Test product: dimaleate of the compound of formula (1), self-made.

[0084] Experimental method: using the Mobility Shift Assay method in the case of Km ATP, in the kinase

[0085] Compounds were screened on EGFR_d746-750 / T790M / C797S.

[0086] 1. Reaction buffer

[0087] 20mM Hepes (pH 7.5), 10mM MgCl2, 1mM EGTA, 0.02% Brij35, 0.02mg / ml

[0088] BSA, 0.1mM Na 3 VO 4 , 2mM DTT, 1% DMSO.

[0089] 2. Compound preparation

[0090] (1) According to the highest concentration to be used, the compound was made into a 50× stock solution with 100% DMSO.

[0091] (2) Take a new 96-well plate, add 100 μL of compound master solution to the second well, and add 40 μL of 100% DMSO to the other wells. Take 20 μL of the compound from the second well and add it to the third well, and make 3-fold dilutions successively, and dilute 10 concentrations in total.

[0092](3) 100 μL of ...

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PUM

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Abstract

The present invention relates to new use of a quinazoline derivative tyrosine kinase inhibitor, and specifically relates to new use of a compound represented by the formula (1) (E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazoline-6-yl)-4-(2-azaspiro[3.3]heptane-2-yl)-2-butenamide and pharmaceutically acceptable salts thereof.

Description

1. Technical field [0001] The invention belongs to the field of medicine, and in particular relates to a new application of a quinazoline derivative tyrosine kinase inhibitor and a pharmaceutically acceptable salt thereof. 2. Background technology [0002] Protein tyrosine kinases, a class of enzymes that catalyze the transfer of phosphate groups from ATP to tyrosine residues located on protein substrates, play a role in normal cell growth. Many growth factor receptor proteins act through tyrosine kinases and through this process affect the conduction of signaling pathways that regulate cell growth. However, under certain conditions, these receptors are either mutated or overexpressed, becoming abnormal, causing cells to multiply uncontrollably, leading to tumor growth and ultimately the well-known disease known as cancer. Growth factor receptor protein tyrosine kinase inhibitors function to treat cancer and other diseases characterized by uncontrolled or abnormal cell grow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61P35/00
CPCA61K31/517
Inventor 余立华张宝成
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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