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Novel application of quinazoline derivative type tyrosine kinase inhibitor

An amino, compound technology, applied in the field of medicine, can solve problems such as abnormality and uncontrolled cell reproduction

Pending Publication Date: 2019-11-26
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 - cancer

Method used

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  • Novel application of quinazoline derivative type tyrosine kinase inhibitor
  • Novel application of quinazoline derivative type tyrosine kinase inhibitor
  • Novel application of quinazoline derivative type tyrosine kinase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0168] Experimental example 1 In vitro enzymatic activity experiment

[0169] Test product: compound 18-2 crystal form I, self-made, its chemical name, XRPD pattern and preparation method refer to the preparation example of the international patent application WO2017107985A1.

[0170] 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.

[0171] 1. Reagent preparation

[0172] (1) 1x Kinase Buffer for Kinase Detection

[0173] 50mM HEPES (pH 7.5), 0.0015% Brij-35, 5mM MgCl 2 , 2mM DTT.

[0174] (2) Stop solution

[0175] 100 mM HEPES (pH 7.5), 0.015% Brij-35, 0.2% Coating Reagent #3, 50 mM EDTA.

[0176] 2. Compound preparation

[0177] (1) According to the highest concentration to be used, the compound was made into a 50× stock solution with 100% DMSO.

[0178] (2) Take a new 96-well plate, add 100 μL of compound master solution to the second wel...

experiment example 2

[0203] Experimental example two In vitro enzymatic activity experiment

[0204] Test product: the compound of the present invention is self-made according to the prior art method, and its chemical name and structural formula are shown in the content of the present specification.

[0205] Experimental method: Mobility Shift Assay was used to screen compounds on kinases EGFR_C797S and EGFR_C797S / L858R in the case of Km ATP.

[0206] 1. Reagent preparation

[0207] (1) 1x Kinase Buffer for Kinase Detection

[0208] 50 mM HEPES (pH 7.5), 0.0015% Brij-35.

[0209] (2) Stop solution

[0210] 100 mM HEPES (pH 7.5), 0.015% Brij-35, 0.2% Coating Reagent #3, 50 mM EDTA.

[0211] 2. Compound preparation

[0212] (1) The detection initial concentration of the compound is 10 μM, and the compound is made into a 50× stock solution with 100% DMSO.

[0213] (2) Take 5 μl of 10 mM compound, add 95 μl of 100% DMSO to prepare a 500 μM compound solution, and make 4-fold dilutions to 10 con...

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Abstract

The invention discloses novel application of a quinazoline derivative type tyrosine kinase inhibitor, belongs to the technical field of medicines, and in particular relates to novel application of a compound of a formula (I) shown in the description, and a stereisomer, a pharmaceutically acceptable salt and a crystal forma thereof, and in the formula, R1, R2, R3, R4, R5, R6, L and n are defined inthe description. The invention specifically relates to the compounds and application of medicine preparations and medicine compositions with the compounds in preparing medicines for treating tumor patients with EGFR_T790M mutation, EGFR_L858R mutation, EGFR_C797S mutation, EGFR_d746-750 mutation, EGFR_T790M / L858R mutation, EGFR_T790M / C797S mutation, EGFR_T790M / d746-750 mutation, EGFR_C797S / L858Rmutation, EGFR_L858R / d746-750 mutation, EGFR_C797S / d746-750 mutation, EGFR_L858R / T790M / C797S mutation, EGFT_d746-750 / T790M / C797S mutation or EGFR_d746-750 / L858R / C797S.

Description

[0001] 1. Technical field [0002] The invention belongs to the field of medicine, and specifically relates to a novel use of a quinazoline derivative tyrosine kinase inhibitor, its stereoisomer, its pharmaceutically acceptable salt and its crystal form. [0003] 2. Background technology [0004] 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 act to treat cancer and other diseases characterized by u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08C07D471/10C07D471/08C07D491/107C07D403/12C07D401/12A61K31/517A61P35/00
CPCA61P35/00C07B2200/07C07D401/12C07D403/12C07D471/08C07D471/10C07D491/107C07D493/08
Inventor 史澂空
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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