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Novel epidermal growth factor receptor inhibitor and application thereof

A technology of use and carrier, applied in the field of drug resistance inhibitors and novel epidermal growth factor receptor inhibitors, which can solve the problems of difficult to achieve concentration and drug resistance.

Inactive Publication Date: 2016-10-05
ZHEJIANG WENDA PHARMA TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, clinical trials have shown that the subsequent amplification or high expression of T790M mutations will lead to resistance to these irreversible inhibitors; required concentration

Method used

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  • Novel epidermal growth factor receptor inhibitor and application thereof
  • Novel epidermal growth factor receptor inhibitor and application thereof
  • Novel epidermal growth factor receptor inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0118] Embodiment 1 compound preparation

[0119]

[0120] Intermediate A and N,N,N'-trimethylaminoethyl-1,2-diamine (B) were dissolved in n-butanol, DIPEA was added, and the mixture was stirred overnight in an oil bath at 130°C. with SiO 2 After absorbing the mixed solution, a solid C was separated by column chromatography.

[0121] The solid C, ammonium chloride and iron powder were refluxed and stirred in the mixture of ethanol and water for 2 hours, and the intermediate D was separated by column chromatography.

[0122] Dissolve the intermediate D, DIPEA in dichloromethane cooled in an ice bath, then slowly add the corresponding acid chloride dropwise, and stir until the reaction is complete. Pour into NaHCO 3 solution, extracted with dichloromethane, and purified by silica gel column chromatography to obtain Compound E.

Embodiment 2

[0123] Embodiment 2 compound preparation

[0124]

[0125] Intermediates A and H were dissolved in n-butanol, DIPEA was added, and the mixture was stirred overnight in an oil bath at 130°C. with SiO 2 After absorbing the mixed solution, a solid I was separated by column chromatography.

[0126] The solid C, ammonium chloride and iron powder were refluxed and stirred in the mixture of ethanol and water for 2 hours. The intermediate J was separated by column chromatography.

[0127] The intermediate J, DIPEA was dissolved in dichloromethane cooled in an ice bath, and then the corresponding prepared acid chloride was slowly added dropwise, and stirred until the reaction was complete. Pour into NaHCO 3 solution, extracted with dichloromethane, and purified by silica gel column chromatography to obtain Compound K.

Embodiment 3

[0128] Example 3 compound preparation

[0129]

[0130] The intermediate J, DIPEA was dissolved in dichloromethane cooled in an ice bath, and then the corresponding prepared acid chloride was slowly added dropwise, and stirred until the reaction was complete. Pour into NaHCO 3 solution, extracted with dichloromethane, and purified by silica gel column chromatography to obtain Compound L.

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Abstract

The invention provides a novel epidermal growth factor receptor inhibitor and an application thereof. The novel epidermal growth factor receptor inhibitor can be used as a T790M variation induced drug-resistant inhibitor.

Description

technical field [0001] The invention relates to a kinase inhibitor, in particular to a novel epidermal growth factor receptor inhibitor and application thereof, which can be used as an inhibitor of drug resistance caused by T790M mutation. Background technique [0002] Protein kinases play an important role in cell signaling. It can transfer phosphate groups from ATP or GTP to specific amino acid residues of functional proteins, thereby triggering a series of biochemical reactions. Epidermal growth factor (EGFR) is a well-studied tyrosine kinase, which is highly expressed in a variety of tumors. Their expression is related to the proliferation, metastasis and other phenomena of cancer cells. Therefore, inhibitors targeting epidermal growth factor receptor (EGFR) are one of the important directions of anticancer drug research in recent years. [0003] There are currently two classes of EGFR tyrosine kinase inhibitors on the market, reversible and irreversible inhibitors. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/04C07D401/14A61K31/506A61P35/00A61P35/02
Inventor 王能辉
Owner ZHEJIANG WENDA PHARMA TECH LTD
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