Urea derivative and medicinal application thereof

A technology of urea groups and compounds, applied in the field of medicinal chemistry, can solve problems such as adverse reactions, multiple and serious, etc., and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2013-04-24
SHANGHAI YIZHI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] For now, although there are many kinds of drugs for the treatment and prevention of influenza, the existing drugs are likely to cause many and severe adverse reactions.

Method used

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  • Urea derivative and medicinal application thereof
  • Urea derivative and medicinal application thereof
  • Urea derivative and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine-2 -yl)-2-methoxyacetamide fumarate

[0048] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine- 59.3 g (0.1 mol) of 2-yl)-2-methoxyacetamide and 11.7 (0.1 mol) g of fumaric acid were dissolved in 1500 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood for several hours at a temperature of 0-5°C to precipitate N-(4-((4-(3-(3-tert-butyl -1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide fumarate crystals, filtered off N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine-2 The crystals of -yl)-2-methoxyacetamide fumarate were washed with ethanol and dried under vacuum at 50°C to obtain 63.3 g of product.

Embodiment 2

[0050] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine-2 -yl)-2-methoxyacetamide fumarate

[0051] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine- 50.1 g of 2-yl)-2-methoxyacetamide fumarate and 12.2 g of fumaric acid were stirred in 1200 ml of refluxing ethanol until all the solids were dissolved. Add activated carbon, filter the hot solution through diatomaceous earth, and cool down to room temperature while stirring. Standing for several hours in a temperature environment of 0-5°C, N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)urea is precipitated Base) naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide fumarate crystals, N-(4-((4-(3-(3-tert-butyl Base-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide fumarate crystals, with Washing with ethanol and drying under vacuum at 50°C yielded 52.7 g of product.

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Abstract

The invention relates to N-(4-((4-(3-(3-tert-butyl-1-p-methylphenyl-1H-pyrazole-5-yl) ureido) naphthalene-1-base oxygen) methyl) pyridine-2-yl)-2-methoxy acetamide and fumarate of a derivative thereof or a solvate thereof acceptable in pharmacology and an application for preparing a medicine for treating and / or relieving and / or preventing influenza.

Description

field of invention [0001] The present invention relates to the field of medicinal chemistry, specifically, the present invention relates to N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl) ureido ) Naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide organic acid salts and pharmaceutical applications thereof. Background technique [0002] For now, although there are many kinds of medicines for the treatment and prevention of influenza, these existing medicines easily cause many and severe adverse reactions. PCT International Publication No. WO 2011 / 070368A1 describes some active compounds for treating and preventing influenza virus infection. Contents of the invention [0003] The present invention discloses some new compounds, preparation methods of these compounds, pharmaceutical compositions containing these compounds and pharmaceutical applications of these compounds and compositions. [0004] These compounds exhibit good water solubility stability and sol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P31/16
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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