Salt of apocavidine derivative

A technology of drugs and compounds, applied in the direction of organic chemistry, antibacterial drugs, etc., can solve problems such as adverse reactions and unsatisfactory drug treatment effects, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2014-06-04
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 against methicillin-resistant Staphylococcus aureus, the existing drugs are likely to cause multiple and severe adverse reactions, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • Salt of apocavidine derivative
  • Salt of apocavidine derivative
  • Salt of apocavidine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Apocavidin Fumarate

[0048] Dissolve 3.41 g (0.01 mol) of the compound apocavidin and 1.17 g (0.01 mol) of fumaric acid in 90 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 apocavidin fumarate crystals, and apocavidin was filtered out The fumarate salt crystals were washed with ethanol and dried under vacuum at 50°C, yielding 4.57 g of product.

Embodiment 2

[0050] Apocavidin Fumarate

[0051] 3.41 g of compound apocavidin fumarate and 1.17 g of fumaric acid were stirred in 90 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. Stand for several hours in a temperature environment of 0-5°C, the apocavidin fumarate crystals are precipitated, the apocavidin fumarate crystals are filtered out, washed with ethanol and dried under vacuum at 50°C , 4.55 g of product were obtained.

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Abstract

The invention relates to apocavidine and fumarate or pharmaceutically acceptable solvate of a derivative of apocavidine, and an application of apocavidine and fumarate or pharmaceutically acceptable solvate in preparing a methicillin-resistant staphylococcus aureus medicine.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to apocavidin organic acid salt and its pharmaceutical application. Background technique [0002] For now, although there are many kinds of drugs against methicillin-resistant Staphylococcus aureus, these existing drugs are likely to cause multiple and severe adverse reactions, and the therapeutic effect of the existing drugs is still not ideal. The Chinese invention patent authorization announcement number is CN 100586433C patent specification, which describes some active compounds with resistance to methicillin-resistant Staphylococcus aureus. 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 stabil...

Claims

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Application Information

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IPC IPC(8): C07D455/03A61K31/4375A61P31/04
CPCC07D455/03
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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