Salts of dehydrocheilanthifoline derivatives

A technology of corydine and medicine, which is applied in the field of dehydrocorydine organic acid salt and its pharmaceutical application, can solve problems such as adverse reactions, multiple and heavy, and unsatisfactory drug treatment effects, and achieve practical treatment active effect

Inactive Publication Date: 2013-12-18
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 of hepatitis B virus infection, these existing drugs are prone to cause multiple and severe adverse reactions, and some of them produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • Salts of dehydrocheilanthifoline derivatives
  • Salts of dehydrocheilanthifoline derivatives
  • Salts of dehydrocheilanthifoline derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Dehydroclavine fumarate

[0048] 3.22 g (0.01 mol) of the compound dehydrocorydroline and 1.17 g (0.01 mol) of fumaric acid were dissolved in 100 ml of boiling ethanol. The hot solution is filtered through diatomaceous earth, then slowly cooled under gentle stirring, and left to stand for several hours in a temperature environment of 0-5°C to separate out the crystals of corydine fumarate. The crystals of corydine fumarate were washed with ethanol and dried under vacuum at 50°C to obtain 4.38 g of the product.

Embodiment 2

[0050] Dehydroclavine fumarate

[0051] Stir 3.22 g of the compound dehydrocorrydine fumarate and 1.17 g of fumaric acid in 100 ml of refluxing ethanol until the solids are completely 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, precipitate fumarate crystals, filter out the crystals of corydine fumarate, wash with ethanol and dry under vacuum at 50°C to obtain 4.35 g product.

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Abstract

The invention relates to applications of fumarate of dehydrocheilanthifoline and derivatives thereof or pharmacology-acceptable solvate of the fumarate of dehydrocheilanthifoline and derivatives thereof on preparation of drugs for curing hepatitis B virus infection.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to an organic acid salt of dehydroclindine and its pharmaceutical application. Background technique [0002] For now, although there are many kinds of drugs for the treatment of hepatitis B virus infection, these existing drugs are likely to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal. Chinese Invention Patent Publication No. CN 102078319 B describes some active compounds for treating hepatitis B 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 solid form stability. S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03C07C57/15C07C51/41A61P31/20A61P1/16
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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