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Salt of methoxy dihydronitidine derivate

A methoxydihydro two-sided, needle alkali technology, applied in the direction of drug combination, digestive system, antiviral agent, etc., can solve the problems of adverse reactions, drug resistance, unsatisfactory drug treatment effect, etc., and achieve practical therapeutic activity. Effect

Inactive Publication Date: 2013-10-30
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 easy to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not enough. ideal

Method used

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  • Salt of methoxy dihydronitidine derivate
  • Salt of methoxy dihydronitidine derivate
  • Salt of methoxy dihydronitidine derivate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Methoxydihydrodecauline fumarate

[0048] Dissolve 3.81 g (0.01 mol) of the compound methoxydihydroephedrine and 1.17 g (0.01 mol) of fumaric acid in 100 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood for several hours in a temperature environment of 0-5°C to precipitate methoxydihydro-amphedrine fumarate crystals and filter out methoxy The crystalline fumarate salt of dihydroepaurine was washed with ethanol and dried under vacuum at 50°C to obtain 4.95 g of the product.

Embodiment 2

[0050] Methoxydihydrodecauline fumarate

[0051] Stir 3.81 g of the compound methoxydihydroephedrine 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. Standing for several hours in the temperature environment of 0-5 ℃, the methoxydihydro-amphedrine fumarate crystals are precipitated, the methoxyl-dihydro-amphedrine fumarate crystals are filtered out, washed with ethanol and placed in Drying under vacuum at 50°C yielded 4.93 g of product.

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Abstract

The invention discloses methoxy dihydronitidine as well as fumarate of derivate or thereof pharmaceutically acceptable solvate thereof and application thereof in preparing a medicament for treating hepatitis B.

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 methoxydihydroamphedrine 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 easy to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not enough. ideal. Chinese patent application publication number CN101084906A describes some active compounds for treating hepatitis B. 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....

Claims

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Application Information

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IPC IPC(8): C07D491/056A61K31/4741A61P1/16A61P31/20
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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