Salt of dihydrosanguinarine derivative

A dihydrosanguinarine and drug technology, applied in the field of dihydrosanguinarine organic acid salts and its pharmaceutical application, can solve problems such as adverse reactions, drug resistance, and unsatisfactory drug treatment effects, 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 dihydrosanguinarine derivative
  • Salt of dihydrosanguinarine derivative
  • Salt of dihydrosanguinarine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Dihydrosanguinarine fumarate

[0048] Dissolve 3.35 g (0.01 mol) of the compound dihydrosanguinarine and 1.17 g (0.01 mol) of fumaric acid in 80 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, dihydrosanguinarine fumarate crystals were precipitated, and dihydrosanguinarine was filtered out The fumarate salt crystals were washed with ethanol and dried under vacuum at 50°C to yield 4.48 g of product.

Embodiment 2

[0050] Dihydrosanguinarine Fumarate

[0051] Stir 3.35 g of the compound dihydrosanguinarine fumarate and 1.17 g of fumaric acid in 80 ml of refluxing ethanol until all the solids are 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 dihydrosanguinarine fumarate crystals, filter out dihydrosanguinarine fumarate crystals, wash with ethanol and dry under vacuum at 50°C , 4.47 g of product were obtained.

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Abstract

The invention relates to fumarate or pharmacological acceptable solvates of dihydrosanguinarine and derivatives of the dihydrosanguinarine as well as an application of the fumarate or pharmacological acceptable solvates to the preparation of drugs for treating hepatitis B.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to dihydrosanguinarine organic acid salt 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. Some of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/153A61K31/4741A61P1/16A61P31/20
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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