Salt of chelerythrine derivative

A technique for chelerythrine and a drug, which is applied to the organic acid salt of chelerythrine and its pharmaceutical application field, can solve problems such as adverse reactions, unsatisfactory drug treatment effects, drug resistance and the like, 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

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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...

Method used

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  • Salt of chelerythrine derivative
  • Salt of chelerythrine derivative
  • Salt of chelerythrine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] chelerythrine fumarate

[0048] Dissolve 3.50 g (0.01 mol) of the compound chelerythrine and 1.17 g (0.01 mol) of fumaric acid in 80 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, chelerythrine fumarate crystals are precipitated, and chelerythrine is filtered out The fumarate salt crystals were washed with ethanol and dried under vacuum at 50°C to yield 4.63 g of product.

Embodiment 2

[0050] chelerythrine fumarate

[0051] Stir 3.50 g of the compound chelerythrine 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, chelerythrine fumarate crystals are precipitated, filter out chelerythrine fumarate crystals, wash with ethanol and dry under vacuum at 50°C , 4.61 g of product were obtained.

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Abstract

The invention relates to chelerythrine, fumarate of a derivative of the chelerythrine or a pharmaceutically acceptable solvate of the chelerythrine and applications of the chelerythrine, the fumarate and the solvate in preparation of medicaments for treating hepatitis B.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to chelerythrine 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 these c...

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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