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Salts of evodiamine derivatives

A technology of evodiamine and its compounds, applied in the field of organic acid salts of evodiamine and its pharmaceutical application, can solve problems such as adverse reactions, unsatisfactory therapeutic effects, and drug resistance, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2014-05-07
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 cancer, 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.

Method used

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  • Salts of evodiamine derivatives
  • Salts of evodiamine derivatives
  • Salts of evodiamine derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Evodiamine fumarate

[0048] The compound evodia base 3.03 g (0.01 mol) and fumaric acid 1.17 g (0.01 mol) were dissolved in 90 ml of boiling ethanol. This hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and allowed to stand for several hours in a temperature environment of 0-5°C to precipitate evodia base fumarate crystals and filter out evodia base fumarate crystals. It was washed with ethanol and dried under vacuum at 50°C to obtain 4.18 g of product.

Embodiment 2

[0050] Evodiamine fumarate

[0051] The compound evodialine fumarate 3.03 g and fumaric acid 1.17 g 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 to room temperature while stirring. After standing for several hours in a temperature environment of 0-5°C, evodia base fumarate crystals were precipitated, and the evodia base fumarate crystals were filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 4.15 g of product.

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Abstract

The invention relates to fumarates of evodiamine and evodiamine derivatives or pharmaceutically acceptable solvates of the fumarates, and their use in preparation of drugs for treating cancers.

Description

Invention field [0001] The present invention relates to the field of medicinal chemistry. Specifically, the present invention relates to the organic acid salt of evodia base and its pharmaceutical application. Background technique [0002] At present, although there are many kinds of drugs for the treatment of cancer, these existing drugs are prone to cause many and serious adverse reactions, and some produce drug resistance, and the therapeutic effects of the existing drugs are still not ideal. The Chinese Patent Application Publication No. CN101991575A describes some compounds with cancer treatment activity. Summary of the invention [0003] The present invention discloses certain new compounds, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and pharmaceutical applications of these compounds and compositions. [0004] These compounds show good water solubility stability and solid form stability. Some of these compounds show partic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14A61K31/519A61P35/00
CPCC07D471/14
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH