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Salts of antofine derivatives

A technology of altofen and a drug, applied to the organic acid salt of the alkaloid altofen and its pharmaceutical application field, can solve the problems of adverse reactions, unsatisfactory treatment effect, drug resistance and the like, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2014-01-15
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 antofine derivatives
  • Salts of antofine derivatives
  • Salts of antofine derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Antofen fumarate

[0048] Dissolve 3.63 g (0.01 mol) of the compound Antufen 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, and the crystals of Antufen fumarate were precipitated, and the crystals of Antufen fumarate were filtered out. Washing with ethanol and drying under vacuum at 50°C yielded 4.77 g of product.

Embodiment 2

[0050] Antofen fumarate

[0051] Stir 3.63 g of the compound Antufen fumarate and 1.17 g of fumaric acid in 100 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. After standing for several hours in a temperature environment of 0-5°C, the crystals of Antufen fumarate were precipitated, and the crystals of Antufin fumarate were filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 4.75 g of the product.

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Abstract

The invention relates to fumarates of antofine and antofine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparing drugs for treating cancers.

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 alkaloid antofine and its pharmaceutical application. Background technique [0002] For now, although there are many kinds of drugs for treating 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. Some active compounds for treating cancer are described in the Chinese invention patent application publication number CN 101962381 A. 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 compounds...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07C57/15A61K31/437A61P35/00
CPCC07D471/04
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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