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Salts of 14-hydroxyantofine derivative

A technology of hydroxyantaufen and drugs, which is applied in the field of medicinal chemistry, can solve problems such as adverse reactions, unsatisfactory therapeutic effects, and drug resistance, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2014-01-15
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 14-hydroxyantofine derivative
  • Salts of 14-hydroxyantofine derivative
  • Salts of 14-hydroxyantofine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] 14-Hydroxyantifen fumarate

[0048] Dissolve 3.79 g (0.01 mol) of compound 14-hydroxyantuofen 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 14-hydroxyantuofen fumarate crystals, and filter out 14-hydroxyantuofen The fumarate salt crystals were washed with ethanol and dried under vacuum at 50°C to yield 4.94 g of product.

Embodiment 2

[0050] 14-Hydroxyantifen fumarate

[0051] Stir 3.79 g of compound 14-hydroxyantuofen 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 at a temperature of 0-5°C, the crystals of 14-hydroxyantuofen fumarate were precipitated, filtered out, washed with ethanol and dried under vacuum at 50°C , 4.92 g of product were obtained.

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Abstract

The present invention relates to fumarates of 14-hydroxyantofine and 14-hydroxyantofine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparation of drugs for treating cancer.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular to an organic acid salt of alkaloid 14-hydroxyantofine (14-hydroxyantofine) 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 c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04C07C57/15C07C51/41A61K31/4745A61P35/00
CPCC07D471/04
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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