A lycobetaine derivative

A technology of lycorine oxide and compound, which is applied in the directions of organic chemistry, drug combination, carboxylate preparation, etc., can solve the problems of adverse reactions, easy generation of drug resistance, unsatisfactory therapeutic effect, etc., and achieves the effect of practical therapeutic activity

Inactive Publication Date: 2015-06-10
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 are prone to drug resistance, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • A lycobetaine derivative
  • A lycobetaine derivative
  • A lycobetaine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Lycorine oxide maleate

[0048] Dissolve 0.266 g (1 mmol) of the compound lycorine oxide and 0.12 g (1 mmol) of maleic acid in 10 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood for several hours at a temperature of 0-5°C to precipitate lycorine oxide maleate crystals, and lycorine oxide maleate was filtered out. Salt crystals were washed with cold ethanol and dried under vacuum at 50°C to obtain 0.38 g of product.

Embodiment 2

[0050] Lycorine oxide maleate

[0051] Stir 0.26 g of the compound lycorine oxide maleate and 0.12 g of maleic acid in 10 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 lycorine oxide maleate crystals, filter out lycorine oxide maleate crystals, wash with cold ethanol and dry under vacuum at 50°C, Yield 0.32 g of product.

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Abstract

The invention relates to lycobetaine maleate or pharmaceutically acceptable solvates thereof, and applications thereof in preparation of medicines inhibiting tumor.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to organic acid salts of oxylycorine derivatives and pharmaceutical applications thereof. 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 are prone to drug resistance, and the therapeutic effect of the existing drugs is still not ideal. Some active compounds for treating cancer are described in the patent document of Chinese Invention Patent Application Publication No. CN102772362A. 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 stabili...

Claims

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Application Information

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IPC IPC(8): C07D491/16C07C57/145C07C51/41A61K31/4745A61P35/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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