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Cytisine derivative

A technology of cytisine and its derivatives, which is applied in the field of organic acid salts of cytisine derivatives and its pharmaceutical applications, can solve problems such as adverse reactions, easy drug resistance, and unsatisfactory therapeutic effects, and achieve practical treatment active effect

Inactive Publication Date: 2015-06-17
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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Cytisine Derivative Maleate

[0048] Dissolve 0.32 g (1 mmol) of the compound cytisine derivative and 0.12 g (1 mmol) of maleic acid in 10 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, cytisine derivative maleate crystals are precipitated, and cytisine is filtered out The derivative maleate salt crystals were washed with cold ethanol and dried under vacuum at 50°C to obtain 0.43 g of product.

Embodiment 2

[0050] Cytisine Derivative Maleate

[0051] Stir 0.32 g of the compound cytisine derivative 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, the cytisine derivative maleate crystals are precipitated, the cytisine derivative maleate crystals are filtered out, washed with cold ethanol and vacuumed at 50°C Drying under low conditions yielded 0.42 g of product.

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Abstract

The invention relates to a cytisine derivative maleate or its pharmaceutically acceptable solvate and an application of the cytisine derivative maleate or its pharmaceutically acceptable solvate in preparation of medicines for treating tumors.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to organic acid salts of cytisine derivatives and their 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 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. CN102952134A. 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. S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/18A61K31/439A61P35/00
CPCC07D471/18
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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