Tetrahydropalmatine derivative

A technology of derivatives and drugs, applied in the field of organic acid salts of tetrahydropalmatine derivatives and their pharmaceutical applications, can solve problems such as adverse reactions, easy drug resistance, and unsatisfactory therapeutic effects, and achieve the effect of practical therapeutic activity

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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  • Tetrahydropalmatine derivative
  • Tetrahydropalmatine derivative
  • Tetrahydropalmatine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Tetrahydropalmatine Derivatives Maleate

[0048] Dissolve 0.37 g (1 mmol) of the compound tetrahydropalmatine derivatives 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, and the maleate crystals of the derivatives of tetrahydropalmatine are precipitated, and the derivatives of tetrahydropalmatine are filtered out The maleate salt crystals were washed with cold ethanol and dried under vacuum at 50°C to yield 0.50 g of product.

Embodiment 2

[0050] Tetrahydropalmatine Derivatives Maleate

[0051] Stir 0.36 g of the compound tetrahydropalmatine 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. Standing for several hours in a temperature environment of 0-5°C, the crystals of the maleic acid salt of the derivatives of tetrahydropalmatine are precipitated, the crystals of the maleic acid salt of the derivatives of tetrahydropalmatine are filtered out, washed with cold ethanol and placed under vacuum at 50°C Drying yielded 0.47 g of product.

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Abstract

The invention relates to a tetrahydropalmatine derivative maleate or its pharmaceutically acceptable solvate and an application of the tetrahydropalmatine 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 an organic acid salt of a tetrahydropalmatine derivative 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 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. CN101830897A. 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 s...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07C51/41C07C57/145A61K31/4375A61P35/00
CPCC07D455/03
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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