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Salts of nuciferine derivatives

A technology of nuciferine and medicine, which is applied in the organic acid salt of nuciferine and its pharmaceutical application field, can solve problems such as adverse reactions, easy drug resistance, and unsatisfactory therapeutic effect, 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 acetylcholinesterase inhibitors, 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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  • Salts of nuciferine derivatives
  • Salts of nuciferine derivatives
  • Salts of nuciferine derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Nuciferine fumarate

[0048] The compound nuciferine 2.95 g (0.01 mol) and fumaric acid 1.17 g (0.01 mol) were dissolved in 80 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 at a temperature of 0-5°C to precipitate nuciferine fumarate crystals and filter out nuciferine fumarate crystals , washed with ethanol and dried under vacuum at 50°C to yield 4.10 g of product.

Embodiment 2

[0050] Nuciferine fumarate

[0051] 2.95 g of the compound nuciferine fumarate and 1.17 g of fumaric acid were stirred in 80 ml of refluxing ethanol until all the solids were 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 nuciferine fumarate crystals were precipitated, the nuciferine fumarate crystals were filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 4.08 g of the product .

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Abstract

The invention relates to fumarates of nuciferine and nuciferine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparation of acetylcholinesterase inhibitor drugs.

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 nuciferine and its pharmaceutical application. Background technique [0002] For now, although there are many kinds of acetylcholinesterase inhibitors, 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 compounds with acetylcholinesterase inhibitory activity are described in the patent of China Invention Patent Authorization No. CN 101712649 B. 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 ...

Claims

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Application Information

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IPC IPC(8): C07D221/18C07C57/15C07C51/41A61K31/473A61P25/28A61P27/06A61P1/00A61P21/04
CPCC07D221/18
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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