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Conimine derivative salts

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

Inactive Publication Date: 2014-05-07
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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  • Conimine derivative salts
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Conic imine fumarate

[0048] Dissolve 3.29 g (0.01 mol) of the compound conesimine and 1.17 g (0.01 mol) of fumaric acid in 90 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, and the crystals of conesimine fumarate were precipitated, and the conesine fumarate was filtered out. Salt crystals were washed with ethanol and dried under vacuum at 50°C to yield 4.45 g of product.

Embodiment 2

[0050] Conic imine fumarate

[0051] 3.29 g of the compound conesimine fumarate and 1.17 g of fumaric acid were stirred in 90 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 crystals of conesimine fumarate are precipitated, the crystals of conesine fumarate are filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 4.44 g of product.

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Abstract

The invention relates to fumarates of conimine derivatives or pharmaceutically acceptable solvates of the fumarates, and their use in preparation of an acetylcholinesterase inhibition drug.

Description

field of invention [0001] The present invention relates to the field of medicinal chemistry, in particular, the present invention relates to organic acid salts of conesimine derivatives and their 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 Chinese invention patent application publication number CN102153614A. 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 a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/58A61P43/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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