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Salts of conessine derivative

A kind of technology of antisepsis 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 to produce drug resistance, etc., 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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  • Salts of conessine derivative
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  • Salts of conessine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Conic Mineral Fumarate

[0048] Dissolve 3.43 g (0.01 mol) of the compound trismin (0.01 mol) and 1.17 g (0.01 mol) of fumaric acid in 90 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 crystals of azimin fumarate are precipitated, and azizimin fumarate is filtered out The crystals, washed with ethanol and dried under vacuum at 50°C, yielded 4.59 g of product.

Embodiment 2

[0050] Conic Mineral Fumarate

[0051] Stir 3.43 g of the compound trismin fumarate and 1.17 g of fumaric acid in 90 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 crystals of trismin fumarate are precipitated, the crystals of trismin fumarate are filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 4.57 g product.

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Abstract

The invention relates to fumarate or pharmaceutically acceptable solvates of a conessine derivative and application of fumarate or the pharmaceutically acceptable solvates to prepare acetylcholinesterase inhibitor medicaments.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to organic acid salts of triuramine derivatives and their pharmaceutical applications. 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. Chinese invention patent application publication number CN 102153614A describes some compounds with acetylcholinesterase inhibitory activity. 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. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00C07C57/15C07C51/41A61K31/58A61P43/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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