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Salts of delta 11,12-antofine derivatives

A technology of tofin and drugs, applied in the field of medicinal chemistry, can solve problems such as adverse reactions, drug resistance, and unsatisfactory therapeutic effects, 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 drugs for the treatment of cancer, these existing drugs are likely to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • Salts of delta 11,12-antofine derivatives
  • Salts of delta 11,12-antofine derivatives
  • Salts of delta 11,12-antofine derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Apoprofen fumarate

[0048] Dissolve 3.61 g (0.01 mol) of the compound apoprofen and 1.17 g (0.01 mol) of fumaric acid in 100 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 apoprofen fumarate crystals, and apoprofen fumarate is filtered out Salt crystals were washed with ethanol and dried under vacuum at 50°C to obtain 4.76 g of product.

Embodiment 2

[0050] Apoprofen fumarate

[0051] Stir 3.61 g of the compound apoprofen fumarate and 1.17 g of fumaric acid in 100 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. After standing for several hours in a temperature environment of 0-5°C, the crystals of apoantifen fumarate are precipitated, and the crystals of apoantifen fumarate are filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 4.74 g of product.

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Abstract

The invention relates to fumarates of delta 11,12-antofine and delta 11,12-antofine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparing drugs for treating cancers.

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 alkaloid apoantofine (Δ11,12-antofine) 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 produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal. Some active compounds for treating cancer are described in the Chinese invention patent application publication number CN 101962381A. 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. Som...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07C57/15A61K31/437A61P35/00
CPCC07D471/04
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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