Salt of cyclopropane-carboxylic acid amide derivative

A technology of cyclopropane carboxylic acid and amide, which is applied in the direction of drug combination, organic chemistry, antineoplastic drugs, etc., can solve problems such as adverse reactions, drug resistance, and unsatisfactory therapeutic effects, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2013-08-14
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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  • Salt of cyclopropane-carboxylic acid amide derivative
  • Salt of cyclopropane-carboxylic acid amide derivative
  • Salt of cyclopropane-carboxylic acid amide derivative

Examples

Experimental program
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Effect test

Embodiment 1

[0047] Cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide fumarate

[0048] Compound cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide 4.1 grams (0.01mol) and fumaric acid 1.17 grams (0.01 mol) was dissolved in 100 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood for several hours at a temperature of 0-5°C to precipitate cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-benzene Cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidine-4- Amino]phenyl}-amide fumarate crystals were washed with ethanol and dried under vacuum at 50°C to obtain 5.25 g of product.

Embodiment 2

[0050] Cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide fumarate

[0051] Compound cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide fumarate 4.1 grams and fumaric acid 1.17 grams in reflux Stir in 100 ml of ethanol until all 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, cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide rich Mamate salt crystals, cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide fumarate crystals were filtered off and washed with ethanol and dried under vacuum at 50°C to yield 5.2 g of product.

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Abstract

The invention relates to cyclopropane-carboxylic acid {3-[6-(3-(trifluoromethyl)-phenylamino)-pyrimidine-4-yl-amino]-phenyl}-amide and a derivative fumarate or a pharmaceutically acceptable solvate thereof, and an application thereof in preparation of medicines for treating cancers.

Description

field of invention [0001] The present invention relates to the field of medicinal chemistry, in particular, the present invention relates to cyclopropanecarboxylic acid {3-[6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino]phenyl}-amide organic acid Salt and its pharmaceutical applications. 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. Chinese invention patent application publication number CN 101300234A describes some active compounds for treating cancer. 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/48A61K31/505A61P35/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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