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Salt of quinoline benzamide derivative

A technology of benzamide and quinoline, 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: 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 quinoline benzamide derivative
  • Salt of quinoline benzamide derivative
  • Salt of quinoline benzamide derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] N-[5-(9H-Purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide fumarate

[0048] Compound N-[5-(9H-purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide 4.5 grams (0.01mol) and fumaric acid 1.17 grams ( 0.01mol) was dissolved in 100ml 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 N-[5-(9H-purin-6-yloxy)-quinone Phenyl-8-yl]-3-trifluoromethyl-benzamide fumarate crystals, N-[5-(9H-purin-6-yloxy)-quinolin-8-yl]- 3-Trifluoromethyl-benzamide fumarate crystals were washed with ethanol and dried under vacuum at 50°C, yielding 5.66 g of product.

Embodiment 2

[0050] N-[5-(9H-Purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide fumarate

[0051] Compound N-[5-(9H-purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide fumarate 4.5 grams and fumaric acid 1.17 grams in Stir in 100 ml of refluxing 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, N-[5-(9H-purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide is precipitated Fumarate crystals, filter out N-[5-(9H-purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide fumarate crystals, and Washing with ethanol and drying under vacuum at 50°C yielded 5.65 g of product.

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Abstract

The invention relates to N-[5-(9H-purine-6-yloxy)-quinoline-8-yl]-3-(trifluoromethyl)-benzamide 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 N-[5-(9H-purin-6-yloxy)-quinolin-8-yl]-3-trifluoromethyl-benzamide organic Salts and their 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 patent application publication number CN 101296928A 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 good water solubility stability and solid for...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P35/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH