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Salts of isoxazole derivatives

A technology of isoxazole and isopropyl, applied in the field of medicinal chemistry, can solve problems such as adverse reactions and unsatisfactory therapeutic effects, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2013-05-08
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 drugs are likely to cause many and severe adverse reactions, and the therapeutic effect of some drugs is still not ideal.

Method used

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  • Salts of isoxazole derivatives
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  • Salts of isoxazole derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-formylethylamide fumarate salt

[0048] 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-formylethylamide 46.6 gram (0.1mol) and 11.7 (0.1mol) grams of fumaric acid were dissolved in 1000 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood at a temperature of 0-5°C for several hours to precipitate 5-(2,4-dihydroxy-5-isopropyl-phenyl )-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-formylethylamide fumarate crystals, 5-(2,4-dihydroxy-5- Crystals of isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylethylamide fumarate, washed with ethanol and vacuumed at 50 °C Drying under low conditions yielded 52.9 g of product.

Embodiment 2

[0050] 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-formylethylamide fumarate salt

[0051] 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-formylethylamide 45.9 g of maleate and 11.7 g of fumaric acid were stirred in 1000 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, 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-benzene was precipitated base)-isoxazole-3-formylethylamine fumarate crystals, 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholine-4 Crystals of -(-methyl-phenyl)-isoxazole-3-carboxylethylamide fumarate were washed with ethanol and dried under vacuum at 50°C to yield 53.6 g of product.

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Abstract

The invention relates to applications of fumarates of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholine-4-yl-methyl-phenyl)-isoxazole-3-ethylformamide and derivatives thereof, or pharmaceutically acceptable solvates in the preparation of medicines for treating cancers.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl) Organic acid salts of )-isoxazole-3-carboxamide and pharmaceutical applications thereof. Background technique [0002] For now, although there are many kinds of drugs for treating cancer, these existing drugs are likely to cause many and severe adverse reactions, and the therapeutic effect of some drugs is still not ideal. Chinese Invention Patent Granted Publication No. CN 1771235B 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 form stability. Some of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D261/18A61K31/5377A61P35/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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