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Salts of indolone derivatives

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

Inactive Publication Date: 2013-05-29
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 indolone derivatives
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  • Salts of indolone derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] (E)-1,3-Dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one fumarate

[0048] 29.7 grams (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 (E)-1,3-dihydro-5,6-dimethoxy -3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one fumarate crystals, and (E)-1,3-dihydro-5,6-dimethyl Crystals of oxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one fumarate were washed with ethanol and dried under vacuum at 50°C to yield 36.6 g of product.

Embodiment 2

[0050] (E)-1,3-Dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one fumarate

[0051] Compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one fumarate 29.8 G 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. After standing for several hours in a temperature environment of 0-5°C, (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]- 2H-indol-2-one fumarate crystals, (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene] filtered off - 2H-indol-2-one fumarate crystals, washed with ethanol and dried under vacuum at 50°C, yielding 37.2 g of product.

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Abstract

The invention relates to (E)-1, 3-dihydro-5, 6-dimethoxy-3-[(4-hydroxyphenyl) methylene]-2H-indol-2-ketone, fumarates of derivatives thereof or pharmaceutically acceptable solvates thereof and an application thereof to preparation of a medicament for treating cancer.

Description

field of invention [0001] The present invention relates to the field of medicinal chemistry, specifically, the present invention relates to (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H - Organic acid salts of indol-2-ones and their pharmaceutical use. 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. PCT International Application Publication No. WO 2004 / 009083 describes some compounds with activity in the treatment of 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 solubilit...

Claims

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Application Information

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IPC IPC(8): C07D209/34A61K31/404A61P35/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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