Use of certain crystal modifications of 1-(2,6-difluorobenzyl)-1h-1,2,3-triazole-4-carboxamide in treating epilepsy

A technology of difluorobenzyl and formamide, which is applied in the direction of medical preparations containing active ingredients, drug combinations, active ingredients of heterocyclic compounds, etc.

Inactive Publication Date: 2007-02-07
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is not clear in EP199262 whether such recrystallization

Method used

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  • Use of certain crystal modifications of 1-(2,6-difluorobenzyl)-1h-1,2,3-triazole-4-carboxamide in treating epilepsy
  • Use of certain crystal modifications of 1-(2,6-difluorobenzyl)-1h-1,2,3-triazole-4-carboxamide in treating epilepsy
  • Use of certain crystal modifications of 1-(2,6-difluorobenzyl)-1h-1,2,3-triazole-4-carboxamide in treating epilepsy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Embodiment 1: Improved body B

[0076] 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide (18.29 kg) was dissolved in formic acid (89.3 kg) with stirring at 58-63°C. The above solution was added to stirred methanol (105.5 L) at 20°C to 0°C over 30 minutes and washed with formic acid (6.1 kg) to form a suspension. The product was isolated immediately by filtration and washed with cold methanol (150 L, ca. 4°C). Vacuum drying at about 60°C yields improved product B with a yield of about 94%.

Embodiment 2

[0077] Embodiment 2: Improved Body C

[0078] 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide (15.0 g) was dissolved in acetic acid (120 ml) with stirring at about 90°C. The solution was cooled to 20°C over a period of about 8 minutes, forming a suspension. The product was immediately isolated by filtration, washed with toluene (120ml) and dried under vacuum at about 60°C. The improved product C was obtained. Yield 67.3%.

preparation Embodiment 1

[0081] The active ingredient is granulated together with deionized water. Ground lactose, corn starch, Avicel PH 102, Cellulose-HP-M-603 and sodium lauryl sulfate were then added to the above mixture and further granulated with deionized water.

[0082] The resulting wet material was dried and ground. After addition of the remaining ingredients the homogeneous mixture is compressed to obtain tablet cores having the above content of active ingredient.

[0083] The tablet cores are coated with a coating consisting of suitable ingredients dissolved or suspended in water or a small amount of ethanol containing 5% isopropanol.

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Abstract

The invention relates to the novel modification C of the compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide of formula (I), its use for the treatment of epilepsy, and pharmaceutical preparations comprising this crystal modification.

Description

[0001] Amide crystal modification and use thereof [0002] The application number is 98805675.5, the application date is June 8, 1998, and the invention name is "1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide The divisional application of the Chinese patent application of the improved crystalline body and its use as an antiepileptic drug. technical field [0003] The present invention relates to a crystal modified body of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide and its use as an antiepileptic drug. Background technique [0004] Compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide represented by the following formula: [0005] [0006] It has been described, eg in Example 4, in European Patent Application Publication No. 0 199 262 A2 (EP 199262). This compound exhibits valuable pharmacological properties; it can therefore be used, for example, as an antiepileptic drug. Compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide is a...

Claims

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Application Information

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IPC IPC(8): C07D249/06A61K31/4192A61P25/08A61K31/41C07D249/04
CPCC07D249/04A61P25/08
Inventor R·波特曼U·C·霍夫梅尔A·布克哈德W·谢尔M·司泽拉吉维茨
Owner NOVARTIS AG
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