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 should be specially adopted or carried out under specific conditions

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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PUM

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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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