C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 261/12 (2006.01) A61K 31/42 (2006.01) C07D 261/18 (2006.01)
Patent
CA 2400290
A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5- methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4- trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.
L'invention concerne un procédé permettant d'effectuer la synthèse du léflunomide à partir de l'acide 5-methylisoxazole-4-carboxylique et de 4-trifluoromethylaniline. L'invention concerne également le léflunomide préparé à partir du procédé de l'invention, ledit léflunomomide ne présentant sensiblement aucune difficulté à se séparer des impuretés souvent trouvées dans le léflunomide préparé au moyen des procédés connus, notamment N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamise et N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. L'invention concerne également des formes de composition et des dosage pharmaceutiques contenant du léflunomide très pur, et des procédés de traitement de maladies à l'aide dudit léflunomide.
Avrutov Ilya
Gershon Neomi
Liberman Anita
Ridout & Maybee Llp
Teva Pharmaceutical Industries Ltd.
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