Isoxazole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 261/12 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) C07D 261/10 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2247439

Isoxazole derivatives represented by general formula (I), which have an excellent monoamine oxidase inhibitory activity and are useful for the treatment or prevention of nervous diseases such as depression, wherein R1 represents optionally substituted aryl or optionally substituted heteroaryl; R2 represents hydrogen, halogeno, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkoxy, cyano, carboxy, alkanoyl, alkoxycarbonyl, or optionally substituted carbamoyl; R3 represents optionally substituted amino or saturated heterocyclic group; X represents oxygen or sulfur; and n is an integer of 2 to 6.

Cette invention concerne des dérivés d'isoxazole qui correspondent à la formule générale (I) où R?1¿ représente aryle éventuellement substitué ou hétéroaryle éventuellement substitué; R?2¿ représente hydrogène, halogéno, alkyle éventuellement substitué, alcényle, alcynyle, cycloalkyle, cycloalcényle, alcoxy, cyano, carboxy, alcanoyle, alcoxycarbonyle ou carbamoyle éventuellement substitué; R?3¿ représente amino éventuellement substitué ou un groupe hétérocyclique saturé; X représente oxygène ou soufre; et n est un nombre entier allant de 2 à 6. Ces dérivés possèdent une excellente activité inhibitrice de monoamine oxydase, et peuvent être utilisés dans le traitement ou la prévention de maladies nerveuses telle que la dépression.

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