Acid amide derivatives and process for the preparation thereof

Details Acid amide derivatives and process for the preparation thereof Acid amide derivatives and process for the preparation thereof

C - Chemistry, Metallurgy

07

D

C07D 241/44 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2190532

The invention relates to new acid amide derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said acid amide derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The new compounds according to the invention can be characterized by formula (I), wherein R1 represents hydrogen or nitro, R2 and R3 stand, independently from each other, for hydrogen, lower alkyl or lower alkenyl optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated heteroring containing 1 or 2 nitrogen and/or oxygen atom(s); or R2 and R3 form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group containing optionally 1 or 2 additional nitrogen atoms and/or oxygen atom(s), said ring optionally carrying a hydroxy or a hydroxy-lower alkyl group, and possess valuable AMPA and kainate antagonizing properties, so they can be used to advantage in the therapy.

Nouveaux dérivés d'amide acide, leur procédé de préparation, compositions pharmaceutiques les comportant, et application desdits dérivés d'amide acide au traitement de maladies et à la préparation de compositions pharmaceutiques utilisables dans le traitement de maladies. Ces nouveaux composés peuvent être caractérisés par la formule (I), dans laquelle R?1¿ représente hydrogène ou nitro; R?2¿ et R?3¿, indépendamment l'un de l'autre, représentent hydrogène, alkyle inférieur ou alcényle inférieur portant éventuellement un substituant sélectionné dans le groupe constitué d'halogène, hydroxy, alcoxy inférieur, di(alkyle inférieur)amino, phénylalcoxy inférieur-carbonyle et un hétérocycle saturé pentagonal ou hexagonal contenant 1 ou 2 atomes d'azote et/ou d'oxygène; ou R?2¿ et R?3¿, pris ensemble avec l'atome d'azote adjacent, forment un groupe hétérocyclique saturé hexagonal contenant éventuellement 1 ou 2 atomes supplémentaires d'azote et/ou d'oxygène, ledit cycle portant éventuellement un groupe hydroxy-alkyle inférieur ou hydroxy; et ces nouveaux composés présentent de précieuses propriétés antagonistes d'AMPA et de kaïnate, ce qui les rend avantageux dans le domaine thérapeutique.

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