N,n'-disubstituted amide derivative

Details N,n'-disubstituted amide derivative N,n'-disubstituted amide derivative

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2131722

N,N'-disubstituted amide derivatives having potent and selective antagonistic action to 5-HT3 receptor have been developed by the present invention, which provides antagonistic drugs to 5-HT3 receptor containing novel N,N'-disubstituted amide derivatives represented by a general formula [I] (see fig. I) (wherein R1 denotes a hydrogen atom or lower alkyl group, R2 and R3, which may be identical or different, denote respectively a hydrogen atom, lower alkyl group, lower alkenyl group, nonsubstituted or substituted aryl-lower alkyl group, acyl group or lower alkoxycarbonyl group, R4 denotes a hydrogen atom, lower alkyl group or lower alkoxy group, A denotes CH or N, and n denotes 1, 2 or 3), their hydrates or acid addition salts.

Antagoniste de 5-HT3 renfermant un nouveau dérivé amide à double substitution N,N', ayant un effet antagoniste puissant et sélectif du récepteur de 5-HT3, représenté par la formule générale (I), hydrate ou sel d'addition d'acide issu de ce dérivé. Dans la formule, R1 représente hydrogène ou un alkyle inférieur; R2 et R3 peuvent être identiques ou différents l'un de l'autre et représenter indépendamment hydrogène, un alkyle inférieur, un alcényle inférieur, un alkyle inférieur à substitution aryle pouvant être substitué, un acyle ou un alcoxycarbonyle inférieur; R4 représente hydrogène, un alkyle inférieur ou un alcoxy inférieur; A représente CH ou N; et n représente 1, 2 ou 3.

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