Azabicycloalkyl derivatives of imidazo(1,5-a)indol-3-one and...

C - Chemistry – Metallurgy – 07 – D

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C07D 519/00 (2006.01) A61K 31/435 (2006.01) C07D 451/04 (2006.01) C07D 451/14 (2006.01) C07D 453/02 (2006.01)

Patent

CA 2166621

Novel 5-HT3 receptor antagonist compounds having general formula (I) wherein each of R, R1 and R2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C1-C6 alkyl, CF3, C1-C6 alkoxy, C1-C6 alkylthio, formyl, C2-C6 alkanoyl, carboxy, C1-C6 alkoxy-carbonyl, nitro, -N(R4 R5) in which each of R4 and R5 independently is hydrogen, C1-C6 alkyl, formyl or C2- C6 alkanoyl; or a (R6 R7)N-SO2 group, in which each of R6 and R7 independently is hydrogen or C1-C6 alkyl; R3 is a group (a) or (b) wherein n is an integer of 1 or 2 and R8 is hydrogen, C1-C6 alkyl unsubstituted or substituted by phenyl, C2-C4 alkenyl, C2-C4 alkynyl, formyl or C2-C6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.

Cette invention se rapporte à de nouveaux composés antagonistes du récepteur 5-HT3, qui sont représentés par la formule générale (I), où chacun des éléments R, R1 et R2, qui peuvent être identiques ou différents, représente hydrogène, halogène, hydroxy, cyano, alkyle C1-C6, CF3, alcoxy C1-C6, alkylthio C1-C6, formyle, alcanoyle C2-C6, carboxy, alcoxy-carbonyle C1-C6, nitro, -N(R4 R5), où chacun des éléments R4 et R5 représente séparément hydrogène, alkyle C1-C6, formyle ou alcanoyle C2-C6; ou un groupe (R6 R7)N-SO2, où chacun des éléments R6 et R7 représente séparément hydrogène ou alkyle C1-C6; R3 représente un groupe (a) ou (b), où n représente un nombre entier égal à 1 ou à 2 et R8 représente hydrogène, alkyle C1-C6 insubstitué ou substitué par phényle, alcényle C2-C4, alcynyle C2-C4, formyle ou alcanoyle C2-C6; ainsi qu'aux sels de ces composés qui soient acceptables sur le plan pharmaceutique.

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