2-substituted-1-piperidyl benzimidazole compounds as...

Details 2-substituted-1-piperidyl benzimidazole compounds as... 2-substituted-1-piperidyl benzimidazole compounds as...

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/445 (2006.01) C07D 211/58 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2339621

A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1- C7)alkyl or (C2-C5)alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri-substituted (C1-C10)alkyl-M-, (C3-C7)cycloalkyl-M-, (C2- C6)alkenyl-M-, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M-, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M-, aryl-M-, aromatic or non-aromatic heterocyclic-M-, aryl-(C1-C5)alkyl-M- or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M-, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

La présente invention concerne un composé représenté par la formule générale (I) ou l'un de ses sels pharmaceutiquement acceptables. Ce composé qui pésente une activité agoniste du récepteur ORL-1, convient comme analgésique ou analogue chez des mammifères. Dans cette formule R est (C3-C11)cycloalkyle ou (C3-C11)cycloalcényle non substitué, mono-, di- ou tri-substitué ou analogue. A est (C1-C7)alkyle ou (C2-C5)alcényle non substitué ou aryle non substitué, mono-, di- ou tri-substitué ou analogue. Y est hydrogène, halo, amino ou mercapto, ou (C1-C10)alkyl-M- non substitué, mono-, di- ou tri-substitué ou analogue, (C3-C7)cycloalkyl-M-, (C2-C6)alcényl-M-, (C1-C4)alkyl)-NH-((C1-C4)alkyl)-M-, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M-, aryl-M-, -M- hétérocyclique aromatique ou non-aromatique, aryl-(C1-C5)alkyl-M- ou -(C1-C5)alkyl-M- hétérocyclique aromatique ou non-aromatique, ou analogue. En l'occurrence, M est O à liaison covalente, S, NH ou analogue. Z<1>, Z<2>, Z<3> et Z<4> sont hydrogène ou analogue.

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