Amide derivatives as glycogen synthase kinase 3-beta inhibitors

This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl...

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Hauptverfasser: EMBRECHTS WERNER CONSTANT J, BUIJNSTERS PETER JACOBUS JOHANNES A, HEERES JAN, DE JONGE MARC R, KOYMANS LUCIEN MARIA H, WILLEMS MARC, MERCKEN MARC H, ARTS THEODORA JOANNA F, DAEYAERT FREDERIK FRANS D, LACRAMPE JEAN FERNAND A, JANSSEN MAROUSSIA GODELIEVE F, FREYNE EDDY JEAN E, JANSSEN GRAZIELLA M.C, JANSSEN PAUL ADRIAAN J, NUYDENS RONY M, JANSSEN HERWIG JOSEPHUS M, LEWI PAULUS J, JANSSEN PAUL P.M, JANSSEN JASMINE J.W
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Sprache:eng
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Zusammenfassung:This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(-O)-; R21-S(-O)p-; R7-S(-O)p-; R7-S(-O)p-NH-; R21-S(-O)p-NH-; R7-C(-O)-; -NHC(-O)H; -C(-O)NHNH2; R7-C(-O)-NH-; R21-C(-O)-NH-; -C(-NH)R7; -C(-NH)R21; R4a or R4b each independently represent hydrogen, R8, -Y1-NR9-Y2-NR10R11, -Y1-NR9-Y1-R8, -Y1-NR9R10; provided that -X-R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.