AMIDDERIVATE ALS INHIBITOREN DER GLYCOGENSYNTHASEKINASE-3-BETA

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: BUIJNSTERS, PETER JACOBUS JOHANNES ANTONIUS, LACRAMPE, JEAN FERNAND ARMAND, DE JONGE, MARC RENE, FREYNE, EDDY JEAN EDGARD, WILLEMS, MARC, JANSSEN, MAROUSSIA GODELIEVE, JANSSEN, GRAZIELLA MARIA, MERCKEN, MARC HUBERT, JANSSEN, PAUL PETER, EMBRECHTS, WERNER CONSTANT JOHAN, LEWI, PAULUS JOANNES, ARTS, THEODORA JOANNA, JANSSEN, PAUL ADRIAAN JAN, DAEYAERT, FREDERIK FRANS DESIRE, HEERES, JAN, KOYMANS, LUCIEN MARIA HENRICUS, GEERTS, HUGO ALFONS, KUKLA, MICHAEL JOSEPH, LUDOVICI, DONALD WILLIAM, NUYDENS, RONY MARIA, JANSSEN, JASMIN JOSEE, JANSSEN, HERWIG JOSEPHUS
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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.