发明名称 Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (GSK3 inhibitors)
摘要 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 is 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 a direct bond or a linker atom or group; 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; R4 is an optionally substituted heterocycle provided that -X-R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
申请公布号 US7514445(B2) 申请公布日期 2009.04.07
申请号 US20040493452 申请日期 2004.04.23
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 FREYNE EDDY JEAN EDGARD;BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS;WILLEMS MARC;EMBRECHTS WERNER CONSTANT JOHAN;LOVE CHRISTOPHER JOHN;JANSSEN PAUL ADRIAAN JAN;LEWI PAULUS JOANNES;HEERES JAN;DE JONGE MARC RENE;KOYMANS LUCIEN MARIA HENRICUS;VINKERS HENDRIK MAARTEN;VAN AKEN KOEN JEANNE ALFONS;DIELS GASTON STANISLAS MARCELLA
分类号 A61K31/506;A61K31/435;A61K31/4406;A61K31/50;A61K31/501;A61K31/505;A61K31/5377;A61P3/10;A61P17/00;A61P21/04;A61P25/00;A61P25/02;A61P25/04;A61P25/16;A61P25/18;A61P25/24;A61P25/28;A61P29/00;A61P31/18;A61P35/00;A61P35/02;C07D213/53;C07D213/74;C07D239/42;C07D239/48;C07D401/04;C07D401/12;C07D403/04;C07D403/06;C07D403/12;C07D403/14;C07D405/12;C07D409/12;C07D417/12 主分类号 A61K31/506
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