发明名称 AMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3-BETA INHIBITORS
摘要 This invention concerns a compound of formula (I' ),a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-member ed 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)amin o; 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.
申请公布号 CA2463821(A1) 申请公布日期 2003.05.08
申请号 CA20022463821 申请日期 2002.10.29
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 LEWI, PAULUS JOANNES;LACRAMPE, JEAN FERNAND ARMAND;JANSSEN, PAUL ADRIAAN JAN;EMBRECHTS, WERNER CONSTANT JOHAN;WILLEMS, MARC;KUKLA, MICHAEL JOSEPH;DE JONGE, MARC RENE;NUYDENS, RONY MARIA;HEERES, JAN;GEERTS, HUGO ALFONS GABRIEL;BUIJNSTERS, PETER JACOBUS JOHANNES ANTONIUS;FREYNE, EDDY JEAN EDGARD;KOYMANS, LUCIEN MARIA HENRICUS;LUDOVICI, DONALD WILLIAM;DAEYAERT, FREDERIK FRANS DESIRE;MERCKEN, MARC HUBERT
分类号 A61K31/44;A61K31/4409;A61K31/505;A61K31/506;A61K31/5377;A61P3/10;A61P7/00;A61P17/00;A61P21/04;A61P25/00;A61P25/04;A61P25/16;A61P25/18;A61P25/24;A61P25/28;A61P29/00;A61P35/00;A61P43/00;C07D213/81;C07D213/82;C07D239/42;C07D401/12;C07D403/12;C07D403/14;C07D405/12;C07D407/12;C07D413/12;C07D413/14;C07D417/12;(IPC1-7):C07D213/82 主分类号 A61K31/44
代理机构 代理人
主权项
地址