- 专利标题: Amide derivatives as glycogen synthase kinase 3-β inhibitors
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申请号: US10493454申请日: 2002-10-29
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公开(公告)号: US07183288B2公开(公告)日: 2007-02-27
- 发明人: Paul Adriaan Jan Janssen, deceased
- 申请人: Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Jean Fernand Armand Lacrampe , Herwig Josephus Margareta Janssen, legal representative , Paul Peter Maria Janssen, legal representative , Graziella Maria Constantina Janssen, legal representative , Jasmine Josée Werner Janssen, legal representative , Maroussia Godelieve Frank Janssen, legal representative , Theodora Joanna Francisca Arts , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Michael Joseph Kukla , Hugo Alfons Gabriel Geerts , Rony Maria Nuydens , Marc Hubert Mercken , Donald William Ludovici
- 优先权: EP01204193 20011101
- 国际申请: PCT/EP02/12067 WO 20021029
- 国际公布: WO03/037869 WO 20030508
- 主分类号: A61K31/505
- IPC分类号: A61K31/505 ; C07D239/42
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 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.
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