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1. 发明申请

US20060205721A1 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
公开(公告)号：US20060205721A1
公开(公告)日：2006-09-14
申请号：US10564844
申请日：2004-07-12
申请人： Eddy Edgard Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijinsters
发明人： Eddy Edgard Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijinsters
IPC分类号： A61K31/5377 , A61K31/519 , C07D487/02
CPC分类号： C07D487/04
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 phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; or C1-6alkyloxyC1-6alkylcarbonyl optionally substituted with C1-6alkyloxycarbonyl; X represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents C3-7cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatom selected from O, S or N; benzoxazolyl or a radical of formula wherein said R2 substituent may optionally be substituted; R3 represents halo; hydroxy; optionally substituted C1-6alkyl; C2-6alkenyl or C2-6alkynyl, each optionally substituted; optionally substituted polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted polyhaloC1-6alkyloxy; C1-6alkylthio; polyhaloC1-6alkylthio; C1-6alkyl-oxycarbonyl; C1-6alkylcarbonyloxy; C1-6alkylcarbonyl; polyhaloC1-6alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR6bR7b; C(═O)—NR6bR7b; —NR5—C(═O)—NR6bR7b; —NR5—C(═O)—R5; —S(═O)n1—R8b; —NR5—S(═O)n1—R8b; —S—CN; —NR5—CN; R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; C2-4alkenyl or C2-4alkynyl, each optionally substituted; polyhaloC1-3alkyl; optionally substituted C1-4alkyloxy; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; nitro; cyano; carboxyl; NR10R11; C(═O)NR10R11; —NR5—C(═O)—NR10R11; —NR5—C(═O)—R5; —S(═O)Sn1—R12; —NR5—S(═O)n1—R12; —S—CN; —NR5—CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

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