Invention Application
WO2003037869A1 AMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3-BETA INHIBITORS
审中-公开
作为GLYCOGEN SYNTHASE KINASE 3-BETA抑制剂的酰胺衍生物
- Patent Title: AMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3-BETA INHIBITORS
- Patent Title (中): 作为GLYCOGEN SYNTHASE KINASE 3-BETA抑制剂的酰胺衍生物
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Application No.: PCT/EP2002/012067Application Date: 2002-10-29
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Publication No.: WO2003037869A1Publication Date: 2003-05-08
- Inventor: FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LACRAMPE, Jean, Fernand, Armand , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
- Applicant: JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LACRAMPE, Jean, Fernand, Armand , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
- Applicant Address: Turnhoutseweg 30, B-2340 Beerse BE
- Assignee: JANSSEN PHARMACEUTICA N.V.,FREYNE, Eddy, Jean, Edgard,BUIJNSTERS, Peter, Jacobus, Johannes, Antonius,WILLEMS, Marc,EMBRECHTS, Werner, Constant, Johan,LACRAMPE, Jean, Fernand, Armand,JANSSEN, Paul, Adriaan, Jan,LEWI, Paulus, Joannes,HEERES, Jan,DE JONGE, Marc, René,KOYMANS, Lucien, Maria, Henricus,DAEYAERT, Frederik, Frans, Desire,KUKLA, Michael, Joseph,GEERTS, Hugo, Alfons, Gabriel,NUYDENS, Rony, Maria,MERCKEN, Marc, Hubert,LUDOVICI, Donald, William
- Current Assignee: JANSSEN PHARMACEUTICA N.V.,FREYNE, Eddy, Jean, Edgard,BUIJNSTERS, Peter, Jacobus, Johannes, Antonius,WILLEMS, Marc,EMBRECHTS, Werner, Constant, Johan,LACRAMPE, Jean, Fernand, Armand,JANSSEN, Paul, Adriaan, Jan,LEWI, Paulus, Joannes,HEERES, Jan,DE JONGE, Marc, René,KOYMANS, Lucien, Maria, Henricus,DAEYAERT, Frederik, Frans, Desire,KUKLA, Michael, Joseph,GEERTS, Hugo, Alfons, Gabriel,NUYDENS, Rony, Maria,MERCKEN, Marc, Hubert,LUDOVICI, Donald, William
- Current Assignee Address: Turnhoutseweg 30, B-2340 Beerse BE
- Agency: JANSSEN PHARMACEUTICA N.V.
- Priority: EP01204193.5 20011101
- Main IPC: C07D213/82
- IPC: C07D213/82
Abstract:
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-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=O)-; R 21 -S(=O) p -; R 7 -S(=O) p -; R 7 -S(=O) p -NH-; R 21 -S(=O) p -NH-; R 7 -C(=O)-; -NHC(=O)H;-C(=O)NHNH 2 ; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
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