Amide derivatives as glycogen synthase kinase 3-beta inhibitors

   
   

This invention concerns a compound of formula 1 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.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; optionally substituted C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; optionally substituted C.sub.1-6alkyloxyC.sub.- 1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R.sup.2 is hydrogen, C.sub.1-10alkyl, C.sub.2-10alkenyl, C.sub.2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R.sup.3 is hydrogen; hydroxy; halo; optionally substituted C.sub.1-6alkyl or C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.1-6alkyloxy; C.sub.1-6alkylthio; C.sub.1-6alkyloxycarbonyl; C.sub.1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C.sub.1-6alkyl)amino; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkylox- y; polyhaloC.sub.1-6alkylthio; R.sup.21; R.sup.21-C.sub.1-6alkyl; R.sup.21--O--; R.sup.21--S--; R.sup.21--C(.dbd.O)--; R.sup.21--S(.dbd.O).sub.p--; R.sup.7--S(.dbd.O).sub.p--; R.sup.7--S(.dbd.O).sub.p--NH--; R.sup.21--S(.dbd.O).sub.p--NH--; R.sup.7--C(.dbd.O)--; --NHC(.dbd.O)H; --C(.dbd.O)NHNH.sub.2; R.sup.7--C(.dbd.O)--NH--; R.sup.21--C(.dbd.O)--NH--; --C(.dbd.NH)R.sup.7; --C(.dbd.NH)R.sup.21; R.sup.4a or R.sup.4b each independently represent hydrogen, R.sup.8, --Y.sub.1--NR.sup.9--Y.sub.2--NR.sup.10R.sup.11, --Y.sub.1--NR.sup.9--Y.sub.1--R.sup.8, --Y.sub.1--NR.sup.9R.sup.10; provided that --X--R.sup.2 and/or R.sup.3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

 
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