AMID DERIVATIVES AS INHIBITORS OF GLYCOGEN SYNTHASE KINASE-3-BETA

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; RSUP1 /SUPis hydrogen; aryl; formyl; CSUB1-6/SUBalkylcarbonyl; optionally substituted CSUB1-6/SUBalkyl; CSUB1-6/SUBalkyloxycarbonyl; optionally substituted CSUB1-6/SUBalkyloxyCSUB1-6/SUBalkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; RSUP2 /SUPis hydrogen, CSUB1-10/SUBalkyl, CSUB2-10/SUBalkenyl, CSUB2-10/SUBalkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; RSUP3 /SUPis hydrogen; hydroxy; halo; optionally substituted CSUB1-6/SUBalkyl or CSUB2-6/SUBalkenyl or CSUB2-6/SUBalkynyl; CSUB1-6/SUBalkyloxy; CSUB1-6/SUBalkylthio; CSUB1-6/SUBalkyloxycarbonyl; CSUB1-6/SUBalkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(CSUB1-6/SUBalkyl)amino; polyhaloCSUB1-6/SUBalkyl; polyhaloCSUB1-6/SUBalkyloxy; polyhaloCSUB1-6/SUBalkylthio; RSUP21/SUP; RSUP21/SUP-CSUB1-6/SUBalkyl; RSUP21/SUP-O-; RSUP21/SUP-S-; RSUP21/SUP-C(-O)-; RSUP21/SUP-S(-O)SUBp/SUB-; RSUP7/SUP-S(-O)SUBp/SUB-; RSUP7/SUP-S(-O)SUBp/SUB-NH-; RSUP21/SUP-S(-O)SUBp/SUB-NH-; RSUP7/SUP-C(-O)-; -NHC(-O)H; -C(-O)NHNHSUB2/SUB; RSUP7/SUP-C(-O)-NH-; RSUP21/SUP-C(-O)-NH-; -C(-NH)RSUP7/SUP; -C(-NH)RSUP21/SUP; RSUP4a /SUPor RSUP4b /SUPeach independently represent hydrogen, RSUP8/SUP, -YSUB1/SUB-NRSUP9/SUP-YSUB2/SUB-NRSUP10/SUPRSUP11/SUP, -YSUB1/SUB-NRSUP9/SUP-YSUB1/SUB-RSUP8/SUP, -YSUB1/SUB-NRSUP9/SUPRSUP10/SUP; provided that -X-RSUP2 /SUPand/or RSUP3 /SUPis other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.