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