abstract |
This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a<SUP>1</SUP>=a<SUP>2</SUP>-a<SUP>3</SUP>=a<SUP>4</SUP>-and -b<SUP>1</SUP>=b<SUP>2</SUP>-b<SUP>3</SUP>=b<SUP>4</SUP>represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R<SUP>1 </SUP>is hydrogen; aryl; formyl; C<SUB>1-6</SUB>alkylcarbonyl; C<SUP>1-6</SUP>alkyl; C<SUB>1-6</SUB>alkyloxycarbonyl, substituted C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkylcarbonyl; R<SUP>2 </SUP>is hydroxy, halo, optionally substituted C<SUB>1-6</SUB>alkyl, C<SUB>3-7</SUB>cycloalkyl, optionally substituted C<SUB>2-6</SUB>alkenyl, optionally substituted C<SUB>2-6</SUB>alkynyl, C<SUB>1-6</SUB>alkyloxy, C<SUB>1-6</SUB>alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C<SUB>1-6</SUB>alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(-O)<SUB>p</SUB>R<SUP>6</SUP>, -NH-S(-O)<SUB>p</SUB>R<SUP>6</SUP>, -C(-O)R<SUP>6</SUP>, -NHC(-O)H, -C(-O)NHNH?2?, -NHC(-O)R<SUP>6</SUP>, -C(-NH)R<SUP>6 </SUP>or a 5-membered hetrocycl; X<SUB>1 </SUB>is -NR<SUP>5</SUP>-, -NH-NH-, -N-N-, -O-, -C(-O)-, C<SUB>1-4</SUB>alkanediyl, -CHOH-, -S-, -S(-O)<SUB>p</SUB>-, -X<SUB>2</SUB>-C<SUB>1-4</SUB>alkanediyl- or -C<SUB>1-4</SUB>alkanediyl-X<SUB>2</SUB>-; R<SUP>3 </SUP>is NHR<SUP>13</SUP>, NR<SUP>13</SUP>R<SUP>14</SUP>; -C(-O)-NHR<SUP>13</SUP>; -C(-O)-NR<SUP>13</SUP>R<SUP>14</SUP>; -C(-O)-R<SUP>15</SUP>; -CH-N-NH-C(-O)-R<SUP>16</SUP>; substituted C<SUB>1-6</SUB>alkyl; optionally substituted C<SUB>1-6</SUB>alkyloxyC<SUB>1-6</SUB>alkyl; substituted C<SUB>2-6</SUB>alkenyl; substituted C<SUB>2-6</SUB>alkynyl; substituted C<SUB>2-6</SUB>alkylenyl; C<SUB>1-6</SUB>alkyl substituted with hydroxy and a second substituent; -C(-N-O-R<SUP>8</SUP>)-C<SUB>1-4</SUB>alkyl; R<SUP>7</SUP>; or -X<SUB>3</SUB>-R<SUP>7</SUP>; R<SUP>4 </SUP>is halo, hydroxy, C<SUB>1-6</SUB>alkyl, C<SUB>3-7</SUB>cycloalkyl, C<SUB>1-6</SUB>alkyloxy, cyano, nitro, polyhaloC<SUB>1-6</SUB>alkyl, polyhaloC<SUB>1-6</SUB>alkyloxy, aminocarbonyl, C<SUB>1-6</SUB>alkyloxycarbonyl, C<SUB>1-6</SUB>alkylcarbonyl, formyl, amino, mono- or di(C<SUB>1-4</SUB>alkyl) amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them |