| abstract |
This invention relates to HIV replication inhibitors of formula C1-6 an N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein R4 is halo, OH, C1-6 alkyl, C3-7 cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6 alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di (C1-4alkyl) amino or R7; R7 is a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic carbocycle or a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic heterocycle, wherein each of the carbocyclic or heterocyclic ring substituents may be, or five substituents each independently selected from halo, hydroxy, mercapto, C 1-6 alkyl, C 1-6 alkyl, amino C 1-6 alkyl, mono or di (C 1-6 alkyl), aminoC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 3-7 cycloalkyl, C 1 -6alkyloxy, C1-6alkyloxycarbonyl, C1-6alkylthio, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, -CH (= NO-R8), R7a, -X3-R7a or R7a-C1-4alkyl; R7a is a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic carbocycle or a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic heterocycle, wherein each of the carbocyclic or heterocyclic substituted optionally may be one, or five substituents each independently selected from halo, OH, mercapto, C 1-6 alkyl, C 1-6 alkyl, amino C 1-6 alkyl, mono or di C 1-6 alkyl) aminoC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 3-7 cycloalkyl, C 1-6 alkyloxy , C1-6alkyloxycarbonyl, C1-6alkylthio, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, -CH (= NO-R8); R8 is hydrogen, C1-4alkyl, aryl or arylC1-4alkyl; and X 1 is -NR 5 -, -NH-NH-, -N = N-, -O-, -C (= O) -, C 1-4 alkanediyl, -CHOH-, -S-, -S (= O) p -, -X2-C1-4alkanediyl- or -C1-4alkanediyl-X2-; X 2 is -NR 5 -, -NH-NH-, -N = N-, -O-, -C (= O) -, -CHOH-, -S-, -S (= O) p-; R5 is hydrogen; aryl; formyl; C1-6alkylkarbonyl; C1-6alkyl; C1-6alkyloksykarbonyl; C1-6 alkyl substituted by formyl, C1-6 alkylcarbonyl, C1-6alkyloxycarbonyl or C1-6alkylcarbonyloxy; C1-C1-6 alkylcarbonyl substituted with C1-6alkyloxycarbonyl; p = 1 or 2; provided that 3- (3,4,5-trimethoxyphenyl) -2-propenitrile is not included. |