| abstract |
This invention relates to HIV (I) proliferation inhibitors, N-oxides, pharmaceutically acceptable addition salts, quaternary amines and their stereochemically isomeric forms, wherein the ring containing -a1 = a2-a3 = a4- and - b1 = b2-b3 = b4- represents phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; 6 alkyl; C 1-6 alkyloxycarbonyl, substituted C 1-6 alkyl, C 1-6 alkylcarbonyl; R 2 is hydroxy, halo, optionally substituted C 1-6 alkyl, C 3-7 cyclo alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-, di- (C 1-6 alkyl), poly (ethyl), poly (ethyl), di (C 1-6 alkyl); = O) pR6, -NH-S (= O) pR6, -C (= O) R6, -NHC (= O) H, -C (= O) NHNH2, -NHC (= O) R6, -C ( = NH) R6 or a 5-membered heterocycle; X1 is -NR5-, -NH-NH-, -N = N-, -O-, -C (= O) -, C1-4 alkanediyl, -CHOH-, -S-, -S (= O) p-, -X2-C1-4 alkanodiyl- or -C1-4 alkanodiyl-X2-; R3 is NHR13; NR13R14; -C (= O) -NHR13 · -C (= O ) -NR 13 R 14 · -C (= O) -R 15 · -CH = N-NHC (= O) -R 16; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenes · Substituted C2-6alkynyl · C1-6alkyl substituted with hydroxy and a second substituent; -C (= NO-R8) -C1-4alkyl · R7; or -X3-R7; R4 is halo, hydroxy, C1-6alkyl, C3 -7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, cycloalkylamino (di), formyl or amyl, amyl (cycloalkyl), amyl, cycloalkyl) processes for their preparation and pharmaceutical compositions comprising them. |