HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES

摘要

HIV replication inhibitors of formula (I), N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a¹=a²-a³=a⁴- is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; -b¹=b²-b³=b⁴- is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R¹ is hydrogen; aryl; formyl; C_1-6alkylcarbonyl; optionally substituted C_1-6alkyl; C_1-6alkyloxycarbonyl; R² is OH; halo; optionally substituted C_1-6alkyl, C_2-6alkenyl or C_2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; -S(=O)_PR⁶; C(=NH)R⁶; R^2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C_1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R¹⁶; optionally substituted C_1-6alkyloxyC_1-6alkyl; substituted C_2-6alkenyl or C _2-6 alkynyl; -C(=N-O-R⁸)-C_1-4alkyl; R⁷ or -X₃-R⁷; X₁ is -NR¹-, -O-, -C(=O)-, -CH₂-, -CHOH-, -S-, -S(=O)_P- R³ is CN; amino; C_1-6alkyl; halo; optionally substituted C_1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R¹⁶; substituted C_1-6alkyl; optionally substituted C_1-6alkyloxyC_1-6alkyl; substituted C_2-6alkenyl or C_2-6alkynyl; -C(=N-O-R⁸)-C_1-4alkyl; R⁷; -X₃-R⁷ ; R⁴ is halo; OH; optionally substituted C_1-6alkyl, C_2-6alkenyl or C_2-6alkynyl; C_3-7cycloalkyl; C_1-6alkyloxy; CN; nitro; polyhaloC_1-6alkyl; polyhaloC_1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C_1-4alkyl)amino or R⁷; R⁵ is a 5- or 6-membered completely unsaturated ring system wherein 1 - 4 ring members are nitrogen, oxygen or sulfur; which ring may optionally be substituted and may optionally be annelated with a benzene ring; methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of these compounds for the prevention or the treatment of HIV infection.