HIV INHIBITING 5,6-SUBSTITUTED PYRIMIDINES.

摘要

R1 is hydrogen; aryl; formyl; C1_6alkylcarbonyl; C1_6alkyl; C1_6alkyloxycarbonyl; R2, R3, R7 and R8 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1_6alkyloxy; carboxyl; C1_6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1_6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; -C(=O)R10; C1_6alkyl optionally substituted with halo, cyano or -C(=O)R10; optionally substituted C1_6alkyl, C2-6alkenyl, or C2-6alkynyl; R4 and R9 are hydroxy; halo; C3_7Cycloalkyl; C1_6alkyloxy; carboxyl; C1_6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1_6alkyl)amino; polyhaloC1_6alkyl; polyhaloC1_6alkyloxy; -C(=O)R10; cyano; -S(=O)rR10; -NH-S(=O)2R10; -NHC(=O)H; -C(=O)NHNH2; -NHC(=O)R10; Het; -Y-Het; optionally substituted C1_6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is C2-6alkenyl or C2-6alkynyl both substituted with cyano, aminocarbonyl, mono- and di(C1_6alkyl)aminocarbonyl, aryl, pyridyl, thienyl, furanyl, or with one or two C1_6alkyloxy groups; Het; -C(=O)NR5aR5b; -CH(OR5c)R5d; X is -NR1-, -O-, -CH2-, or -S-; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.