HIV inhibiting bicyclic pyrimdine derivatives

HIV replication inhibitors of formula 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...

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Hauptverfasser: LEWI PAULUS JOANNES, DELEST BRUNO FRANCOIS MARIE, HEERES JAN, JANSSEN PAUL ADRIAAN JAN, GUILLEMONT JEROME EMILE GEORGES, ARTS, LEGAL REPRESENTATIVE FRANK XAVIER JOZEF HERWIG, PAUGAM MIKAEL
Format: Patent
Sprache:eng
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Zusammenfassung:HIV replication inhibitors of formula 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-; n and m is 0, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; -S( O)pR6; C( NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH N-NH-C( O)-R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7 or -X-R7; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH N-NH-C( O)-R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7; -X-R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B- is -CR5 N-, -N N-, -CH2-CH2-, -CS-NH-, -CO-NH-, -CH CH-; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.