Hiv inhibiting bicyclic pyrimidine derivatives

Details Hiv inhibiting bicyclic pyrimidine derivatives Hiv inhibiting bicyclic pyrimidine derivatives

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/52 (2006.01) A61P 31/18 (2006.01) C07D 473/00 (2006.01)

Patent

CA 2577588

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-; 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)-C1-4 alkyl; 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)-C1-4 alkyl; 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.

Inhibiteurs de réplication de VIH de formule (I) N-oxydes, sels d'addition acceptables sur le plan pharmaceutique, amines quaternaires ou formes stéréoisomères desdits inhibiteurs. Dans ladite formule, -a1=a2-a3=a4- représente -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; -b1=b2-b3=b4- représente -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; n et m valent 0, 1, 2, 3 et dans certains cas également 4; R1 représente hydrogène; aryle; formyle; C1-6alkylcarbonyle; C1-6alkyle éventuellement substitué; C1-6alkyloxycarbonyle; R2 représente OH; halo; C1-6alkyle, C2-6alcényle ou C2-6alcynyle éventuellement substitués; carbonyle substitué; carboxyle; CN; nitro; amino; amino substitué; polyhalométhyle; polyhalométhylthio; -S(=O)pR6; C(=NH)R6; R2a représente CN; amino; amino substitué; C1-6alkyle éventuellement substitué; halo; C1-6alkyloxy éventuellement substitué; carbonyle substitué; -CH=N-NH-C(=O)-R16; C1-6alkyloxyC1-6alkyle éventuellement substitué; C2-6alcényle ou C2-6alcynyle substitués; -C(=N-O-R8)-C1-4alkyle; R7 ou -X-R7; R3 représente CN; amino; C1-6alkyle; halo; C1-6alkyloxy éventuellement substitué; carbonyle substitué; -CH=N-NH-C(=O)-R16; C1-6alkyle substitué; C1-6alkyloxyC1-6alkyle éventuellement substitué; C2-6alcényle ou C2-6alcynyle substitués; -C(=N-O-R8)-C1-4 alkyle; R7; -X-R7; R4 représente halo; OH; C1-6alkyle, C2-6alcényle ou C2-6alcynyle éventuellement substitués; C3-7cycloalkyle; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyle; polyhaloC1-6alkyloxy; carbonyle substitué; formyle; amino; mono- ou di(C1-4alkyl)amino ou R7; -A-B- représente -CR5=N-, -N=N-, -CH2-CH2-, -CS-NH-, -CO-NH-, -CH=CH-. La présente invention concerne également des compositions pharmaceutiques contenant lesdits composés, des procédés de préparation de ces composés et compositions et l'utilisation de ces composés pour prévenir ou traiter l'infection due au VIH.

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