Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines

Details Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines

C - Chemistry, Metallurgy

07

D

C07D 239/48 (2006.01) A61K 31/505 (2006.01) A61P 31/18 (2006.01) C07D 239/50 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/14 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2573976

HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a 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; C1- 6alkylcarbonyl; optionally subst ituted 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; polyhalo methylt hio; -S(=O)rR6; C(=NH)R6; R2a is CN; amino; substituted amino; optionally subst ituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; - C(=N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 is -NR1-, -O-, -C(=O)-, CH2 , -CHOH-, - S-, -S(=O)r-; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1- 6alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2- 6alkynyl; -C(=N-O-R8)-C1-4alkyl; R7; -X3-R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1- 6alkyloxy; CN; nitro; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is-Y-CqH2q-L or -CqH2q-Y-CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceut ical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

L'invention porte sur des inhibiteurs de réplication du VIH de formule (I), leurs >N</i>-oxydes, leurs sels d'addition pharmaceutiquement acceptables, des amines quaternaires ou leurs formes stéréoisomères, dans laquelle -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-; R1 représente hydrogène ; aryle ; formyle ; alkylcarbonyle C1-6; alkyle C1-6 éventuellement substitué ; alkyloxycarbonyle C1-6; R2 représente OH; halo; alkyle C1-6 éventuellement substitué, alcényle C2-6 ou alcynyle C2-6; carbonyle substitué; carboxyle; CN; nitro; amino; amino substitué; polyhalométhyle; polyhalométhylthio; -S(=O)rR6; C(=NH)R6; R2a représente CN; amino; amino substitué; alkyle C1-6 éventuellement substitué ; halo; alkyloxy C1-6 éventuellement substitué; carbonyle substitué; -CH=N-NH-C(=O)-R16; alkyloxy C1-6 éventuellement substitué ; alkyle C1-6; alcényle C2-6 ou alcynyle C2-6 substitués; -C(=N-O-R8)alkyle-C1-4; R7 ou -X3-R7; X1 est -NR1-, -O-, -C(=O)-, CH2, -CHOH-, -S-, -S(=O)r-; R3 représente CN; amino; alkyle C1-6; halo; alkyloxy C1-6 éventuellement substitué ; carbonyle substitué; -CH=N-NH-C(=O)-R16; alkyle C1-6 substitué ; alkyle C1-6 alkyloxy C1-6 éventuellement substitués; alcényle C2-6 ou alcynyle C2-6 substitués; alkyle-C(=N-O-R8)-C1-4; R7; -X3-R7; R4 représente halo; OH; alkyle C1-6 éventuellement substitué, alcényle C2-6 ou alcynyle C2-6; cycloalkyle C3-7; alkyloxy C1-6; CN; nitro; polyhalo alkyle C1-6; polyhalo alkyloxy C1-6; carbonyle substitué; formyle; amino; mono- ou di(C1-4alkyle)amino ou R7; R5 représente-Y-CqH2q-L ou -CqH2q-Y-CrH2r-L; L est aryle ou Het; procédés de préparation de ces composés, compositions pharmaceutiques renfermant ces composés comme ingrédients actifs et utilisation de ces composés pour la prévention ou le traitement de l'infection par VIH.

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