C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/48 (2006.01) A61K 31/505 (2006.01) A61K 31/506 (2006.01) A61P 31/18 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 405/04 (2006.01) C07D 405/12 (2006.01) C07D 409/04 (2006.01) C07D 409/12 (2006.01) C07D 417/06 (2006.01)
Patent
CA 2674185
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.
L'invention porte sur la formule d'un inhibiteur de la réplication du VIH dans laquelle:R1 est hydrogène; aryle; foumyle; C1_6alkylcarbonyle; C1_6alkyle; C1_6alkyloxycarbonyle; R2, R3, R7 et R8 sont hydrogène; hydroxy; halo; C3-7cycloalkyle; C1_6alkyloxy; carboxyle; C1_6alkyloxycarbonyle; cyano; nitro; amino; mono- ou di(C1_6alkyl)amino; polyhaloC1-6alkyle; polyhaloC1-6alkyloxy; -C(=O)R10; C1_6alkyle facultativement substitué par halo, cyano ou -C(=O)R10; facultativement substitué par C1_6alkyle, C2-6alcényle, ou C2-6alkynyle; R4 et R9 sont hydroxy; halo; C3_7Cycloalkyle; C1_6alkyloxy; carboxyle; C1_6alkyloxycarbonyle; formyle; cyano; nitro; amino; mono- ou di(C1_6alkyl)amino; polyhaloC1_6alkyle; 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; facultativement substitué C1_6alkyle, C2-6alcényle ou C2-6alkynyle; R5 est C2-6alcényle ou C2-6alkynyle tous deux substitués par cyano, aminocarbonyle, mono- et di(C1_6alkyl)aminocarbonyle, aryle, pyridyle, thiényle, furanyle, ou par un ou deux groupes C1_6alkylyoxy; Het; -C(=O)NR5aR5b; -CH(OU5c)R5d; X is -NR1-, -O-, -CH2-, ou -S-; L'invention porte aussi sur des préparations pharmaceutiques contenant ces composés dont ils sont le principe actif, et sur les procédés de préparation desdits composés et desdites compositions.
Guillemont Jerome Emile Georges
Mordant Celine Isabelle
Schmitt Benoit Antoine
Gowling Lafleur Henderson Llp
Tibotec Pharmaceuticals Ltd.
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