| abstract |
HEPATITIS C VIRUS MACROCYCLIC INHIBITORS, USE OF THE SAME, PROCESS FOR THE PREPARATION OF THE SAME, COMBINATION AND PHARMACEUTICAL COMPOSITION. The present invention relates to HGV replication inhibitors of formula (I) and the N-oxides, salts and stereoisomers thereof, wherein X is N, CH and where X carries a double bond it is C; R 4 is R-5, -NH-So-2-R 6; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 13 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, or C 3-7 cycloalkyl; R 4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halo, C 1-6 polyalkyl, polyalkylC 1-6 alkoxy, amino, moono- or diC 1-6 alkylamino, mono- or diC 1-6 alkylaminocarbonyl, C 1-6 alkylcarbonylamino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by - - - - -) represents an optional double bond; R5 is hydrogen; arila; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; R6 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each Het is a 5- or 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, and optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of HCV inhibitors of formula (I) with ritonavir are also provided. |