MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS

摘要

Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; Ris –OR, -NH-SOR; Ris hydrogen, and where X is C or CH, Rmay also be C-alkyl; Ris hydrogen, C-alkyl, C-alkoxy C-alkyl, or C-cycloalkyl; n is 3, 4, 5, or 6; Rand Rtaken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from formula (II) wherein said ring system may optionally be substituted with 1-3 substituents; Ris hydrogen; aryl; Het; C-cycloalkyl optionally substituted with C-alkyl; or C-alkyl optionally substituted with C-cycloalkyl, aryl or with Het; Ris aryl; Het; C-cycloalkyl optionally substituted with C-alkyl; or C-alkyl optionally substituted with C-cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being optionally substituted with 1-3 substituents pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.