Macrocyclic inhibitors of hepatitis C virus

Details Macrocyclic inhibitors of hepatitis C virus Macrocyclic inhibitors of hepatitis C virus

2006-07-28

2010-02-23

Tsang, Cecilia (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

Reexamination Certificate

active

07666834

ABSTRACT:
Inhibitors of HCV replication of formula (I)and the N-oxides, salts, or stereoisomers thereof, whereineach dashed line (represented by - - - - -) represents an optional double bond;X is N, CH and where X bears a double bond it is C;R1is —OR6, —NH—SO2R7;R2is hydrogen, and where X is C or CH, R2may also be C1-6alkyl;R3is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl;n is 3, 4, 5, or 6;R4and R5independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het;W is aryl or Het;R6is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;R7is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents;Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and 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.

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