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Title:
C型肝炎ウイルスの大環状阻害剤
Document Type and Number:
Japanese Patent JP5230414
Kind Code:
B2
Abstract:
Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently 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; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is 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.

Inventors:
La Boisson, Pierre Jean-Marie Bernard
De Kok, Hermann Augustine
Simene, Kenneth Alan
Karl Erik Daniel, Youngson
Karl Magnus, Nilsson
Rosenquist, Asa Anika Christina
Samuel Elson, Bengt Vertail
Antonov, Dmitri
Salvador Oden, Ruhldeath
Aeza Albarez, Suzana
Klason, Bjorn Olov
Application Number:
JP2008523378A
Publication Date:
July 10, 2013
Filing Date:
July 28, 2006
Export Citation:
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Assignee:
Tibotec Pharmaceuticals
International Classes:
C07D245/04; A61K31/395; A61K31/407; A61K31/4155; A61K31/422; A61K31/427; A61K31/4523; A61P31/12; A61P31/14; A61P43/00; C07D401/12; C07D403/12; C07D413/12; C07D417/12; C07D487/04
Foreign References:
WO2005010029A1
WO2005028501A1
WO2004094452A1
WO2004037855A1
WO2003053349A1
WO2000059929A1
WO2005073216A1
WO2005073195A1
WO2007017144A1
WO2007014921A1
WO2007014920A1
WO2007014926A1
Attorney, Agent or Firm:
Patent business corporation Odashima patent office