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    HCV INHIBITIING SULFONAMIDES
    1.
    发明公开
    HCV INHIBITIING SULFONAMIDES 有权
    HCV耐磺胺

    公开(公告)号：EP1670448A1

    公开(公告)日：2006-06-21

    申请号：EP04766871.0

    申请日：2004-09-30

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： SIMMEN, Kenneth Alan ,  VAN ACKER, Koenraad Lodewijk August ,  WIGERINCK, Piet Tom Bert Paul ,  SURLERAUX, Dominique Louis Nestor Ghislain ,  DAMS, Géry Karel Julia ,  QUIRYNEN, Ludo Maria Marcel ,  HERTOGS, Kurt ,  PAUWELS, Rudi Wilfried Jan

    IPC分类号： A61K31/18 ,  A61K31/426 ,  A61K31/421 ,  A61P31/14

    CPC分类号： A61K45/06 ,  A61K31/18 ,  A61K31/421 ,  A61K31/426 ,  A61K2300/00

    摘要： The present invention concerns sulfonamide derivatives having the general formula (I) and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is -S- or -O-; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono-or di(C1-4 alkyl)amino; R2 is hydrogen or C1-6 alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4 alkyl, or arylC1-4 alkyl; R4 is hydrogen, C1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het1, Het2, C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4 alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(=O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4 alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het1, Het2 Het1C1-4alkyl and Het2C1-4 alkyl; Q2 is a radical of formulae (III, IV, V, VI, VII) for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.

    HCV INHIBITING SULFONAMIDES
    5.
    发明授权
    HCV INHIBITING SULFONAMIDES 有权
    HCV-HEMMENDE磺酰胺

    公开(公告)号：EP1670448B1

    公开(公告)日：2007-11-21

    申请号：EP04766871.0

    申请日：2004-09-30

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： SIMMEN, Kenneth Alan ,  VAN ACKER, Koenraad Lodewijk August ,  WIGERINCK, Piet Tom Bert Paul ,  SURLERAUX, Dominique Louis Nestor Ghislain ,  DAMS, Géry Karel Julia ,  QUIRYNEN, Ludo Maria Marcel ,  HERTOGS, Kurt ,  PAUWELS, Rudi Wilfried Jan

    IPC分类号： A61K31/18 ,  A61K31/426 ,  A61K31/421 ,  A61P31/14

    CPC分类号： A61K45/06 ,  A61K31/18 ,  A61K31/421 ,  A61K31/426 ,  A61K2300/00

    摘要： The present invention concerns sulfonamide derivatives having the general formula (I) and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is -S- or -O-; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono-or di(C1-4 alkyl)amino; R2 is hydrogen or C1-6 alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4 alkyl, or arylC1-4 alkyl; R4 is hydrogen, C1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het , Het , C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4 alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(=O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4 alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het , Het Het C1-4alkyl and Het C1-4 alkyl; Q2 is a radical of formulae (III, IV, V, VI, VII) for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.