公开(公告)号：EP1919904A1

公开(公告)日：2008-05-14

申请号：EP06778068.4

申请日：2006-07-28

申请人： Tibotec Pharmaceuticals Ltd. ,  MEDIVIR AB

发明人： RABOISSON, Pierre Jean-Marie Bernard ,  DE KOCK, Herman Augustinus ,  DORANGE, Ismet ,  VENDEVILLE, Sandrine Marie Helene ,  SURLERAUX, Dominique Louis Nestor Ghislain ,  TAHRI, Abdellah ,  SIMONNET, Yvan ,  VAN DE VREKEN, Wim ,  HU, Lili ,  SIMMEN, Kenneth Alan ,  NILSSON, Karl Magnus ,  SAMUELSSON, Bengt Bertil ,  ROSENQUIST, Åsa Annica Kristina ,  WALLBERG, Hans Kristian

IPC分类号： C07D401/14 ,  C07K5/078 ,  A61K31/4725 ,  A61P31/14

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D487/04 ,  C07K5/06191

摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R1 is -OR5, -NH-SO2R6; 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; R4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhalo- C1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or DiC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by ) represents an optional double bond; R5 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R6 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with 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 completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three 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.

公开(公告)号：EP1919904B1

公开(公告)日：2014-01-08

申请号：EP06778068.4

申请日：2006-07-28

申请人： Janssen R&D Ireland ,  MEDIVIR AB

发明人： RABOISSON, Pierre Jean-Marie Bernard ,  DE KOCK, Herman Augustinus ,  DORANGE, Ismet ,  VENDEVILLE, Sandrine Marie Helene ,  SURLERAUX, Dominique Louis Nestor Ghislain ,  TAHRI, Abdellah ,  SIMONNET, Yvan ,  VAN DE VREKEN, Wim ,  HU, Lili ,  SIMMEN, Kenneth Alan ,  NILSSON, Karl Magnus ,  SAMUELSSON, Bengt Bertil ,  ROSENQUIST, Åsa Annica Kristina ,  WALLBERG, Hans Kristian

IPC分类号： C07D401/14 ,  C07K5/078 ,  A61K31/4725 ,  A61P31/14

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D487/04 ,  C07K5/06191