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

公开(公告)号：EP2097402B1

公开(公告)日：2014-04-09

申请号：EP07822656.0

申请日：2007-11-16

申请人： Janssen R&D Ireland

发明人： RABOISSON, Pierre Jean-Marie Bernard ,  DE KOCK, Herman Augustinus ,  MC GOWAN, David Craig ,  VAN DE VREKEN, Wim ,  HU, Lili ,  TAHRI, Abdellah ,  VENDEVILLE, Sandrine Marie Helene

IPC分类号： C07D401/12 ,  C07D491/04 ,  A61K31/4709 ,  A61K31/4741 ,  A61P31/14

CPC分类号： C07D491/056 ,  A61K31/427 ,  A61K31/4741 ,  C07D401/12 ,  C07D491/04 ,  C07D491/048 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/393 ,  A61K2300/00

摘要： Inhibitors of HCV replication of formula (I) and the salts and 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 -OR7, -NH-SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or -NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

公开(公告)号：EP1913015B1

公开(公告)日：2013-12-11

申请号：EP06764266.0

申请日：2006-07-28

申请人： Janssen R&D Ireland

发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  VAN DE VREKEN, Wim ,  SURLERAUX, Dominique, Louis, Nestor, Ghislain ,  SIMMEN, Kenneth, Alan

IPC分类号： C07K5/078 ,  A61K38/05 ,  C07D403/04 ,  A61K31/41 ,  A61P31/14

CPC分类号： C07D487/04 ,  C07D403/04

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.