发明公开
- 专利标题: MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
- 专利标题(中): MAKROZYKLISCHE缝边DES肝炎C-VIRUS
-
申请号: EP06778068.4申请日: 2006-07-28
-
公开(公告)号: EP1919904A1公开(公告)日: 2008-05-14
- 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
- 申请人: Tibotec Pharmaceuticals Ltd. , MEDIVIR AB
- 申请人地址: Eastgate Village Eastgate Little Island Co Cork IE
- 专利权人: Tibotec Pharmaceuticals Ltd.,MEDIVIR AB
- 当前专利权人: Tibotec Pharmaceuticals Ltd.,MEDIVIR AB
- 当前专利权人地址: Eastgate Village Eastgate Little Island Co Cork IE
- 代理机构: Wante, Dirk Paul Maria
- 优先权: EP05107069 20050729
- 国际公布: WO2007014921 20070208
- 主分类号: C07D401/14
- IPC分类号: C07D401/14 ; C07K5/078 ; A61K31/4725 ; A61P31/14
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/授权文献
- EP1919904B1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 公开/授权日:2014-01-08
信息查询