发明申请
- 专利标题: MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
- 专利标题(中): 丙型肝炎病毒大肠杆菌抑制剂
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申请号: US11995714申请日: 2006-07-28
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公开(公告)号: US20090281141A1公开(公告)日: 2009-11-12
- 发明人: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Lili Hu , Abdellah Tahri , Dominique Louis nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Hans Kristian Wallberg
- 申请人: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Lili Hu , Abdellah Tahri , Dominique Louis nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Hans Kristian Wallberg
- 优先权: EP05107069.6 20050729
- 国际申请: PCT/EP06/64815 WO 20060728
- 主分类号: A61K31/4709
- IPC分类号: A61K31/4709 ; C07D245/00 ; A61P31/12
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 —OR1, —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, polyhaloC1-6alkyl, 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
- US08012939B2 Macrocyclic inhibitors of hepatitis C virus 公开/授权日:2011-09-06
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