Invention Grant
- Patent Title: Macrocyclic inhibitors of hepatitis C virus
- Patent Title (中): 丙型肝炎病毒的大环抑制剂
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Application No.: US11632102Application Date: 2006-07-28
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Publication No.: US08148399B2Publication Date: 2012-04-03
- Inventor: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist
- Applicant: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist
- Applicant Address: IE Eastgate, County Cork SE Huddinge
- Assignee: Tibotec Pharmaceuticals Ltd.,Medivar AB
- Current Assignee: Tibotec Pharmaceuticals Ltd.,Medivar AB
- Current Assignee Address: IE Eastgate, County Cork SE Huddinge
- Agency: Woodcock Washburn LLP
- Priority: EP05107074 20050729; EP05107417 20050811; EP06101280 20060203
- International Application: PCT/EP2006/064820 WO 20060728
- International Announcement: WO2007/014926 WO 20070208
- Main IPC: C07D487/04
- IPC: C07D487/04 ; A61K31/33 ; A61P31/14

Abstract:
Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line 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, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms 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.
Public/Granted literature
- US20090281140A1 Macrocyclic inhibitors of hepatitis c virus Public/Granted day:2009-11-12
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