发明授权
- 专利标题: MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
- 专利标题(中): 丙型肝炎病毒大环抑制剂
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申请号: EP06764265.2申请日: 2006-07-28
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公开(公告)号: EP1912996B1公开(公告)日: 2012-06-20
- 发明人: DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , TAHRI, Abdellah , SIMMEN, Kenneth, Alan , NILSSON, Karl, Magnus, , SAMUELSSON, Bengt, Bertil, , ROSENQUIST, Åsa, Annica, Kristina, , ANTONOV, Dmitry,
- 申请人: Janssen R&D Ireland , Medivir Aktiebolag
- 申请人地址: Eastgate Village Eastgate, Little Island, County Cork IE
- 专利权人: Janssen R&D Ireland,Medivir Aktiebolag
- 当前专利权人: Janssen R&D Ireland,Medivir Aktiebolag
- 当前专利权人地址: Eastgate Village Eastgate, Little Island, County Cork IE
- 代理机构: Daelemans, Frank F.R.
- 优先权: EP05107068 20050729; EP05107414 20050811
- 国际公布: WO2007014920 20070208
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; C07K5/078 ; A61K38/05 ; A61K31/33 ; A61P31/14 ; C07D413/12
摘要:
Inhibitors of HCV replication of formula (I), the N-oxides, salts, and stereochemically isomeric forms 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 aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, -O-. -O-C1-4alkanediyl-, -O-C(=O)-, -O-C(=O)-NR4a- or -O-C(=O)-NR4aC1-4alkanediyl-; R2 is hydrogen, -OR5, -C(O)OR5, -C(=O)R6, -C(=O)NR4aR4b, -C(=O)NHR4c,-NR4aR4b, -NHR4c, -NR4aSOpNR4aR4b, -NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl; n is 3, 4, 5, or 6; p is 1 or 2; aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be 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 each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be 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
- EP1912996A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 公开/授权日:2008-04-23
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