发明公开
- 专利标题: PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDES
- 专利标题(中): 磷酰胺核苷衍生物
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申请号: EP10765608.4申请日: 2010-09-29
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公开(公告)号: EP2483288A2公开(公告)日: 2012-08-08
- 发明人: JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen , PELCMAN, Michael , SUND, Bengt Christian , WÄHLING, Horst Jürgen , PASSOS PINHO, Pedro Manuel , WINQVIST, Anna , NILSSON, Karl Magnus
- 申请人: Janssen Products, L.P. , Medivir AB
- 申请人地址: 800/850 Ridgeway Drive Horsham PA 19044 US
- 专利权人: Janssen Products, L.P.,Medivir AB
- 当前专利权人: Janssen Products, L.P.,Medivir AB
- 当前专利权人地址: 800/850 Ridgeway Drive Horsham PA 19044 US
- 代理机构: van Wanrooij, Eva
- 优先权: EP09171607 20090929
- 国际公布: WO2011039221 20110407
- 主分类号: C07H19/10
- IPC分类号: C07H19/10 ; A61K31/7072 ; A61P31/14
摘要:
Compounds of formula I : including any possible stereoisomers thereof, wherein: R
1 is hydrogen, -C(=O)R
6 or -C(=O)CHR
7 -NH
2 ; R
2 is hydrogen; or C
1 -C
6 alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C
1 -C
6 alkyl, C
2 -C
6 -alkenyl and C
1 -C
6 alkoxy, hydroxy or amino, or R
2 is naphtyl; or R
2 is indolyl, R
3 is hydrogen, Ci-C6alkyl, benzyl; R
4 is hydrogen, Ci-C6alkyl, benzyl; or R
3 and R
4 together with the carbon atom to which they are attached form C
3 -C
7 Cyclo- alkyl; R
5 is C
1 -C
10 alkyl, C
3 -C
7 -cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C
1 -C
6 alkoxy, amino, mono- and diC
1 -C
6 alkylamino; R
6 is C
1 -C
6 alkyl; R
7 is C
1 -C
6 alkyl; R
8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.
1 is hydrogen, -C(=O)R
6 or -C(=O)CHR
7 -NH
2 ; R
2 is hydrogen; or C
1 -C
6 alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C
1 -C
6 alkyl, C
2 -C
6 -alkenyl and C
1 -C
6 alkoxy, hydroxy or amino, or R
2 is naphtyl; or R
2 is indolyl, R
3 is hydrogen, Ci-C6alkyl, benzyl; R
4 is hydrogen, Ci-C6alkyl, benzyl; or R
3 and R
4 together with the carbon atom to which they are attached form C
3 -C
7 Cyclo- alkyl; R
5 is C
1 -C
10 alkyl, C
3 -C
7 -cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C
1 -C
6 alkoxy, amino, mono- and diC
1 -C
6 alkylamino; R
6 is C
1 -C
6 alkyl; R
7 is C
1 -C
6 alkyl; R
8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.
公开/授权文献
- EP2483288B1 PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDES 公开/授权日:2016-11-16
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