公开(公告)号：EP2483288B1

公开(公告)日：2016-11-16

申请号：EP10765608.4

申请日：2010-09-29

申请人： Janssen Products, L.P. ,  Medivir AB

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

IPC分类号： C07H19/10 ,  A61K31/7072 ,  A61P31/14

CPC分类号： C07H19/10

公开(公告)号：EP2483288A2

公开(公告)日：2012-08-08

申请号：EP10765608.4

申请日：2010-09-29

申请人： Janssen Products, L.P. ,  Medivir AB

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

IPC分类号： C07H19/10 ,  A61K31/7072 ,  A61P31/14

CPC分类号： C07H19/10

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.

公开(公告)号：EP2084175A1

公开(公告)日：2009-08-05

申请号：EP07820934.3

申请日：2007-10-04

申请人： Medivir AB

发明人： JOHANSSON, Nils-Gunnar ,  KALAYANOV, Genadiy ,  MARTIN, Joseph Armstrong ,  SMITH, David Bernard ,  WINQVIST, Anna

IPC分类号： C07H19/073 ,  A61K31/513 ,  A61P31/12

CPC分类号： C07H19/073 ,  A61K31/513 ,  A61K38/191 ,  A61K38/193 ,  A61K38/20 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

摘要： 4-Amino-1-((2R,3S,4S,5R)-5-azido-4hydroxy-5-hydroxymethyl-3-methyl-tetrahyclrofuran-2- yl)-1 H-pyrimidin-2-one(22) are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.

公开(公告)号：EP2084175B1

公开(公告)日：2010-12-29

申请号：EP07820934.3

申请日：2007-10-04

申请人： Medivir AB

发明人： JOHANSSON, Nils-Gunnar ,  KALAYANOV, Genadiy ,  MARTIN, Joseph Armstrong ,  SMITH, David Bernard ,  WINQVIST, Anna

IPC分类号： C07H19/073 ,  A61K31/513 ,  A61P31/12

CPC分类号： C07H19/073 ,  A61K31/513 ,  A61K38/191 ,  A61K38/193 ,  A61K38/20 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

摘要： 4-Amino-1-((2R,3S,4S,5R)-5-azido-4hydroxy-5-hydroxymethyl-3-methyl-tetrahyclrofuran-2- yl)-1 H-pyrimidin-2-one(22) are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.