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：EP1912981B1

公开(公告)日：2010-01-20

申请号：EP06764268.6

申请日：2006-07-28

申请人： Tibotec Pharmaceuticals ,  MEDIVIR AB

发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  HU, Lili ,  SIMMEN, Kenneth, Alan ,  LINDQUIST, Karin Charlotta ,  LINDSTRÖM, Mats Stefan ,  BELFRAGE, Anna Karin Gertrud Linnea ,  WÄHLING, Horst Jürgen ,  NILSSON, Karl Magnus ,  SAMUELSSON, Bengt Bertil ,  ROSENQUIST, Åsa Annica Kristina ,  SAHLBERG, Sven Crister ,  WALLBERG, Hans, Kristian ,  KAHNBERG, Pia, Cecilia ,  CLASSON, Björn, Olof

IPC分类号： C07D417/04

CPC分类号： C07D487/10 ,  C07D245/04

摘要： Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(=O)PR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl- carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.

公开(公告)号：EP1912981A2

公开(公告)日：2008-04-23

申请号：EP06764268.6

申请日：2006-07-28

申请人： Tibotec Pharmaceuticals Ltd. ,  MEDIVIR AB

发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  HU, Lili ,  SIMMEN, Kenneth, Alan ,  LINDQUIST, Karin Charlotta ,  LINDSTRÖM, Mats Stefan ,  BELFRAGE, Anna Karin Gertrud Linnea ,  WÄHLING, Horst Jürgen ,  NILSSON, Karl Magnus ,  SAMUELSSON, Bengt Bertil ,  ROSENQUIST, Åsa Annica Kristina ,  SAHLBERG, Sven Crister ,  WALLBERG, Hans, Kristian ,  KAHNBERG, Pia, Cecilia ,  CLASSON, Björn, Olof

IPC分类号： C07D417/04

CPC分类号： C07D487/10 ,  C07D245/04

摘要： Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(=O)PR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl- carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.

摘要翻译： 式（I）化合物及其N-氧化物，盐和立体异构体，其中A是OR1，NHS（= O）PR2; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3亚烷基碳环基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3亚烷基碳环基，C 0 -C 3亚烷基杂环基; p独立地为1或2; n是3,4,5或6; ----定义一个可选的双键; L是N或CRz; Rz是H或与星号碳形成双键; Rq是H或当L是CRz时，Rq也可以是C1-C6烷基; 任选被一个或两个或三个各自独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，卤素，卤代C 1 -C 6烷基，氨基，单或二烷基氨基，单或二烷基氨基羰基，C 1 -C 6烷基 - 羰基氨基 C 0 -C 3亚烷基碳环基和C 0 -C 3亚烷基杂环基; R5是氢，C1-C6烷基，C1-C6烷氧基C1-C6烷基或C3-C7环烷基; R 6为氢，C 1 -C 6烷基，C 1 -C 6烷氧基，C 0 -C 3亚烷基碳环基，C 0 -C 3亚烷基杂环基，羟基，溴，氯或氟可用于治疗或预防诸如HCV的黄病毒感染。