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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
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。
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公开(公告)号:EP2509950B1
公开(公告)日:2015-02-25
申请号:EP10790938.4
申请日:2010-12-10
申请人: Janssen R&D Ireland , Medivir AB
发明人: KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
IPC分类号: C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04 , A61K31/506 , A61P31/18
CPC分类号: C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04
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公开(公告)号:EP2509950A1
公开(公告)日:2012-10-17
申请号:EP10790938.4
申请日:2010-12-10
申请人: Janssen R&D Ireland , Medivir AB
发明人: KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
IPC分类号: C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04 , A61K31/506 , A61P31/18
CPC分类号: C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04
摘要: HIV inhibitors of formula (I) wherein R
1 is halo, C
1-4 alkoxy, trifluoromethoxy; R
2 is a group of formula (A); R
3 is a group of formula (B); R
4 is a group of formula (C); n is 0 or 1; A is CH or N; R
5 and R
6 are hydrogen, C
1-4 alkyl, halo; R
7 and R
8 are C
1-4 alkyl or C
1-4 alkoxyC
1-4 alkyl; R
9 is C
1-4 alkyl, cyclopropyl, trifluoromethyl, C
1-4 alkoxy, or dimethylamino; R
10 is hydrogen, C
1-4 alkyl, cyclopropyl, trifluoromethyl, C
1-4 alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.摘要翻译: 式(I)的HIV抑制剂,其中R 1是卤素,C 1-4烷氧基,三氟甲氧基; R 2是式(A)的基团; R 3是式(B)的基团; R 4是式(C)的基团; n是0或1; A是CH或N; R 5和R 6是氢,C 1-4烷基,卤素; R 7和R 8是C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 9是C 1-4烷基,环丙基,三氟甲基,C 1-4烷氧基或二甲氨基; R 10为氢,C 1-4烷基,环丙基,三氟甲基,C 1-4烷氧基或二甲基氨基; 药学上可接受的加成盐和溶剂合物; 含有这些化合物作为活性成分的药物组合物和制备所述化合物的方法。
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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
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.
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