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公开(公告)号：US09006209B2
公开(公告)日：2015-04-14
申请号：US13884835
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
摘要翻译： 本发明涉及抑制丙型肝炎病毒（HCV）的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。
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公开(公告)号：US20120135953A1
公开(公告)日：2012-05-31
申请号：US13389277
申请日：2010-08-06
申请人： David Mc Gowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
发明人： David Mc Gowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
IPC分类号： A61K31/4184 , C07D401/14 , A61K31/4439 , A61K31/454 , A61K31/7068 , A61K31/5377 , A61K31/4709 , A61K31/443 , A61K31/55 , A61P31/14 , C07D403/14 , C07D413/14
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14
摘要： Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R′ have the meaning as defined herein.The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
摘要翻译： 式I的HCV复制抑制剂包括立体化学异构形式，以及其盐，水合物，溶剂化物，其中R和R'具有如本文所定义的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HCV治疗中单独或与其它HCV抑制剂组合的用途。
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公开(公告)号：US08399429B2
公开(公告)日：2013-03-19
申请号：US13130602
申请日：2009-12-08
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
CPC分类号： C07H19/10
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen or halo; R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is a group of formula R7 is optionally substituted phenyl; naphthyl; indolyl or N—C1-C6alkyloxycarbonyl-indolyl; R8 is hydrogen, C1-C6alkyl, benzyl; R8′ is hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ together with the carbon atom to which they are attached form C3-C7cycloalkyl; R9 is C1-C10alkyl, benzyl, or optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译： 式I化合物：包括其任何可能的立体异构体，其中：R 1是氢或卤素; R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4是式R7的基团是任选取代的苯基; 萘基; 吲哚基或N-C 1 -C 6烷氧基羰基 - 吲哚基; R8是氢，C1-C6烷基，苄基; R 8'是氢，C 1 -C 6烷基，苄基; 或R 8和R 8'与它们所连接的碳原子一起形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，苄基或任选取代的苯基; 或其药学上可接受的盐或溶剂合物。 药物制剂和化合物I用作HCV抑制剂。
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公开(公告)号：US20120065156A1
公开(公告)日：2012-03-15
申请号：US13319735
申请日：2010-05-11
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Raboisson , Koen Vandyck , Steven Maurice Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Raboisson , Koen Vandyck , Steven Maurice Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： A61K31/7072 , A61P31/12 , A61P31/14 , C07H19/06 , C07H19/10
CPC分类号： C07H19/10 , C07D493/10 , C07H15/04 , C07H15/18 , C07H19/067
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8′ form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译： 式I化合物：包括其任何可能的立体异构体，其中：R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4为R 7为任选取代的苯基，任选取代的萘基或任选取代的吲哚基; R8和R8'是氢，C1-C6烷基，苄基或苯基; 或R 8和R 8'形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，C 3 -C 7环烷基，苯基或苯基-C 1 -C 6烷基，其中苯基或苯基-C 1 -C 6烷基中的苯基部分任选被取代; 或其药学上可接受的盐或溶剂化物; 药物制剂和化合物I用作HCV抑制剂。
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公开(公告)号：US20110230436A1
公开(公告)日：2011-09-22
申请号：US13130602
申请日：2009-12-08
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
IPC分类号： A61K31/7072 , C07H19/10 , A61P31/14
CPC分类号： C07H19/10
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen or halo; R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is a group of formula R7 is optionally substituted phenyl; naphthyl; indolyl or N—C1-C6alkyloxycarbonylindolyl; R8 is hydrogen, C1-C6alkyl, benzyl; R8′ is hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ together with the carbon atom to which they are attached form C3-C7cycloalkyl; R9 is C1-C10alkyl, benzyl, or optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译： 式I化合物：包括其任何可能的立体异构体，其中：R 1是氢或卤素; R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4是式R7的基团是任选取代的苯基; 萘基; 吲哚基或N-C 1 -C 6烷氧基羰基吲哚基; R8是氢，C1-C6烷基，苄基; R 8'是氢，C 1 -C 6烷基，苄基; 或R 8和R 8'与它们所连接的碳原子一起形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，苄基或任选取代的苯基; 或其药学上可接受的盐或溶剂合物。 药物制剂和化合物I用作HCV抑制剂。
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公开(公告)号：US09012428B2
公开(公告)日：2015-04-21
申请号：US13884852
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
CPC分类号： C07H19/10 , A61K9/2068 , A61K9/284 , A61K9/2866 , C07H19/06
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
摘要翻译： 本发明涉及可用于治疗感染丙型肝炎病毒（HCV）的患者的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。
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公开(公告)号：US08815849B2
公开(公告)日：2014-08-26
申请号：US13812388
申请日：2011-07-26
IPC分类号： A61K31/549 , A61K31/517 , A61K31/4709 , A61K31/4725 , C07D285/22 , C07D417/02 , C07D471/04 , C07D217/00 , C07D215/00
CPC分类号： A61K31/549 , A61K31/4375 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/14 , C07D471/04 , C07D491/10
摘要： Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R′ have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
摘要翻译： 式I的HCV复制抑制剂包括立体化学异构形式，以及其盐，水合物，溶剂化物，其中R和R'具有如本文所定义的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HCV治疗中单独或与其它HCV抑制剂组合的用途。
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公开(公告)号：US08623899B2
公开(公告)日：2014-01-07
申请号：US13389277
申请日：2010-08-06
申请人： David McGowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
发明人： David McGowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
IPC分类号： A61K31/4184 , C07D403/10
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14
摘要： Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R′ have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
摘要翻译： 式I的HCV复制抑制剂包括立体化学异构形式，以及其盐，水合物，溶剂化物，其中R和R'具有如本文所定义的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HCV治疗中单独或与其它HCV抑制剂组合的用途。
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公开(公告)号：US20130244968A1
公开(公告)日：2013-09-19
申请号：US13884852
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： C07H19/10
CPC分类号： C07H19/10 , A61K9/2068 , A61K9/284 , A61K9/2866 , C07H19/06
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
摘要翻译： 本发明涉及用于治疗感染丙型肝炎病毒（HCV）的患者的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。
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公开(公告)号：US20130123244A1
公开(公告)日：2013-05-16
申请号：US13812388
申请日：2011-07-26
IPC分类号： A61K31/549 , A61K31/4709 , A61K45/06 , A61K31/4375 , C07D403/14 , A61K31/517 , C07D417/14 , C07D471/04 , C07D401/14 , A61K31/4725
CPC分类号： A61K31/549 , A61K31/4375 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/14 , C07D471/04 , C07D491/10
摘要： Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R′ have the meaning as defined herein.The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
摘要翻译： 式I的HCV复制抑制剂包括立体化学异构形式，以及其盐，水合物，溶剂化物，其中R和R'具有如本文所定义的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HCV治疗中单独或与其它HCV抑制剂组合的用途。
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