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1.发明申请NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开作为RNA依赖性RNA病毒聚合酶抑制剂的核苷衍生物公开(公告)号：US20140309412A1
公开(公告)日：2014-10-16
申请号：US13916322
申请日：2013-06-12
申请人： Balkrishen Bhat , Anne B. El drup , Thazha P. Prakash , Phillip Dan Cook , Robert L. LaFemina , Amy L. Simcoe , Carrie A. Rutkowski , Mario A. Valenciano
发明人： Balkrishen Bhat , Anne B. El drup , Thazha P. Prakash , Phillip Dan Cook , Robert L. LaFemina , Amy L. Simcoe , Carrie A. Rutkowski , Mario A. Valenciano
IPC分类号： C07H17/02
CPC分类号： C07H19/10 , A61K9/4858 , C07D471/04 , C07D473/34 , C07D487/04 , C07H17/02 , C07H19/06 , C07H19/16 , C07H19/207 , Y02P20/582
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
摘要翻译： 本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。 这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。 本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。 还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。
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公开(公告)号：US08481712B2
公开(公告)日：2013-07-09
申请号：US11701682
申请日：2007-02-02
申请人： Balkrishen Bhat , Anne B. Eldrup , Thazha P. Prakash , Phillip Dan Cook , Robert L. LaFemina , Amy L. Simcoe , Carrie A. Rutkowski , Mario A. Valenciano
发明人： Balkrishen Bhat , Anne B. Eldrup , Thazha P. Prakash , Phillip Dan Cook , Robert L. LaFemina , Amy L. Simcoe , Carrie A. Rutkowski , Mario A. Valenciano
CPC分类号： C07H19/10 , A61K9/4858 , C07D471/04 , C07D473/34 , C07D487/04 , C07H17/02 , C07H19/06 , C07H19/16 , C07H19/207 , Y02P20/582
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
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公开(公告)号：US08354518B2
公开(公告)日：2013-01-15
申请号：US10577893
申请日：2004-11-03
申请人： Steven W. Ludmerer , Donald J. Graham , Robert L. LaFemina , Osvaldo A. Flores , Maura Pizzuti , Cinzia Traboni
发明人： Steven W. Ludmerer , Donald J. Graham , Robert L. LaFemina , Osvaldo A. Flores , Maura Pizzuti , Cinzia Traboni
CPC分类号： C12Q1/707 , C07K14/005 , C12N7/00 , C12N2770/24221 , C12N2770/24222
摘要： The present invention features methods for enhancing the ability of a genotype 2b NS5B sequence to function in a replicon, for producing replicons containing a functional genotype 2b NS5B, and for using replicons to measure the ability of a compound to affect HCV replication that is sustained with the genotype 2b polymerase. Also featured is a genotype 1b NS4B adaptive mutation. The ability to produce replicons containing a functional genotype 2b NS5B is illustrated by the production of chimeric replicons based on HCV genotype 1b where substantially all the NS5B sequence is replaced with a genotype 2b NS5B.
摘要翻译： 本发明的特征在于增强基因型2b NS5B序列在复制子中起作用的能力的方法，用于产生含有功能性基因型2b NS5B的复制子，并且使用复制子来测量化合物影响HCV复制的能力 基因型2b聚合酶。 还有一个基因型1b NS4B自适应突变。 通过产生基于HCV基因型1b的嵌合复制子来说明产生含有功能性基因型2b NS5B的复制子的能力，其中基本上所有NS5B序列被基因型2b NS5B替代。
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公开(公告)号：US07569374B2
公开(公告)日：2009-08-04
申请号：US12002392
申请日：2007-12-17
CPC分类号： C07K14/005 , C07H21/00 , C07H21/04 , C12N9/127 , C12N2770/24222 , G01N2333/18 , G01N2333/9125 , G01N2500/04
摘要： The present invention features NS5B polypeptides from different clinically important HCV genotypes. The polypeptides can be used individually, or as part of a panel of RNA-dependent RNA polymerases, to evaluate the effectiveness of a compound to inhibit NS5B activity.
摘要翻译： 本发明特征来自不同临床重要HCV基因型的NS5B多肽。 多肽可以单独使用或作为一组RNA依赖性RNA聚合酶的一部分使用，以评估化合物抑制NS5B活性的有效性。
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公开(公告)号：US07329732B2
公开(公告)日：2008-02-12
申请号：US10584810
申请日：2005-01-06
CPC分类号： C07K14/005 , C07H21/00 , C07H21/04 , C12N9/127 , C12N2770/24222 , G01N2333/18 , G01N2333/9125 , G01N2500/04
摘要： The present invention features NS5B polypeptides from different clinically important HCV genotypes. The polypeptides can be used individually, or as part of a panel of RNA-dependent RNA polymerases, to evaluate the effectiveness of a compound to inhibit NS5B activity.
摘要翻译： 本发明特征来自不同临床重要HCV基因型的NS5B多肽。 多肽可以单独使用或作为一组RNA依赖性RNA聚合酶的一部分使用，以评估化合物抑制NS5B活性的有效性。
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公开(公告)号：US20080187903A1
公开(公告)日：2008-08-07
申请号：US12002392
申请日：2007-12-17
IPC分类号： C12Q1/00 , C07K14/005 , C07H21/04 , C12N15/63
CPC分类号： C07K14/005 , C07H21/00 , C07H21/04 , C12N9/127 , C12N2770/24222 , G01N2333/18 , G01N2333/9125 , G01N2500/04
摘要： The present invention features NS5B polypeptides from different clinically important HCV genotypes. The polypeptides can be used individually, or as part of a panel of RNA-dependent RNA polymerases, to evaluate the effectiveness of a compound to inhibit NS5B activity.
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7.发明授权公开(公告)号：US07323453B2
公开(公告)日：2008-01-29
申请号：US10504445
申请日：2003-02-07
CPC分类号： A61K31/7064 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/655 , A61K31/7068 , A61K31/7076 , A61K31/708 , A61K45/06
摘要： The present invention provides methods of inhibiting orthopoxvirus replication and/or treating orthopoxvirus infection with certain nucleoside compounds and derivatives thereof. These compounds are particularly useful as inhibitors of vaccinia virus and variola virus replication and/or for the treatment of vaccinia virus and variola virus infection. The nucleoside compounds may be administered alone or in combination with other agents active against orthopoxvirus infection, in particular against vaccinia virus or variola virus infection. Another aspect of the present invention provides for the use of such nucleoside compounds in the manufacture of a medicament for the inhibition of orthopoxvirus replication and/or for the treatment of orthopoxvirus infection. Yet a further aspect of the present invention provides such nucleoside compounds for use as a medicament for the inhibition of orthopoxvirus replication and/or for the treatment of orthopoxvirus infection.
摘要翻译： 本发明提供了用某些核苷化合物及其衍生物抑制正痘病毒复制和/或治疗正痘病毒感染的方法。 这些化合物特别可用作痘苗病毒和天花病毒复制的抑制剂和/或用于治疗痘苗病毒和天花病毒感染。 核苷化合物可以单独施用或与其它对抗正痘病毒感染，特别是针对痘苗病毒或天花病毒感染的试剂组合施用。 本发明的另一方面提供了这样的核苷化合物在制备用于抑制正痘病毒复制和/或治疗正痘病毒感染的药物中的用途。 本发明的另一方面提供了用作抑制正痘病毒复制和/或治疗正痘病毒感染的药物的这种核苷化合物。
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8.发明申请Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase 有权核苷衍生物作为RNA依赖性RNA病毒聚合酶的抑制剂公开(公告)号：US20120165515A1
公开(公告)日：2012-06-28
申请号：US11701682
申请日：2007-02-02
申请人： Balkrishen Bhat , Anne B. Eldrup , Thazha P. Prakash , Phillip Dan Cook , Robert L. LaFemina , Amy L. Simcoe , Carrie A. Rutkowski , Mario A. Valenciano
发明人： Balkrishen Bhat , Anne B. Eldrup , Thazha P. Prakash , Phillip Dan Cook , Robert L. LaFemina , Amy L. Simcoe , Carrie A. Rutkowski , Mario A. Valenciano
IPC分类号： C07H19/20
CPC分类号： C07H19/10 , A61K9/4858 , C07D471/04 , C07D473/34 , C07D487/04 , C07H17/02 , C07H19/06 , C07H19/16 , C07H19/207 , Y02P20/582
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
摘要翻译： 本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。 这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。 本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。 还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。
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公开(公告)号：US20110250628A1
公开(公告)日：2011-10-13
申请号：US10577893
申请日：2004-11-03
申请人： Steven W. Ludmerer , Donald J. Graham , Robert L. Lafemina , Osvaldo A. Flores , Maura Pizzuti , Cinzia Traboni
发明人： Steven W. Ludmerer , Donald J. Graham , Robert L. Lafemina , Osvaldo A. Flores , Maura Pizzuti , Cinzia Traboni
CPC分类号： C12Q1/707 , C07K14/005 , C12N7/00 , C12N2770/24221 , C12N2770/24222
摘要： The present invention features methods for enhancing the ability of a genotype 2b NS5B sequence to function in a replicon, for producing replicons containing a functional genotype 2b NS5B, and for using replicons to measure the ability of a compound to affect HCV replication that is sustained with the genotype 2b polymerase. Also featured is a genotype 1b NS4B adaptive mutation. The ability to produce replicons containing a functional genotype 2b NS5B is illustrated by the production of chimeric replicons based on HCV genotype 1b where substantially all the NS5B sequence is replaced with a genotype 2b NS5B.
摘要翻译： 本发明的特征在于增强基因型2b NS5B序列在复制子中起作用的能力的方法，用于产生含有功能性基因型2b NS5B的复制子，并且使用复制子来测量化合物影响HCV复制的能力 基因型2b聚合酶。 还有一个基因型1b NS4B自适应突变。 通过产生基于HCV基因型1b的嵌合复制子来说明产生含有功能性基因型2b NS5B的复制子的能力，其中基本上所有NS5B序列被基因型2b NS5B替代。
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