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    Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
    1.
    发明授权
    Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection 有权
    用于治疗RNA依赖性RNA病毒感染的核苷芳基氨基磷酸酯

    公开(公告)号：US07879815B2

    公开(公告)日：2011-02-01

    申请号：US12223940

    申请日：2007-02-12

    申请人： Malcolm MacCoss ,  David B. Olsen ,  Monica Donghi ,  Cristina Gardelli ,  Steven Harper ,  Malte Meppen ,  Frank Narjes ,  Barbara Pacini

    发明人： Malcolm MacCoss ,  David B. Olsen ,  Monica Donghi ,  Cristina Gardelli ,  Steven Harper ,  Malte Meppen ,  Frank Narjes ,  Barbara Pacini

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07H19/06

    摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 aryl phosphoramidates of the present invention.

    摘要翻译： 本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。 这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，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聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。 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含有这种核苷芳基氨基磷酸酯的药物组合物。 还公开了本发明的核苷芳基氨基磷酸酯抑制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。

    Nucleoside Aryl Phosphoramidates for the Treatment of RNA-Dependent RNA Viral Infection
    2.
    发明申请
    Nucleoside Aryl Phosphoramidates for the Treatment of RNA-Dependent RNA Viral Infection 有权
    用于治疗RNA依赖性RNA病毒感染的核苷芳基磷酰胺化物

    公开(公告)号：US20100234316A1

    公开(公告)日：2010-09-16

    申请号：US12223940

    申请日：2007-02-12

    申请人： Malcolm MacCoss ,  David B. Olsen ,  Monica Donghi ,  Cristina Gardelli ,  Steven Harper ,  Malte Meppen ,  Frank Narjes ,  Barbara Pacini

    发明人： Malcolm MacCoss ,  David B. Olsen ,  Monica Donghi ,  Cristina Gardelli ,  Steven Harper ,  Malte Meppen ,  Frank Narjes ,  Barbara Pacini

    IPC分类号： A61K31/7068 ,  C07H19/10 ,  A61P31/14

    CPC分类号： C07H19/06

    摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 aryl phosphoramidates of the present invention.

    摘要翻译： 本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。 这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，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聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。 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含有这种核苷芳基氨基磷酸酯的药物组合物。 还公开了本发明的核苷芳基氨基磷酸酯抑制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。

    Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
    4.
    发明授权
    Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection 有权
    用于治疗RNA依赖性RNA病毒感染的核苷芳基氨基磷酸酯

    公开(公告)号：US08071568B2

    公开(公告)日：2011-12-06

    申请号：US12520738

    申请日：2007-12-28

    申请人： Frank Narjes ,  Cristina Gardelli ,  Monica Donghi ,  Barbara Attenni ,  Philippe L. Durette

    发明人： Frank Narjes ,  Cristina Gardelli ,  Monica Donghi ,  Barbara Attenni ,  Philippe L. Durette

    IPC分类号： A61K31/70 ,  C07H19/10

    CPC分类号： C07H19/04 ,  C07H19/048 ,  C07H19/10 ,  C07H19/20

    摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 aryl phosphoramidates of the present invention. (I)

    摘要翻译： 本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。 这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，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聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。 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含有这种核苷芳基氨基磷酸酯的药物组合物。 还公开了本发明的核苷芳基氨基磷酸酯抑制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。 （一世）

    NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION
    5.
    发明申请
    NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 有权
    用于治疗RNA依赖性RNA病毒感染的核苷类ARYL磷酸酯

    公开(公告)号：US20100035835A1

    公开(公告)日：2010-02-11

    申请号：US12520738

    申请日：2007-12-28

    申请人： Frank Narjes ,  Cristina Gardelli ,  Monica Donghi ,  Barbara Attenni ,  Philippe L. Durette

    发明人： Frank Narjes ,  Cristina Gardelli ,  Monica Donghi ,  Barbara Attenni ,  Philippe L. Durette

    IPC分类号： A61K31/7068 ,  C07H19/10 ,  A61P31/00

    CPC分类号： C07H19/04 ,  C07H19/048 ,  C07H19/10 ,  C07H19/20

    摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 aryl phosphoramidates of the present invention.

    摘要翻译： 本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。 这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，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聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。 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含有这种核苷芳基氨基磷酸酯的药物组合物。 还公开了本发明的核苷芳基氨基磷酸酯抑制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。

    Hiv integrase inhibitors
    8.
    发明申请
    Hiv integrase inhibitors 审中-公开
    Hiv整合酶抑制剂

    公开(公告)号：US20070161639A1

    公开(公告)日：2007-07-12

    申请号：US10587601

    申请日：2005-03-01

    申请人： Philip Jones ,  Vincenzo Summa ,  Monica Donghi ,  Cristina Gardelli

    发明人： Philip Jones ,  Vincenzo Summa ,  Monica Donghi ,  Cristina Gardelli

    IPC分类号： A61K31/525 ,  A61K31/498 ,  C07D487/02

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D487/16

    摘要： Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula (I); wherein G, Q, bond a, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

    摘要翻译： 吡啶并吡嗪和嘧啶并吡嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二羟基吡啶甲酰胺具有式（I）; 其中G，Q，键a，R 5，R 6和R 7均在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

    HIV Integrase inhibitors
    9.
    发明申请
    HIV Integrase inhibitors 审中-公开
    HIV整合酶抑制剂

    公开(公告)号：US20090099168A1

    公开(公告)日：2009-04-16

    申请号：US12316027

    申请日：2008-12-09

    申请人： Monica Donghi ,  Cristina Gardelli

    发明人： Monica Donghi ,  Cristina Gardelli

    IPC分类号： A61K31/5377 ,  C07D471/16 ,  A61P31/18 ,  A61K31/4985

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D487/16

    摘要： Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula I: wherein G, Q, bond a, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

    摘要翻译： 吡啶并吡嗪和嘧啶并吡嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二羟基吡啶甲酰胺具有式I：其中G，Q，键a，R 5，R 6和R 7在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

    HIV INTEGRASE INHIBITORS
    10.
    发明申请
    HIV INTEGRASE INHIBITORS 有权
    艾滋病毒整合抑制剂

    公开(公告)号：US20090221571A1

    公开(公告)日：2009-09-03

    申请号：US11992531

    申请日：2006-09-26

    申请人： Vincenzo Summa ,  Olaf Kinzel ,  Monica Donghi

    发明人： Vincenzo Summa ,  Olaf Kinzel ,  Monica Donghi

    IPC分类号： A61K31/519 ,  C07D471/04 ,  C07D413/14 ,  A61K31/5377 ,  A61P31/18

    CPC分类号： C07D471/04

    摘要： Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

    摘要翻译： 式I的吡啶并嘧啶羧酰胺化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中R1，R2，R3，R4，R5和R6如本文所定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。