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1. 发明授权

US08148349B2 Nucleoside cyclic phosphoramidates for the treatment of RNA-dependent RNA viral infection 有权
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷环状氨基磷酸酯
公开(公告)号：US08148349B2
公开(公告)日：2012-04-03
申请号：US12519038
申请日：2007-12-14
申请人： Malte Meppen , Frank Narjes , Barbara Pacini , Cristina Gardelli , Philippe L. Durette
发明人： Malte Meppen , Frank Narjes , Barbara Pacini , Cristina Gardelli , Philippe L. Durette
IPC分类号： A61K31/70 , C07H19/11
CPC分类号： C07H19/06
摘要： The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I).
摘要翻译：本发明提供式（I）的核苷环状氨基磷酸酯，包含式（I）化合物的药物组合物和抑制RNA依赖性RNA聚合酶的方法，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒使用式（I）化合物的感染。

2. 发明申请

US20100022468A1 NUCLEOSIDE CYCLIC PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 有权
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷酸环磷酰胺
公开(公告)号：US20100022468A1
公开(公告)日：2010-01-28
申请号：US12519038
申请日：2007-12-14
申请人： Malte Meppen , Frank Narjes , Barbara Pacini , Cristina Gardelli , Philippe L. Durette
发明人： Malte Meppen , Frank Narjes , Barbara Pacini , Cristina Gardelli , Philippe L. Durette
IPC分类号： A61K31/7068 , C07H19/06 , A61P31/12
CPC分类号： C07H19/06
摘要： The present invention provides nucleoside cyclic 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 pre-cursors 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 cyclic 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 cyclic phosphoramidates of the present invention.
摘要翻译：本发明提供了作为RNA依赖性RNA病毒聚合酶抑制剂前体的结构式（I）核苷环状氨基磷酸酯。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。它们作为丙型肝炎病毒（HCV）NS5B聚合酶抑制剂作为HCV复制抑制剂前体和/或用于治疗丙型肝炎感染的前体特别有用。本发明还描述了含有这种核苷环状氨基磷酸酯的药物组合物，或者与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合。还公开了本发明的核苷环状氨基磷酸酯抑制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。

3. 发明申请

US20100152128A1 Antiviral Agents 审中-公开
标题翻译：抗病毒药物
公开(公告)号：US20100152128A1
公开(公告)日：2010-06-17
申请号：US12601002
申请日：2008-05-19
申请人： Barbara Attenni , Monica Donghi , Cristina Gardelli , Malte Meppen , Frank Narjes , Barbara Pacini
发明人： Barbara Attenni , Monica Donghi , Cristina Gardelli , Malte Meppen , Frank Narjes , Barbara Pacini
IPC分类号： A61K31/7068 , C07H19/10 , C07H19/14 , A61P31/12 , A61P31/14
CPC分类号： C07H19/10 , A61K31/706 , A61K31/7064 , A61K31/7076 , C07H19/04 , C07H19/20
摘要： A compound of formula (I) and pharmaceutically acceptable salts thereof; compositions containing it and its use in medicine, particularly for the treatment or inhibition of HCV infections, and processes for making it are disclosed.
摘要翻译：式（I）化合物及其药学上可接受的盐; 公开了含有它的组合物及其在药物中的用途，特别是用于治疗或抑制HCV感染的药物及其制备方法。

4. 发明申请

US20100234316A1 Nucleoside Aryl Phosphoramidates for the Treatment of RNA-Dependent RNA Viral Infection 有权
标题翻译：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。

5. 发明授权

US07879815B2 Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection 有权
标题翻译：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。

6. 发明授权

US07232819B2 Dihydroxypyrimidine carboxamide inhibitors of HIV integrase 失效
标题翻译： HIV整合酶的二羟基嘧啶羧酰胺抑制剂
公开(公告)号：US07232819B2
公开(公告)日：2007-06-19
申请号：US10493279
申请日：2002-10-21
申请人： Maria E. Di Francesco , Cristina Gardelli , Steven Harper , Victor G. Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
发明人： Maria E. Di Francesco , Cristina Gardelli , Steven Harper , Victor G. Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
IPC分类号： C07D239/54 , A61K31/515 , C07D209/14
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/10
摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described
摘要翻译：式（I）的4,5-二羟基嘧啶-6-甲酰胺; 被描述为HIV整合酶和HIV复制抑制剂的抑制剂，其中R 1，R 2，R 3和R 4， / SUP>。这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。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。还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法

7. 发明申请

US20070083045A1 Dihydroxypyrimidine carboxamide inhibitors of HIV integrase 失效
标题翻译： HIV整合酶的二羟基嘧啶羧酰胺抑制剂
公开(公告)号：US20070083045A1
公开(公告)日：2007-04-12
申请号：US11516831
申请日：2006-09-07
申请人： Maria Di Francesco , Cristina Gardelli , Steven Harper , Victor Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
发明人： Maria Di Francesco , Cristina Gardelli , Steven Harper , Victor Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
IPC分类号： C07D417/02 , C07D403/14 , C07D413/02
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/10
摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：具有下式的4,5-二羟基嘧啶-6-甲酰胺被描述为HIV整合酶的抑制剂和HIV复制抑制剂，其中R 1，R 2，R 2， 3和R 4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艾滋病的预防，延迟发作和治疗。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。还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

8. 发明授权

US07459452B2 Dihydroxypyrimidine carboxamide inhibitors of HIV integrase 失效
标题翻译： HIV整合酶的二羟基嘧啶羧酰胺抑制剂
公开(公告)号：US07459452B2
公开(公告)日：2008-12-02
申请号：US11516831
申请日：2006-09-07
申请人： Maria E. Di Francesco , Cristina Gardelli , Steven Harper , Victor G. Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
发明人： Maria E. Di Francesco , Cristina Gardelli , Steven Harper , Victor G. Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
IPC分类号： A61K31/515
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/10
摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：描述了下式的4,5-二羟基嘧啶-6-甲酰胺：HIV整合酶抑制剂和HIV复制抑制剂，其中R1，R2，R3和R4如本文所定义。这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。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。还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

9. 发明申请

US20050075356A1 Dihydroxypyrimidine carboxamide inhibitors of hiv integrase 失效
标题翻译：二氢嘧啶甲酰胺抑制剂
公开(公告)号：US20050075356A1
公开(公告)日：2005-04-07
申请号：US10493279
申请日：2002-10-21
申请人： Maria Di Francesco , Cristina Gardelli , Steven Harper , Victor Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
发明人： Maria Di Francesco , Cristina Gardelli , Steven Harper , Victor Matassa , Ester Murgalia , Emanuela Nizi , Paola Pace , Barbara Pacini , Alessia Petrocchi , Marco Poma , Vincenzo Summa
IPC分类号： C07D239/54 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K45/00 , A61K45/06 , A61P31/18 , A61P43/00 , C07D239/557 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/08 , C07D491/10
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/10
摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：式（I）的4,5-二羟基嘧啶-6-甲酰胺; 被描述为HIV整合酶和HIV复制抑制剂的抑制剂，其中R 1，R 2，R 3和R 4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艾滋病的预防，延迟发作和治疗。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。还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

10. 发明申请

US20090136449A1 Tetracyclic Indole Derivatives as Antiviral Agents 审中-公开
标题翻译：四环吲哚衍生物作为抗病毒剂
公开(公告)号：US20090136449A1
公开(公告)日：2009-05-28
申请号：US12084846
申请日：2006-11-09
申请人： Marcello Di Filippo , Steven Harper , Frank Narjes , Barbara Pacini , Alessia Petrocchi , Michael Rowley , Ian Stansfield
发明人： Marcello Di Filippo , Steven Harper , Frank Narjes , Barbara Pacini , Alessia Petrocchi , Michael Rowley , Ian Stansfield
IPC分类号： A61K38/21 , C07D487/04 , A61K31/407 , C07D498/04
CPC分类号： C07D487/04
摘要： The present invention relates to tetracyclic indole derivatives of formula (I); wherein Ar, D1, D2, D3, D4, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
摘要翻译：本发明涉及式（I）的四环吲哚衍生物; 其中Ar，D1，D2，D3，D4，W，X，Y和Z如本文所定义，及其药学上可接受的盐，包含它们的药物组合物及其用于治疗或预防丙型肝炎病毒感染的用途。

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