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1. 发明申请

US20070161639A1 Hiv integrase inhibitors 审中-公开
标题翻译： 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。

2. 发明授权

US08314062B2 Macrocyclic compounds as antiviral agents 有权
标题翻译：大环化合物作为抗病毒剂
公开(公告)号：US08314062B2
公开(公告)日：2012-11-20
申请号：US12306137
申请日：2007-06-21
申请人： Benedetta Crescenzi , Monica Donghi , Marco Ferrara , Cristina Gardelli , Steven Harper , Uwe Koch , Michael Rowley , Vincenzo Summa
发明人： Benedetta Crescenzi , Monica Donghi , Marco Ferrara , Cristina Gardelli , Steven Harper , Uwe Koch , Michael Rowley , Vincenzo Summa
IPC分类号： A61K38/00
CPC分类号： C07K5/0827 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R1, R2, R3, R4, R5, Ra, M, Z and ring B 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）的大环化合物：其中W，n，m，R1，R2，R3，R4，R5，Ra，M，Z和环B在本文中定义，及其药学上可接受的盐，药物组合物包括它们，以及它们用于治疗或预防丙型肝炎病毒感染的用途。

3. 发明申请

US20090312241A1 Macrocyclic Compounds as Antiviral Agents 有权
标题翻译：大环化合物作为抗病毒剂
公开(公告)号：US20090312241A1
公开(公告)日：2009-12-17
申请号：US12306137
申请日：2007-06-21
申请人： Benedetta Crescenzi , Monica Donghi , Marco Ferrara , Cristina Gardelli , Steven Harper , Uwe Koch , Michael Rowley , Vincenzo Summa
发明人： Benedetta Crescenzi , Monica Donghi , Marco Ferrara , Cristina Gardelli , Steven Harper , Uwe Koch , Michael Rowley , Vincenzo Summa
IPC分类号： A61K38/12 , C07K5/12 , A61P31/12
CPC分类号： C07K5/0827 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R1, R2, R3, R4, R5, Ra, M, Z and ring B 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）的大环化合物：其中W，n，m，R1，R2，R3，R4，R5，Ra，M，Z和环B在本文中定义，及其药学上可接受的盐，药物组合物包括它们，以及它们用于治疗或预防丙型肝炎病毒感染的用途。

4. 发明授权

US08071568B2 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：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）

5. 发明申请

US20100035835A1 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。

6. 发明申请

US20090099168A1 HIV Integrase inhibitors 审中-公开
标题翻译： 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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US07169780B2 N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase 有权
标题翻译： HIV整合酶的N-取代羟基嘧啶酮羧酰胺抑制剂
公开(公告)号：US07169780B2
公开(公告)日：2007-01-30
申请号：US10493280
申请日：2002-10-21
申请人： Benedetta Crescenzi , Cristina Gardelli , Ester Muraglia , Federica Orvieto , Paola Pace , Giovanna Pescatore , Alessia Petrocchi , Marco Poma , Michael Rowley , Rita Scarpelli , Vincenzo Summa , Emanuela Nizi
发明人： Benedetta Crescenzi , Cristina Gardelli , Ester Muraglia , Federica Orvieto , Paola Pace , Giovanna Pescatore , Alessia Petrocchi , Marco Poma , Michael Rowley , Rita Scarpelli , Vincenzo Summa , Emanuela Nizi
IPC分类号： C07D239/54 , A61K31/515 , C07D209/14
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D513/04
摘要： N-substituted 5-hydroxypyrimidin-6-one-4-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N-取代的5-羟基嘧啶-6-酮-4-甲酰胺：描述为HIV整合酶的抑制剂和HIV复制抑制剂，其中R 1，R 2， / SUP>，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

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