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    C-Purine Nucleoside Analogs As Inhibitors Of Rna-Dependent Rna Viral Polymerase
    1.
    发明申请
    C-Purine Nucleoside Analogs As Inhibitors Of Rna-Dependent Rna Viral Polymerase 有权
    C-嘌呤核苷类似物作为Rna依赖性Rna病毒聚合酶的抑制剂

    公开(公告)号：US20080021047A1

    公开(公告)日：2008-01-24

    申请号：US11628513

    申请日：2005-06-10

    申请人： Gabor Butora ,  Malcolm MacCoss ,  Balkrishen Bhat ,  Anne Eldrup

    发明人： Gabor Butora ,  Malcolm MacCoss ,  Balkrishen Bhat ,  Anne Eldrup

    IPC分类号： A61K31/52 ,  A61K31/519 ,  A61P31/12 ,  C07D473/18 ,  C07D473/34 ,  C07D487/04 ,  C07D491/048 ,  C07D498/04

    CPC分类号： C07D491/04 ,  C07D487/04 ,  C07H19/16 ,  C07H19/20

    摘要： The present invention provides C-purine nucleoside analogs 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 C-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 C-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C-嘌呤核苷类似物及其某些衍生物。 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含有这种C-核苷化合物的药物组合物。 还公开了本发明的C-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。

    C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase
    2.
    发明授权
    C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase 有权
    C-嘌呤核苷类似物作为RNA依赖性RNA病毒聚合酶的抑制剂

    公开(公告)号：US07534767B2

    公开(公告)日：2009-05-19

    申请号：US11628513

    申请日：2005-06-10

    申请人： Gabor Butora ,  Malcolm MacCoss ,  Balkrishen Bhat ,  Anne B. Eldrup

    发明人： Gabor Butora ,  Malcolm MacCoss ,  Balkrishen Bhat ,  Anne B. Eldrup

    IPC分类号： A01N43/04

    CPC分类号： C07D491/04 ,  C07D487/04 ,  C07H19/16 ,  C07H19/20

    摘要： The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors 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 C-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 C-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C-嘌呤核苷类似物及其某些衍生物。 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含有这种C-核苷化合物的药物组合物。 还公开了本发明的C-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。

    Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection
    3.
    发明授权
    Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection 失效
    用于治疗RNA依赖性RNA病毒感染的核糖核苷环缩醛衍生物

    公开(公告)号：US07632821B2

    公开(公告)日：2009-12-15

    申请号：US11990051

    申请日：2006-08-04

    申请人： Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

    发明人： Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of 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 or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals 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 ribonucleoside 2′,3′-cyclic acetals of the present invention.

    摘要翻译： 本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前药。 这些化合物是RNA依赖性RNA病毒复制的抑制剂的前体，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或前药，作为HCV复制抑制剂的前体或前药，和/或用于治疗丙型肝炎感染。 本发明还描述了含有这种核糖核苷2'，3'-环状缩醛单独或与其它对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糖核苷2'，3'-环状缩醛的抑制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。

    Ribonucleoside Cyclic Acetal Derivatives for the Treatment of RNA-Dependent RNA Viral Infection
    4.
    发明申请
    Ribonucleoside Cyclic Acetal Derivatives for the Treatment of RNA-Dependent RNA Viral Infection 失效
    用于治疗RNA依赖性RNA病毒感染的核糖核苷环形缩醛衍生物

    公开(公告)号：US20090099126A1

    公开(公告)日：2009-04-16

    申请号：US11990051

    申请日：2006-08-04

    申请人： Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

    发明人： Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

    IPC分类号： A61K31/7076 ,  C07H19/16 ,  A61K31/7064 ,  A61P31/12 ,  C07H19/06

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of 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 or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals 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 ribonucleoside 2′,3′-cyclic acetals of the present invention.

    摘要翻译： 本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前药。 这些化合物是RNA依赖性RNA病毒复制的抑制剂的前体，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聚合酶的抑制剂的前体或前药，作为HCV复制抑制剂的前体或前药，和/或用于治疗丙型肝炎感染。 本发明还描述了含有这种核糖核苷2'，3'-环状缩醛单独或与其它对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糖核苷2'，3'-环状缩醛的抑制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。

    Aminocyclopentyl pyridopyrazinone modulators of chemokine receptor activity
    5.
    发明申请
    Aminocyclopentyl pyridopyrazinone modulators of chemokine receptor activity 审中-公开
    氨基环戊基吡啶并吡嗪酮调节剂的趋化因子受体活性

    公开(公告)号：US20070155731A1

    公开(公告)日：2007-07-05

    申请号：US10587118

    申请日：2005-01-26

    申请人： Gabor Butora ,  Deodialsingh Guiadeen ,  Shankaran Kothandaraman ,  Malcolm MacCoss ,  Sander Mills ,  Lihu Yang

    发明人： Gabor Butora ,  Deodialsingh Guiadeen ,  Shankaran Kothandaraman ,  Malcolm MacCoss ,  Sander Mills ,  Lihu Yang

    IPC分类号： A61K31/549 ,  A61K31/538 ,  A61K31/498 ,  C07D498/04 ,  C07D491/04 ,  C07D487/04

    CPC分类号： C07D471/04

    摘要： Compounds of Formula I and Formula II (wherein A, E, j, k, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

    摘要翻译： 式I和式II化合物（其中A，E，j，k，m，n，R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8， R 9，R 10，R 15，R 16，R 17， ，R 18，R 19，R 24，R 25，R 26， R 27，R 28，R 29，R 30，R 31， ，R 32，R 33，R 34，X，Y和Z如本文所定义），其是趋化因子受体活性的调节剂，并且是 可用于预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。