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    Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection
    32.
    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
    33.
    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。

    Compositions and Methods For the Treatment Of Obesity and Sexual Dysfunction
    34.
    发明申请
    Compositions and Methods For the Treatment Of Obesity and Sexual Dysfunction 审中-公开
    肥胖和性功能障碍的治疗方法

    公开(公告)号：US20080200376A1

    公开(公告)日：2008-08-21

    申请号：US11665127

    申请日：2005-10-25

    申请人： Malcolm MacCoss ,  Duncan E. MacIntyre ,  Alison M. Strack

    发明人： Malcolm MacCoss ,  Duncan E. MacIntyre ,  Alison M. Strack

    IPC分类号： A61K38/22 ,  A61K31/155 ,  A61K31/485 ,  A61K31/357 ,  A61K31/42 ,  A61K31/473 ,  A61K31/519 ,  A61P3/00 ,  A61P35/00 ,  A61P9/00 ,  A61P15/00

    CPC分类号： A61K31/519 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to methods of treating and preventing obesity and obesity-related disorders in a subject comprising administering a neurokinin-1 antagonist and an anti-obesity agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further related to methods of treating or preventing sexual dysfunction, including male erectile dysfunction, in a subject comprising administering a neurokinin-1 antagonist and a sexual dysfunction therapeutic agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.

    摘要翻译： 本发明涉及治疗和预防受试者中肥胖和肥胖相关疾病的方法，包括向所述受试者施用神经激肽-1拮抗剂和抗肥胖剂如黑皮质素4受体激动剂。 本发明还涉及治疗或预防包括男性勃起功能障碍在内的性功能障碍的方法，所述方法包括向所述受试者施用神经激肽-1拮抗剂和性功能障碍治疗剂如黑皮质素4受体激动剂。 本发明进一步提供可用于实施这些方法的药物组合物和药物。

    Cyclic amino acid derivatives as cell adhesion inhibitors
    35.
    发明授权
    Cyclic amino acid derivatives as cell adhesion inhibitors 失效
    环状氨基酸衍生物作为细胞粘附抑制剂

    公开(公告)号：US06271252B1

    公开(公告)日：2001-08-07

    申请号：US09554989

    申请日：2000-05-23

    申请人： Linda Chang ,  William K. Hagmann ,  Malcolm MacCoss

    发明人： Linda Chang ,  William K. Hagmann ,  Malcolm MacCoss

    IPC分类号： A61K31401

    CPC分类号： C07D493/08 ,  C07C311/19 ,  C07C311/20 ,  C07C2601/14 ,  C07D207/16

    摘要： Cyclic amino acid derivatives of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

    摘要翻译： 式I的环状氨基酸衍生物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物，并且适用于治疗哮喘，过敏，炎症，多发性硬化以及其它炎性和自身免疫性疾病。

    Nucleoside Aryl Phosphoramidates for the Treatment of RNA-Dependent RNA Viral Infection
    38.
    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。

    Prodrugs of herpes TK inhibitors
    40.
    发明授权
    Prodrugs of herpes TK inhibitors 失效
    疱疹TK抑制剂的前药

    公开(公告)号：US5663175A

    公开(公告)日：1997-09-02

    申请号：US353475

    申请日：1994-12-09

    申请人： Richard L. Tolman ,  John D. Karkas ,  Derek Von Langen ,  Malcolm MacCoss

    发明人： Richard L. Tolman ,  John D. Karkas ,  Derek Von Langen ,  Malcolm MacCoss

    IPC分类号： C07D473/00 ,  C07F9/6561 ,  A61K31/52

    CPC分类号： C07D473/00 ,  C07F9/65616 ,  Y10S514/931 ,  Y10S514/934

    摘要： Certain prodrugs such as ##STR1## are useful in the inhibition of herpes virus thymidine kinase, the prevention or treatment of recurrent infection by herpes virus, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating recurrent infection by herpes virus are also described.

    摘要翻译： 某些前药如“IMAGE”可用于抑制疱疹病毒胸苷激酶，预防或治疗疱疹病毒的复发性感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其它抗病毒药物组合， 免疫调节剂，抗生素或疫苗。 还描述了预防或治疗疱疹病毒复发性感染的方法。