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    Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
    41.
    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。

    Fluorinated Pyrrolo[2,3-D]Pyrimidine Nucleosides for the Treatment of Rna-Dependent Rna Viral Infection
    42.
    发明申请
    Fluorinated Pyrrolo[2,3-D]Pyrimidine Nucleosides for the Treatment of Rna-Dependent Rna Viral Infection 审中-公开
    用于治疗Rna依赖性Rna病毒感染的氟化吡咯并[2,3-D]嘧啶核苷

    公开(公告)号：US20080280842A1

    公开(公告)日：2008-11-13

    申请号：US11664564

    申请日：2005-10-17

    申请人： Malcolm MacCoss ,  David B. Olsen ,  Joseph Leone ,  Philippe L. Durette

    发明人： Malcolm MacCoss ,  David B. Olsen ,  Joseph Leone ,  Philippe L. Durette

    IPC分类号： A61K31/7064 ,  C07H19/04 ,  A61P31/12

    CPC分类号： C07H19/14

    摘要： The present invention provides fluorinated pyrrolo[2,3,d]pyrimidine nucleoside compounds 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 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 fluorinated pyrrolo[2,3-d]pyrimidine nucleoside 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 fluorinated pyrrolo[2,3-d]pyrimidine nucleoside of the present invention.

    摘要翻译： 本发明提供了作为RNA依赖性RNA病毒聚合酶抑制剂的氟化吡咯并[2,3，d]嘧啶核苷化合物。 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。 本发明还描述了含有这种氟化吡咯并[2,3-d]嘧啶核苷的药物组合物，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。 还公开了本发明的氟化吡咯并[2,3-d]嘧啶核苷抑制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
    43.
    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。

    Aminocyclopentyl pyridopyrazinone modulators of chemokine receptor activity
    45.
    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。

    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
    46.
    发明申请
    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase 审中-公开
    核苷衍生物作为rna依赖性rna病毒聚合酶的抑制剂

    公开(公告)号：US20060264389A1

    公开(公告)日：2006-11-23

    申请号：US10521006

    申请日：2003-07-11

    申请人： Balkrishen Bhat ,  Steven Carroll ,  Anne Eldrup ,  Malcolm MacCoss ,  David Olsen ,  Thazha Prakash

    发明人： Balkrishen Bhat ,  Steven Carroll ,  Anne Eldrup ,  Malcolm MacCoss ,  David Olsen ,  Thazha Prakash

    IPC分类号： A61K31/7076 ,  C07H19/22

    CPC分类号： C07H19/14 ,  C07H19/22

    摘要： Thee present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA via 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 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 creating RNA-dependent RNA viral infection with the 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核苷化合物及其某些衍生物。 这些化合物是通过复制的RNA依赖性RNA的抑制剂，并且可用于治疗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药物组合物。 还公开了抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或用本发明的核苷化合物产生RNA依赖性RNA病毒感染的方法。

    Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists
    48.
    发明授权
    Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists 失效
    杂芳基螺醚醚环烷基速激肽受体拮抗剂

    公开(公告)号：US5929094A

    公开(公告)日：1999-07-27

    申请号：US956181

    申请日：1997-10-22

    申请人： Philippe Durette ,  Ihor Kopka ,  Malcolm MacCoss ,  Sander Mills

    发明人： Philippe Durette ,  Ihor Kopka ,  Malcolm MacCoss ,  Sander Mills

    IPC分类号： C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D413/04 ,  A61K31/44

    CPC分类号： C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D413/04

    摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.

    摘要翻译： 本发明涉及由结构式I表示的某些新型化合物或其药学上可接受的盐，其中R3，R6，R7，R8，R11，R12，R13，A，m，n和虚线在本文中定义。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。

    Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
    50.
    发明授权
    Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme 失效
    肽基衍生物作为白细胞介素-1β转换酶的抑制剂

    公开(公告)号：US5430128A

    公开(公告)日：1995-07-04

    申请号：US342991

    申请日：1994-11-21

    申请人： Kevin T. Chapman ,  Malcolm MacCoss ,  Adnan Mjalli

    发明人： Kevin T. Chapman ,  Malcolm MacCoss ,  Adnan Mjalli

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K5/0202 ,  A61K38/00

    摘要： Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia. ##STR1##

    摘要翻译： 发现式I的新型肽基衍生物是白细胞介素-1β转换酶（ICE）的有效抑制剂。 式I化合物可用于治疗肺和气道炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵 关节，骨骼和结缔组织; 包括心包的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 式I化合物也可用于治疗感染（例如，革兰氏阴性休克）的并发症和其中IL1作为自分泌生长因子或作为恶病质介质的肿瘤。