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    Labelled nucleotides
    31.
    发明授权
    Labelled nucleotides 有权
    标记核苷酸

    公开(公告)号：US08084590B2

    公开(公告)日：2011-12-27

    申请号：US12803163

    申请日：2010-06-21

    Applicant: John Milton ,  Silke Ruediger ,  Xiaohai Liu

    Inventor： John Milton ,  Silke Ruediger ,  Xiaohai Liu

    IPC: C07G11/00 ,  C07H21/04 ,  C07H19/04 ,  C12Q1/68

    CPC classification number: C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6869 ,  C12Q1/6874 ,  Y10T436/143333 ,  C12Q2535/113 ,  C12Q2525/186

    Abstract: The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) (wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl). T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

    Abstract translation: 本发明提供了具有通过可切割接头连接到可检测标记的碱基的核苷酸或核苷，其特征在于所述可切割连接体含有选自以下的部分：式（I）（其中X选自O， S，NH和NQ，其中Q是C1-10取代或未取代的烷基，Y选自O，S，NH和N（烯丙基），T是氢或C1-10取代或未取代的烷基， *表示部分连接到核苷酸或核苷的剩余部分）。

    NUCLEOSIDE ANALOGS WITH CARBOXAMIDINE MODIFIED MONOCYCLIC BASE
    35.
    发明申请
    NUCLEOSIDE ANALOGS WITH CARBOXAMIDINE MODIFIED MONOCYCLIC BASE 审中-公开
    用羧甲酰胺改性单烯基的核苷类似物

    公开(公告)号：US20090176721A1

    公开(公告)日：2009-07-09

    申请号：US12400733

    申请日：2009-03-09

    Applicant: Robert Tam ,  Kanda Ramasamy ,  Zhi Hong ,  Johnson Lau

    Inventor： Robert Tam ,  Kanda Ramasamy ,  Zhi Hong ,  Johnson Lau

    IPC: A61K31/7056 ,  A61P31/12 ,  A61P31/18

    CPC classification number: A61K31/7056 ,  A61K31/70 ,  C07H19/056 ,  C07H19/14

    Abstract: Novel nucleoside analog compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.

    Abstract translation: 公开了新的核苷类似物化合物。 新化合物或其药学上可接受的酯或其盐可以用于药物组合物中，并且这些组合物可用于治疗感染，感染，肿瘤或自身免疫性疾病。 新化合物也可用于调节免疫系统的方面，包括调节1型和2型活性。

    Modified nucleotides
    39.
    发明申请
    Modified nucleotides 有权
    修饰的核苷酸

    公开(公告)号：US20070166705A1

    公开(公告)日：2007-07-19

    申请号：US10525401

    申请日：2003-08-22

    Applicant: John Milton ,  Xiaolin Wu ,  Mark Smith ,  Joseph Brennan ,  Colin Barnes ,  Xiaohai Liu ,  Silke Ruediger

    Inventor： John Milton ,  Xiaolin Wu ,  Mark Smith ,  Joseph Brennan ,  Colin Barnes ,  Xiaohai Liu ,  Silke Ruediger

    IPC: C12Q1/68 ,  C07H21/04 ,  C12P19/34 ,  C07F9/6512

    CPC classification number: C12Q1/6869 ,  C07H1/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C12Q2525/186 ,  C12Q2535/113 ,  Y02P20/55 ,  C12Q2525/197

    Abstract: The invention provides modified nucleotide or nucleoside molecule comprising a purine or pyrimidine base and a ribose or deoxyribose sugar moiety having a removable 3′-OH blocking group covalently attached thereto, such that the 3′ carbon atom has attached a group of the structure —O-Z wherein Z is any of —C(R′)2-O—R″, —C(R′)2-N(R″)2, —C(R′)2-N(H)R″, —C(R′)2-S—R″ and —C(R′)2-F, wherein each R″ is or is part of a removable protecting group; each R′ is independently a hydrogen atom, an alkyl, substituted alkyl, arylalkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclic, acyl, cyano, alkoxy, aryloxy, heteroaryloxy or amido group, or a detectable label attached through a linking group; or (R′)2 represents an alkylidene group of formula ═C(R′″)2 wherein each R′″ may be the same or different and is selected from the group comprising hydrogen and halogen atoms and alkyl groups; and wherein said molecule may be reacted to yield an intermediate in which each R″ is exchanged for H or, where Z is —C(R′)2-F, the F is exchanged for OH, SH or NH2, preferably OH, which intermediate dissociates under aqueous conditions to afford a molecule with a free 3′OH; with the proviso that where Z is —C(R′)2-S—R″, both R′ groups are not H.

    Abstract translation: 本发明提供了修饰的核苷酸或核苷分子，其包含嘌呤或嘧啶碱基和核糖或脱氧核糖糖部分，其具有共价连接到其上的可移除的3'-OH封闭基团，使得3'碳原子连接有一组结构-OZ 其中Z是-C（R'）2 -O-R“，-C（R'）2 -N（R”）2，-C（R'）2 -N（H）R“ ，-C（R'）2 -S-R“和-C（R'）2 -F，其中每个R”或是可除去的保护基团的一部分; 每个R'独立地是氢原子，烷基，取代的烷基，芳基烷基，烯基，炔基，芳基，杂芳基，杂环，酰基，氰基，烷氧基，芳氧基，杂芳氧基或酰氨基，或通过连接基团连接的可检测标记; 或（R'）2表示式-C（R“'）2的亚烷基，其中每个R”可以相同或不同，并且选自氢和卤素原子和烷基; 并且其中所述分子可以反应以产生其中每个R“被交换为H的中间体，或者其中Z是-C（R'）2-F，F被交换成OH，SH或NH 2，优选OH， 该中间体在水性条件下解离以得到具有游离3'OH的分子; 条件是其中Z是-C（R'）2 -S-R“，两个R'基团都不是H.

    Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
    40.
    发明授权
    Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase 有权
    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：US07202224B2

    公开(公告)日：2007-04-10

    申请号：US11496338

    申请日：2006-07-31

    Applicant: Anne B. Eldrup ,  Marija Prhavc ,  Phillip Dan Cook ,  Steven S. Carroll ,  David B. Olsen

    Inventor： Anne B. Eldrup ,  Marija Prhavc ,  Phillip Dan Cook ,  Steven S. Carroll ,  David B. Olsen

    IPC: A61K31/70 ,  C07H19/14

    CPC classification number: C07H19/16 ,  A61K9/4858 ,  A61K31/7056 ,  A61K31/7064 ,  A61K31/7076 ,  A61K38/21 ,  A61K45/06 ,  C07D473/00 ,  C07D487/04 ,  C07H19/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/12 ,  C07H19/14 ,  C07H19/20 ,  Y02P20/582 ,  A61K2300/00

    Abstract: The 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 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 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 nucleoside compounds of the present invention.

    Abstract translation: 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药物组合物。 还公开了本发明的核苷化合物抑制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。

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