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    5′ phosphate mimics
    7.
    发明授权
    5′ phosphate mimics 有权
    5'磷酸酯类似物

    公开(公告)号：US08927513B2

    公开(公告)日：2015-01-06

    申请号：US13382346

    申请日：2010-07-07

    申请人： Muthiah Manoharan ,  Kallanthottathil G. Rajeev ,  Marija Prhavc ,  Ivan Zlatev

    发明人： Muthiah Manoharan ,  Kallanthottathil G. Rajeev ,  Marija Prhavc ,  Ivan Zlatev

    IPC分类号： A01N43/04 ,  C07H19/11 ,  C07H19/213

    CPC分类号： C12N15/113 ,  C07H19/10 ,  C07H19/11 ,  C07H19/20 ,  C07H19/213 ,  C12N2310/11

    摘要： The present invention provides nucleosides and oligonucleotides comprising a 5′ phosphate mimics of formula (IVc) or (Vc). One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.

    摘要翻译： 本发明提供了包含式（IVc）或（Vc）的5'磷酸酯模拟物的核苷和寡核苷酸。 本发明的一个方面涉及包含式（Ia）的二核苷酸的修饰核苷和寡核苷酸。 本发明的另一方面涉及一种抑制基因表达的方法，所述方法包括（a）使本发明的寡核苷酸与细胞接触; 和（b）将来自步骤（a）的细胞维持足以获得靶基因的mRNA降解的时间。

    Process for triphosphate oligonucleotide synthesis
    9.
    发明授权
    Process for triphosphate oligonucleotide synthesis 有权
    三磷酸寡核苷酸合成方法

    公开(公告)号：US09035041B2

    公开(公告)日：2015-05-19

    申请号：US13393851

    申请日：2009-12-22

    申请人： Ivan Zlatev ,  Francois Morvan ,  Jean-Jacques Vasseur ,  Francoise Debart ,  Muthiah Manoharan

    发明人： Ivan Zlatev ,  Francois Morvan ,  Jean-Jacques Vasseur ,  Francoise Debart ,  Muthiah Manoharan

    IPC分类号： C07H21/00 ,  C12N15/117

    CPC分类号： C07H21/00 ,  C12N15/117 ,  C12N2310/17 ,  C12N2310/321 ,  C12N2310/3521

    摘要： This invention relates to a process for preparing an oligonucleotide 5′-triphosphate. The process comprises the steps of: (a) synthesizing an oligonucleotide having a 5′ hydroxyl moiety; (b) reacting the 5′ hydroxyl moiety with a reagent of formula I: to convert the 5′ hydroxyl moiety to a 5′-H-phosphonate, wherein R1 and R2 are each independently selected from the group consisting of haloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycle, and substituted heterocycle, acyl, phosphoryl, substituted alkyl acyl, substituted heteroalkyl acyl, substituted aryl acyl or substituted heteroaryl acyl, substituted alkyl phosphoryl, substituted heteroalkyl acyl, substituted aryl phosphoryl, and substituted heteroaryl phosphoryl; (c) activating the H-phosphonate of step (b) by reacting the H-phosphonate with a silylating agent, a halogenated oxidizing agent, a nitrogen-containing heteroaryl, or a combination thereof, to form an activated H-phosphonate; and (d) treating the oligonucleotide having an activated H-phosphonate from step (c) with a poly(alkylammonium)pyrophosphate.

    摘要翻译： 本发明涉及一种制备5'-三磷酸寡核苷酸的方法。 该方法包括以下步骤：（a）合成具有5'羟基部分的寡核苷酸; （b）使5'羟基部分与式I的试剂反应：将5'羟基部分转化为5'-H-膦酸酯，其中R 1和R 2各自独立地选自卤代烷基，芳基，取代的 芳基，杂芳基，取代的杂芳基，环烷基，取代的环烷基，杂环和取代的杂环，酰基，磷酰基，取代的烷基酰基，取代的杂烷基酰基，取代的芳基酰基或取代的杂芳基酰基，取代的烷基磷酰基，取代的杂烷基酰基，取代的芳基磷酰基， 和取代的杂芳基磷酰基; （c）通过使H-膦酸酯与甲硅烷基化试剂，卤化氧化剂，含氮杂芳基或其组合反应来活化步骤（b）的H-膦酸酯，以形成活化的H-膦酸酯; 和（d）用聚（烷基铵）焦磷酸盐处理来自步骤（c）的具有活化的H-膦酸酯的寡核苷酸。