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    Sugar-modified 7-deaza-7-substituted oligonucleotides
    4.
    发明授权
    Sugar-modified 7-deaza-7-substituted oligonucleotides 失效
    糖修饰的7-脱氮-7-取代的寡核苷酸

    公开(公告)号：US6093807A

    公开(公告)日：2000-07-25

    申请号：US272977

    申请日：1999-03-19

    申请人： Guity P. Balow ,  Oscar L. Acevedo ,  Phillip Dan Cook

    发明人： Guity P. Balow ,  Oscar L. Acevedo ,  Phillip Dan Cook

    IPC分类号： C07H19/14 ,  C07H19/16 ,  C07H21/02

    CPC分类号： C07H19/16 ,  C07H19/14

    摘要： Functionalized nucleomonomers and oligonucleotides are provided which have increased nuclease resistance and enhanced binding affinity to target DNA or RNA molecules. The oligonucleotides of the present invention comprise at least one 7-deaza-7-iodo-2'-substituted purine, herein referred to as a functionalized nucleomonomer. A preferred 2' substituent on the sugar moiety is a 2'-O-alkoxy alkyl group. More preferably, the 2'-substituent is 2'--O--CH.sub.2 --CH.sub.2 --O--CH.sub.3 (or 2'-methoxyethoxy). Such oligonucleotides are useful as therapeutics for modulating protein expression in organisms and treating disease states susceptible to oligonucleotide therapeutics. Such oligonucleotides are also useful as diagnostics for the diagnosis and detection of disease states, and as research reagents.

    摘要翻译： 提供功能化的核小体单体和寡核苷酸，其具有增加的核酸酶抗性并增强与靶DNA或RNA分子的结合亲和力。 本发明的寡核苷酸包含至少一种7-脱氮-7-碘-2'-取代嘌呤，在本文中称为官能化核小体单体。 糖部分上优选的2'取代基是2'-O-烷氧基烷基。 更优选地，2'-取代基是2'-O-CH 2 -CH 2 -O-CH 3（或2'-甲氧基乙氧基）。 这样的寡核苷酸可用作调节生物体中的蛋白质表达并治疗对寡核苷酸治疗敏感的疾病状态的治疗剂。 这样的寡核苷酸也可用作诊断和检测疾病状态以及作为研究试剂。