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    Oligomeric compounds for the modulation of Bcl-2
    5.
    发明申请
    Oligomeric compounds for the modulation of Bcl-2 失效
    用于调节Bcl-2的低聚物

    公开(公告)号：US20050203042A1

    公开(公告)日：2005-09-15

    申请号：US11021729

    申请日：2004-12-23

    申请人： Miriam Frieden ,  Jens Hansen ,  Henrik Orum ,  Majken Westergaard ,  Charlotte Thrue

    发明人： Miriam Frieden ,  Jens Hansen ,  Henrik Orum ,  Majken Westergaard ,  Charlotte Thrue

    IPC分类号： A61K48/00 ,  C07H21/02 ,  C12N15/113

    CPC分类号： C12N15/1135 ,  A61K48/00 ,  C07H21/00 ,  C12N2310/315 ,  C12N2310/3231

    摘要： The present invention provides improved oligomeric compound, in particular oligonucleotide compounds, and methods for modulating the expression of the Bcl-2 gene in humans. In particular, this invention relates to oligomeric compounds of 10-30 nucleobases in length which comprise a target binding domain that is specifically hybridizable to a region ranging from base position No. 1459 (5′) to No. 1476 (3′) of the human Bcl-2 mRNA, said target binding domain having the formula: 5′-[(DNA/RNA)0-1-(LNA/LNA*)2-7-(DNA/RNA/LNA*)4-14-(LNA/LNA*)2-7-(DNA/RNA)0-1]-3 and said target binding domain comprising at least two LNA nucleotides or LNA analogue nucleotides linked by a phosphorothioate group (—O—P(O,S)—O—). In particular the oligo is predominantly or fully thiolated. The invention also provides the use of such oligomers or conjugates or chimera for the treatment of various diseases associated with the expression of the Bcl-2 gene, such as cancer.

    摘要翻译： 本发明提供了改进的低聚化合物，特别是寡核苷酸化合物，以及调节人类Bcl-2基因表达的方法。 特别地，本发明涉及长度为10-30个核碱基的寡聚化合物，其包含与从第1459（5'）至第1476（3'）的基础位置区别特异性杂交的靶结合结构域 所述目标结合结构域具有下式：5' - [（DNA / RNA）0-1 - （LNA / LNA *）2-7 - （DNA / RNA / LNA *）4-14 - （LNA / LNA *）2-7 - （DNA / RNA）

    Oligomeric compounds for the modulation of Bcl-2
    6.
    发明授权
    Oligomeric compounds for the modulation of Bcl-2 失效
    用于调节Bcl-2的低聚物

    公开(公告)号：US07622453B2

    公开(公告)日：2009-11-24

    申请号：US11021729

    申请日：2004-12-23

    申请人： Miriam Frieden ,  Jens B. Hansen ,  Henrik Orum ,  Majken Westergaard ,  Charlotte A. Thrue

    发明人： Miriam Frieden ,  Jens B. Hansen ,  Henrik Orum ,  Majken Westergaard ,  Charlotte A. Thrue

    IPC分类号： A01N61/00 ,  A01N43/04 ,  C12Q1/68 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C12N15/1135 ,  A61K48/00 ,  C07H21/00 ,  C12N2310/315 ,  C12N2310/3231

    摘要： The present invention provides improved oligomeric compound, in particular oligonucleotide compounds, and methods for modulating the expression of the Bcl-2 gene in humans. In particular, this invention relates to oligomeric compounds of 10-30 nucleobases in length which comprise a target binding domain that is specifically hybridizable to a region ranging from base position No. 1459 (5′) to No. 1476 (3′) of the human Bcl-2 mRNA, said target binding domain having the formula: 5′-[(DNA/RNA)0-1-(LNA/LNA*)2-7-(DNA/RNA/LNA*)4-14-(LNA/LNA*)2-7-(DNA/RNA)0-1]-3′ and said target binding domain comprising at least two LNA nucleotides or LNA analogue nucleotides linked by a phosphorothioate group (—O—P(O,S)—O—). In particular the oligo is predominantly or fully thiolated. The invention also provides the use of such oligomers or conjugates or chimera for the treatment of various diseases associated with the expression of the Bcl-2 gene, such as cancer.

    摘要翻译： 本发明提供了改进的低聚化合物，特别是寡核苷酸化合物，以及调节人类Bcl-2基因表达的方法。 特别地，本发明涉及长度为10-30个核碱基的寡聚化合物，其包含与从第1459（5'）至第1476（3'）的基础位置区别特异性杂交的靶结合结构域 所述靶结合结构域具有下式：5' - [（DNA / RNA）0-1-（LNA / LNA *）2-7-（DNA / RNA / LNA *）4-14-（ LNA / LNA *）2-7-（DNA / RNA）0-1] -3'，并且所述靶结合结构域包含由硫代磷酸酯基团连接的至少两个LNA核苷酸或LNA类似物核苷酸（-OP（O，S） - O-）。 特别地，寡核苷酸主要或完全硫醇化。 本发明还提供了这种寡聚物或缀合物或嵌合体用于治疗与Bcl-2基因（例如癌症）的表达相关的各种疾病的用途。