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    DERIVATIZED OLIGONUCLEOTIDES HAVING IMPROVED UPTAKE
    4.
    发明授权
    DERIVATIZED OLIGONUCLEOTIDES HAVING IMPROVED UPTAKE 失效
    衍生化寡核苷酸具有改进的记录资产的

    公开(公告)号：EP0724447B1

    公开(公告)日：2003-05-07

    申请号：EP92923139.7

    申请日：1992-10-23

    申请人： ISIS PHARMACEUTICALS, INC.

    发明人： MANOHARAN, Muthiah ,  COOK, Philip, Dan ,  BENNETT, Clarence Frank

    IPC分类号： A61K31/70 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C07H23/00 ,  C07J43/003 ,  C07J51/00

    摘要： Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid soluble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercalator, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2'-position of the functionalized nucleoside via a linking group. If at least a portion of the remaining linked nucleosides are 2'-deoxy-2'-fluoro, 2'-O-methoxy, 2'-O-ethoxy, 2'-O-propoxy, 2'-O-aminoalkoxy or 2'-O-allyloxy nucleosides, the substituent can be attached via a linking group at any of the 3' or the 5' positions of the nucleoside or on the heterocyclic base of the nucleoside or on the inter-nucleotide linkage linking the nucleoside to an adjacent nucleoside.

    IMPROVED PROCESS FOR THE SYNTHESIS OF OLIGONUCLEOTIDES INCORPORATING 2-AMINOADENOSINE
    6.
    发明公开
    IMPROVED PROCESS FOR THE SYNTHESIS OF OLIGONUCLEOTIDES INCORPORATING 2-AMINOADENOSINE 审中-公开
    用于合成2-氨基腺苷的寡核苷酸合成的改进方法

    公开(公告)号：EP1109825A1

    公开(公告)日：2001-06-27

    申请号：EP99945350.9

    申请日：1999-08-31

    申请人： ISIS PHARMACEUTICALS, INC.

    发明人： ROSS, Bruce, S. ,  MANOHARAN, Muthiah

    IPC分类号： C07K1/16

    CPC分类号： C07H21/00

    摘要： This invention presents novel processes for incorporating 2-aminoadenosine and 2-aminoadenosine analogs into oligonucleotides. A halogenated adenosine is incorporated into an oligonucleotide using standard synthesis methods, such as phosphoramidited protocols. Subsequent reaction with an amine results in the desired product. The oligonucleotides produced provide stronger hybridization to their target sequences. These oligonucleotides can be useful compounds, inter alia for diagnostic and therapeutic applications.

    摘要翻译： 本发明提出了将2-氨基腺苷和2-氨基腺苷类似物掺入寡核苷酸的新方法。 使用标准合成方法如磷酰胺化方案将卤化腺苷掺入寡核苷酸中。 随后与胺反应产生所需产物。 产生的寡核苷酸提供了与其靶序列更强的杂交。 这些寡核苷酸尤其可用于诊断和治疗应用。