Nucleosidic and non-nucleosidic folate conjugates
    1.
    发明授权
    Nucleosidic and non-nucleosidic folate conjugates 有权
    核苷和非核苷酸叶酸偶联物

    公开(公告)号:US06335434B1

    公开(公告)日:2002-01-01

    申请号:US09275505

    申请日:1999-03-24

    IPC分类号: C12Q168

    CPC分类号: C07H15/26 C07D475/04

    摘要: Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2′-, 3′-, 5′-, nucleobase and internucleotide linkage sites. The folate can be attached via the &agr;- or &ggr;-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are diclosed. Also disclosed are nucleosidic and non-nucleosidic linkers conjugated to folic acid and related folates.

    摘要翻译: 描述了寡核苷酸 - 叶酸盐缀合物,其中叶酸酯与包含2',3',5',核碱基和核苷酸间位点的寡核苷酸上的一个或多个位点缀合。 叶酸可以通过α-或γ-羧酸盐,任选地通过连接基团连接。 缀合物区域特异性合成的方法是分开的。 还公开了与叶酸和相关叶酸缀合的核苷和非核苷酸接头。

    Labeled oligonucleotides, methods for making same, and compounds useful therefor
    6.
    发明授权
    Labeled oligonucleotides, methods for making same, and compounds useful therefor 失效
    标记的寡核苷酸,其制备方法以及对其有用的化合物

    公开(公告)号:US06825338B2

    公开(公告)日:2004-11-30

    申请号:US09823031

    申请日:2001-03-30

    IPC分类号: C07H2100

    CPC分类号: C07H21/00

    摘要: Selectively functionalized oligonucleotides, methods for making same, and compounds useful therefor are disclosed. The oligonucleotides can be selectively functionalized with a first conjugate group at the 3′-terminial position and optionally functionalized with a second conjugate group at the 5′-terminal position and/or one or more internucleotides. Alternatively, the oligonucleotides can be selectively functionalized with a first conjugate group at the 5′-terminal position and optionally functionalized with a second conjugate group at one or more internucleotides. In yet another embodiment, the oligonucleotides can be functionalized with a first conjugate group at one or more internucleotides and with a second conjugate group at one or more different internucleotides.

    摘要翻译: 公开了选择性官能化的寡核苷酸,其制备方法及其有用的化合物。 寡核苷酸可以在3'-末端位置用第一个共轭基团选择性地官能化,并且任选地在5'-末端位置用第二个共轭基团官能化和/或一个或多个核苷酸。 或者,寡核苷酸可以在5'-末端位置用第一缀合基团选择性官能化,并且任选地在一个或多个核苷酸上用第二缀合物官能化。 在另一个实施方案中,寡核苷酸可以用一个或多个核苷酸上的第一缀合基团和在一个或多个不同核苷酸处的第二缀合基团进行官能化。