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    Methods for the dealkylation of phosphonate esters
    4.
    发明授权
    Methods for the dealkylation of phosphonate esters 有权
    膦酸酯的脱烷基化方法

    公开(公告)号：US06465649B1

    公开(公告)日：2002-10-15

    申请号：US09641547

    申请日：2000-08-17

    申请人： Arnold J. Gutierrez ,  Ernest J. Prisbe ,  John C. Rohloff

    发明人： Arnold J. Gutierrez ,  Ernest J. Prisbe ,  John C. Rohloff

    IPC分类号： C07F902

    CPC分类号： C07F9/38 ,  C07F9/409 ,  C07F9/65616

    摘要： Disclosed are methods for the dealkylation of phosphonate esters by use of trimethylchlorosilane as the dealkylating agent. In particular, this invention is directed to the discovery that high yields for the dealkylation of phosphonate esters can be achieved within relatively short reaction times by the use of trimethylchlorosilane provided that the dealkylation procedure occurs in a sealed vessel containing a compatible solvent.

    摘要翻译： 公开了通过使用三甲基氯硅烷作为脱烷基化剂使膦酸酯脱烷基化的方法。 特别地，本发明涉及如下发现：通过使用三甲基氯硅烷可以在相对较短的反应时间内实现膦酸酯的脱烷基化的高产率，条件是脱烷基化程序发生在含有相容溶剂的密封容器中。

    Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines
    7.
    发明授权
    Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
    增强的三螺旋和双螺旋形成与含有修饰嘧啶的低聚物

    公开(公告)号：US06962783B2

    公开(公告)日：2005-11-08

    申请号：US10024818

    申请日：2001-12-18

    申请人： Brian Froehler ,  Rick Wagner ,  Mark Matteucci ,  Robert J. Jones ,  Arnold J. Gutierrez ,  Jeff Pudlo

    发明人： Brian Froehler ,  Rick Wagner ,  Mark Matteucci ,  Robert J. Jones ,  Arnold J. Gutierrez ,  Jeff Pudlo

    IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C12Q1/68 ,  H04L12/24 ,  C07H21/02 ,  C12P19/34

    CPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C12Q1/6839 ,  C12Q2525/101

    摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.

    摘要翻译： 公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。 低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。 本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体 或由靶基因编码的RNA。 本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。 本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。

    Methods of using oligomers containing modified pyrimidines
    8.
    发明授权
    Methods of using oligomers containing modified pyrimidines 失效
    使用含有修饰嘧啶的寡聚物的方法

    公开(公告)号：US5830653A

    公开(公告)日：1998-11-03

    申请号：US473481

    申请日：1995-06-07

    申请人： Brian Froehler ,  Rick Wagner ,  Mark Matteucci ,  Robert J. Jones ,  Arnold J. Gutierrez ,  Jeff Pudlo

    发明人： Brian Froehler ,  Rick Wagner ,  Mark Matteucci ,  Robert J. Jones ,  Arnold J. Gutierrez ,  Jeff Pudlo

    IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C12Q1/68 ,  C12N5/06 ,  C12N5/10

    CPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C12Q1/6839

    摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.

    摘要翻译： 公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。 低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。 本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体 或由靶基因编码的RNA。 本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。 本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。

    Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines
    9.
    发明授权
    Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
    增强的三螺旋和双螺旋形成与含有修饰嘧啶的低聚物

    公开(公告)号：US06380368B1

    公开(公告)日：2002-04-30

    申请号：US08599738

    申请日：1996-02-12

    申请人： Brian Froehler ,  Rick Wagner ,  Mark Mattencci ,  Robert J. Jones ,  Arnold J. Gutierrez ,  Jeff Pudlo

    发明人： Brian Froehler ,  Rick Wagner ,  Mark Mattencci ,  Robert J. Jones ,  Arnold J. Gutierrez ,  Jeff Pudlo

    IPC分类号： C07H2102

    CPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C12Q1/6839 ,  C12Q2525/101

    摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.

    摘要翻译： 公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。 低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。 本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体 或由靶基因编码的RNA。 本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。 本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。