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    Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines
    1.
    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。

    Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines
    5.
    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
    6.
    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 directed by oligonucleotides containing modified pyrimidines
    7.
    发明授权
    Enhanced triple-helix and double-helix formation directed by oligonucleotides containing modified pyrimidines 失效
    由含有修饰的嘧啶的寡核苷酸引导的增强的三螺旋和双螺旋形成

    公开(公告)号：US06235887B1

    公开(公告)日：2001-05-22

    申请号：US08338352

    申请日：1994-11-14

    申请人： Brian Froehler ,  Robert J. Jones

    发明人： Brian Froehler ,  Robert J. Jones

    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 base analog 5-propynyluracil, 5-propynylcytosine 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 may 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 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。 寡聚体包含碱基类似物5-丙炔基尿嘧啶，5-丙炔基胞嘧啶或相关类似物。 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构建成具有任何所需的序列，条件是该序列通常包括被本发明的类似物替代的一个或多个碱基。 本发明的组合物可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 purines
    9.
    发明授权
    Enhanced triple-helix and double-helix formation with oligomers containing modified purines 失效
    增强的三螺旋和双螺旋形成与含有修饰嘌呤的低聚物

    公开(公告)号：US5594121A

    公开(公告)日：1997-01-14

    申请号：US479248

    申请日：1995-06-07

    申请人： Brian Froehler ,  Mark Matteucci

    发明人： Brian Froehler ,  Mark Matteucci

    IPC分类号： C07H19/04 ,  C07H19/14 ,  C07H19/16 ,  C07H21/00 ,  C12Q1/68 ,  C07H19/00

    CPC分类号： C07H19/04 ,  C07H19/14 ,  C07H19/16 ,  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 7-deaza-7-substituted purines 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 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 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。 寡聚体包含7-脱氮-7-取代的嘌呤或相关类似物。 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。 本发明的低聚物可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。 本发明的组合物可用于诊断目的以检测病毒或疾病状况。

    Oligonucleotides with inverted polarity
    10.
    发明授权
    Oligonucleotides with inverted polarity 失效
    具有反极性的寡核苷酸

    公开(公告)号：US5721218A

    公开(公告)日：1998-02-24

    申请号：US610792

    申请日：1996-03-11

    申请人： Brian Froehler

    发明人： Brian Froehler

    IPC分类号： A61K48/00 ,  C12Q1/68

    CPC分类号： A61K31/7125

    摘要： Oligonucleotides having tandem sequences of inverted polarity, i.e., oligonucleotides comprising regions of the formula: 3'----------5'----C----5'----------3' (1) or 5'----------3'----C----3'----------5' (2) wherein --C-- symbolizes any method of coupling the nucleotide sequence of opposite polarity, are useful for forming an extended triple helix with a double-helical nucleotide duplex. The inverted polarity also stabilizes the single-strand oligonucleotides to exonuclease degradation.

    摘要翻译： 具有反向极性的串联序列的寡核苷酸，即包含下列结构式的区域的寡核苷酸：3' - 5'-C 5' - 3'（1）或5' -3'-C 3'----- 5'（2）其中-C表示任何耦合相反极性的核苷酸序列的方法，可用于形成具有双螺旋核苷酸的延伸的三重螺旋 双工。 反向极性还使单链寡核苷酸稳定到外切核酸酶降解。