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    Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions
    1.
    发明授权
    Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 失效
    用于在温和条件下合成和去保护肽核酸的合成子

    公开(公告)号：US6133444A

    公开(公告)日：2000-10-17

    申请号：US487666

    申请日：1995-06-07

    申请人： James M. Coull ,  Michael Egholm ,  Richard P. Hodge ,  Mohamed Ismail ,  Sharanappa B. Rajur

    发明人： James M. Coull ,  Michael Egholm ,  Richard P. Hodge ,  Mohamed Ismail ,  Sharanappa B. Rajur

    IPC分类号： C07D239/47 ,  C07D239/46 ,  C07D473/18 ,  C07D473/34 ,  C07D473/40 ,  C07K14/00

    CPC分类号： C07D239/47 ,  C07D473/18 ,  C07D473/34 ,  C07D473/40 ,  C07K14/003 ,  Y02P20/55

    摘要： A method is disclosed for preparing novel purine PNA synthons having protecting groups which may be removed under mild conditions. The purine PNA synthons generally are prepared by coupling purine derivatives having carbamate protection to a protected N-(2-aminoethyl)-glycine backbone. By a method of this invention, purine PNA synthons may have orthogonal protection of the carbamate protected purine and the protected backbone. The purine PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. In practicing methods of the invention, novel compositions of matter also are disclosed. For example, disclosed herein are an adenine PNA synthon having the following formula: ##STR1## and a guanine PNA synthon having the following formula: ##STR2##

    摘要翻译： 公开了一种制备具有可在温和条件下除去的保护基的新型嘌呤PNA合成子的方法。 嘌呤PNA合成酶通常通过将具有氨基甲酸酯保护的嘌呤衍生物与保护的N-（2-氨基乙基） - 甘氨酸主链偶联来制备。 通过本发明的方法，嘌呤PNA合成子可具有氨基甲酸酯保护的嘌呤和被保护的主链的正交保护。 嘌呤PNA合成子可用于合成肽核酸（PNA）和其它寡聚体如PNA-DNA嵌合体，并可用于自动合成仪中。 在本发明的实践方法中，还公开了新的物质组合物。 例如，本文公开了具有下式的腺嘌呤PNA合成子和具有下式的鸟嘌呤PNA合成子：

    Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions
    2.
    发明授权
    Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 失效
    用于在温和条件下合成和去保护肽核酸的合成子

    公开(公告)号：US06172226B2

    公开(公告)日：2001-01-09

    申请号：US09116793

    申请日：1998-07-16

    申请人： James M. Coull ,  Michael Egholm ,  Richard P. Hodge ,  Mohamed Ismail ,  S. B. Rajur

    发明人： James M. Coull ,  Michael Egholm ,  Richard P. Hodge ,  Mohamed Ismail ,  S. B. Rajur

    IPC分类号： C07D23910

    CPC分类号： C07D239/47 ,  C07D473/18 ,  C07D473/34 ,  C07D473/40 ,  C07K14/003 ,  Y02P20/55

    摘要： A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.

    摘要翻译： 公开了一种制备具有能够在温和条件下去除的保护基的新型PNA合成子的方法。 通过将具有杂环的外环氨基的氨基甲酸酯保护的新的N-取代的核碱基中间体与氨基酸N-（2-氨基乙基） - 甘氨酸的氨基保护的主链或氨基保护的主链酯偶联来制备PNA合成子。 通过本发明的方法，所得的PNA合成子可以具有氨基甲酸酯保护的核碱基和氨基保护的主链的正交保护。 PNA合成子可用于合成肽核酸（PNA）和其他寡聚体如PNA-DNA嵌合体，并可用于自动合成仪中。 还公开了新的组合物。 此外，公开了具有不受保护的C6羰基的环外2-氨基的选择性氨基甲酸酯保护的鸟嘌呤PNA合成子。

    Binary probe and clamp composition and methods for target hybridization detection
    5.
    发明授权
    Binary probe and clamp composition and methods for target hybridization detection 有权
    二进制探针和夹钳组成及靶杂交检测方法

    公开(公告)号：US08067165B2

    公开(公告)日：2011-11-29

    申请号：US12538823

    申请日：2009-08-10

    申请人： Kenneth Livak ,  Michael Egholm ,  Michael Hunkapiller

    发明人： Kenneth Livak ,  Michael Egholm ,  Michael Hunkapiller

    IPC分类号： C12Q1/68 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C12Q1/6816 ,  C12Q1/6818 ,  C12Q2549/126 ,  C12Q2537/119 ,  C12Q2525/179

    摘要： Binary probe and clamp compositions conduct methods for target hybridization detection. Where the probe is a substrate for exonuclease cleavage, the composition provides quantitation and detection of PCR products, by real-time and end-point measurements. Where the probe is an amplification primer, the composition provides an improved method for labelling and detection of PCR products. Probes and clamps may be labelled with fluorescent dyes, quenchers, hybridization-stabilizing moieties, chemiluminescent dyes, and affinity ligands. Clamps may be nucleic acid analogs, such as 2-aminoethylglycine PNA.

    摘要翻译： 二进制探针和夹具组合物进行靶杂交检测的方法。 当探针是外切核酸酶切割的底物时，组合物通过实时和终点测量提供PCR产物的定量和检测。 当探针是扩增引物时，组合物提供了PCR产物的标记和检测的改进方法。 探针和夹具可以用荧光染料，猝灭剂，杂交稳定部分，化学发光染料和亲和配体标记。 夹具可以是核酸类似物，例如2-氨基乙基甘氨酸PNA。