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41 条记录 (耗时 0.022 秒)

    Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages
    1.
    发明申请
    Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages 审中-公开
    具有可逆羧酸酯连接的载体相关前体药物

    公开(公告)号：US20140249093A1

    公开(公告)日：2014-09-04

    申请号：US14238447

    申请日：2012-08-10

    申请人： Dirk Vetter ,  Harald Rau

    发明人： Dirk Vetter ,  Harald Rau

    IPC分类号： A61K47/48 ,  A61K31/216

    CPC分类号： A61K31/216 ,  A61K31/25 ,  A61K47/60 ,  A61K47/64

    摘要： The invention provides a carrier-linked prodrugs, wherein the biologically active moieties comprise at least one carboxylic acid and wherein the linkage between the drug moiety and linker is in the form of an ester wherein the hydroxyl group required for ester formation is provided by the linker moiety and the carboxyl group required for ester formation is provided by the drug moiety. The hydroxyl group of the linker is sterically hindered by the presence of an alkyl or aryl group on the carbon directly bound to or adjacent to the carbon carrying the hydroxyl group (α-carbon). The steric effect of the alkyl or aryl group enables greater control of the rate of hydrolytic degradation of such carrier-linked prodrugs.

    摘要翻译： 本发明提供载体连接的前药，其中生物活性部分包含至少一种羧酸，并且其中药物部分和接头之间的连接是酯的形式，其中酯形成所需的羟基由连接体提供 部分和酯形成所需的羧基由药物部分提供。 在直接与携带羟基（α-碳）的碳上键合或相邻的碳上存在烷基或芳基，连接体的羟基被空间位阻。 烷基或芳基的立体效应能够更好地控制这种载体连接的前药的水解降解速率。

    Methods of enzymatic discrimination enhancement and surface-bound double-stranded DNA
    2.
    发明授权
    Methods of enzymatic discrimination enhancement and surface-bound double-stranded DNA 有权
    酶鉴别增强方法和表面结合双链DNA

    公开(公告)号：US08236493B2

    公开(公告)日：2012-08-07

    申请号：US12187503

    申请日：2008-08-07

    申请人： David J. Lockhart ,  Mark S. Chee ,  Martin Digglemann ,  Dirk Vetter

    发明人： David J. Lockhart ,  Mark S. Chee ,  Martin Digglemann ,  Dirk Vetter

    IPC分类号： C12Q1/68

    CPC分类号： C40B60/12 ,  B01J2219/00427 ,  B01J2219/00529 ,  B01J2219/00596 ,  B01J2219/00608 ,  B01J2219/00659 ,  B01J2219/00722 ,  C12Q1/6837 ,  C12Q1/6869 ,  C12Q2565/507 ,  C12Q2521/501

    摘要： Methods for discriminating between fully complementary hybrids and those that differ by one or more base pairs and libraries of unimolecular, double-stranded oligonucleotides on a solid support. In one embodiment, the present invention provides methods of using nuclease treatment to improve the quality of hybridization signals on high density oligonucleotide arrays. In another embodiment, the present invention provides methods of using ligation reactions to improve the quality of hybridization signals on high density oligonucleotide arrays. In yet another embodiment, the present invention provides libraries of unimolecular or intermolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA. In a related aspect, the present invention provides libraries of conformationally restricted probes on a solid support. The probes are restricted in their movement and flexibility using double-stranded oligonucleotides as scaffolding. The probes are also useful in various screening procedures associated with drug discovery and diagnosis. The present invention further provides methods for the preparation and screening of the above libraries.

    摘要翻译： 用于区分完全互补的杂交体与通过一个或多个碱基对不同的那些的方法和在固体支持物上的单分子双链寡核苷酸的文库。 在一个实施方案中，本发明提供了使用核酸酶处理来提高高密度寡核苷酸阵列上杂交信号质量的方法。 在另一个实施方案中，本发明提供了使用连接反应来提高高密度寡核苷酸阵列上杂交信号质量的方法。 在另一个实施方案中，本发明提供了在固体支持物上的单分子或分子间双链寡核苷酸的文库。 这些文库在药物发现中可用于筛选许多生物样品，用于双链寡核苷酸与肽，蛋白质，药物和RNA之间的特异性相互作用。 在相关方面，本发明提供了在固体支持物上的构象限制探针的文库。 使用双链寡核苷酸作为脚手架，探针的运动和灵活性受到限制。 探针也可用于与药物发现和诊断相关的各种筛选程序。 本发明还提供了制备和筛选上述文库的方法。

    METHODS OF ENZYMATIC DISCRIMINATION ENHANCEMENT AND SURFACE-BOUND DOUBLE-STRANDED DNA
    5.
    发明申请
    METHODS OF ENZYMATIC DISCRIMINATION ENHANCEMENT AND SURFACE-BOUND DOUBLE-STRANDED DNA 审中-公开
    酶切鉴定增强和表面双重双链DNA的方法

    公开(公告)号：US20120164693A1

    公开(公告)日：2012-06-28

    申请号：US11950213

    申请日：2007-12-04

    申请人： David J. Lockhart ,  Mark S. Chee ,  Dirk Vetter ,  Martin Digglemann

    发明人： David J. Lockhart ,  Mark S. Chee ,  Dirk Vetter ,  Martin Digglemann

    IPC分类号： C12P19/34 ,  C40B40/06 ,  C40B30/04

    CPC分类号： C12N15/1093 ,  B01J19/0046 ,  B01J2219/00529 ,  B01J2219/00608 ,  B01J2219/00612 ,  B01J2219/00626 ,  B01J2219/0063 ,  B01J2219/00659 ,  B01J2219/00722 ,  C07B2200/11 ,  C07H21/00 ,  C12Q1/6827 ,  C12Q1/683 ,  C12Q1/6837 ,  C12Q1/6874 ,  C40B40/06 ,  C40B80/00 ,  G01N33/5308 ,  G01N33/551

    摘要： Methods for discriminating between fully complementary hybrids and those that differ by one or more base pairs and libraries of unimolecular, double-stranded oligonucleotides on a solid support. In one embodiment, the present invention provides methods of using nuclease treatment to improve the quality of hybridization signals on high density oligonucleotide arrays. In another embodiment, the present invention provides methods of using ligation reactions to improve the quality of hybridization signals on high density oligonucleotide arrays. In yet another embodiment, the present invention provides libraries of unimolecular or intermolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA. In a related aspect, the present invention provides libraries of conformationally restricted probes on a solid support. The probes are restricted in their movement and flexibility using double-stranded oligonucleotides as scaffolding. The probes are also useful in various screening procedures associated with drug discovery and diagnosis. The present invention further provides methods for the preparation and screening of the above libraries.

    摘要翻译： 用于区分完全互补的杂交体与通过一个或多个碱基对不同的那些的方法和在固体支持物上的单分子双链寡核苷酸的文库。 在一个实施方案中，本发明提供了使用核酸酶处理来提高高密度寡核苷酸阵列上杂交信号质量的方法。 在另一个实施方案中，本发明提供了使用连接反应来提高高密度寡核苷酸阵列上杂交信号质量的方法。 在另一个实施方案中，本发明提供了在固体支持物上的单分子或分子间双链寡核苷酸的文库。 这些文库在药物发现中可用于筛选许多生物样品，用于双链寡核苷酸与肽，蛋白质，药物和RNA之间的特异性相互作用。 在相关方面，本发明提供了在固体支持物上的构象限制探针的文库。 使用双链寡核苷酸作为脚手架，探针的运动和灵活性受到限制。 探针也可用于与药物发现和诊断相关的各种筛选程序。 本发明还提供了制备和筛选上述文库的方法。