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20 条记录 (耗时 0.041 秒)

    Aminooxy-modified nucleosidic compounds and oligomeric compounds prepared therefrom
    4.
    发明授权
    Aminooxy-modified nucleosidic compounds and oligomeric compounds prepared therefrom 有权
    氨基氧改性的核苷化合物及其制备的低聚化合物

    公开(公告)号：US06639062B2

    公开(公告)日：2003-10-28

    申请号：US09370541

    申请日：1999-08-09

    申请人： Muthiah Manoharan ,  Phillip Dan Cook ,  Thazha P. Prakash ,  Andrew M. Kawasaki

    发明人： Muthiah Manoharan ,  Phillip Dan Cook ,  Thazha P. Prakash ,  Andrew M. Kawasaki

    IPC分类号： C07H2100

    CPC分类号： C07H19/06 ,  C07H19/04 ,  C07H19/16 ,  C07H21/00 ,  Y02P20/582

    摘要： Nucleosidic monomers and oligomeric compounds prepared therefrom are provided which have increased nuclease resistance, substituent groups (such as 2′-aminooxy groups) for increasing binding affinity to complementary strand, and regions of 2′-deoxy-erythro-pentofuranosyl nucleotides that activate RNase H. Such oligomeric compounds are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics.

    摘要翻译： 提供了核苷酸单体和由其制备的低聚化合物，其具有增加的核酸酶抗性，用于增加对互补链的结合亲和力的取代基（例如2'-氨基氧基），以及激活RNase H的2'-脱氧 - 赤式 - 呋喃戊糖基核苷酸的区域 这样的寡聚化合物可用于诊断和其他研究目的，用于调节生物体中蛋白质的表达，以及用于诊断，检测和治疗对寡核苷酸治疗剂敏感的其它病症。

    Aminooxy-modified oligonucleotides and methods for making same
    5.
    发明授权
    Aminooxy-modified oligonucleotides and methods for making same 有权
    氨氧基修饰的寡核苷酸及其制备方法

    公开(公告)号：US06172209B2

    公开(公告)日：2001-01-09

    申请号：US09130973

    申请日：1998-08-07

    申请人： Muthiah Manoharan ,  Phillip Dan Cook ,  Thazha P. Prakash ,  Andrew M. Kawasaki

    发明人： Muthiah Manoharan ,  Phillip Dan Cook ,  Thazha P. Prakash ,  Andrew M. Kawasaki

    IPC分类号： C07H2102

    CPC分类号： C07H21/00 ,  C07H15/203 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  Y02P20/582

    摘要： Oligonucleotides and other macromolecules are provided which have increased nuclease resistance, substituent groups (such as 2′-aminooxy groups) for increasing binding affinity to complementary strand, and subsequences of 2′-deoxy-erythro-pentofuranosyl nucleotides that activate RNase H. Such oligonucleotides and macromolecules are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics.

    摘要翻译： 提供具有增加的核酸酶抗性的寡核苷酸和其它大分子，用于增加对互补链的结合亲和力的取代基（例如2'-氨基氧基），以及激活核糖核酸酶H的2'-脱氧 - 赤 - 戊呋喃糖基核苷酸的子序列。这样的寡核苷酸 和大分子可用于诊断和其他研究目的，用于调节生物体中蛋白质的表达，以及用于诊断，检测和治疗对寡核苷酸治疗敏感的其它病症。

    Alkylation of alcohols, amines, thiols and their derivatives by cyclic sulfate intermediates
    6.
    发明授权
    Alkylation of alcohols, amines, thiols and their derivatives by cyclic sulfate intermediates 失效
    通过环状硫酸盐中间体将醇，胺，硫醇及其衍生物烷基化

    公开(公告)号：US06277982B1

    公开(公告)日：2001-08-21

    申请号：US09378665

    申请日：1999-08-20

    申请人： Allister S. Fraser ,  Muthiah Manoharan ,  Phillip Dan Cook ,  Michael E. Jung ,  Andrew M. Kawasaki

    发明人： Allister S. Fraser ,  Muthiah Manoharan ,  Phillip Dan Cook ,  Michael E. Jung ,  Andrew M. Kawasaki

    IPC分类号： C07H2104

    CPC分类号： C07H19/06 ,  C07H21/00

    摘要： Methods for the alkylation of alcohols, amines and thiols by the use of cyclic sulfates are disclosed. The alkylated sulfates formed are versatile intermediates which may be further elaborated by methods of the invention. In particular, methods for the alkylation of the 2′, 3′ or 5′-hydroxy position of nucleosides and nucleoside analogs with cyclic sulfates to form the 2′, 3′ or 5′-O-alkyl sulfate modified compounds are disclosed. Displacement of the 2′,3′ or 5′-O-sulfate with a nucleophile provides 2′, 3′ or 5′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.

    摘要翻译： 公开了通过使用环状硫酸盐烷基化醇，胺和硫醇的方法。 形成的烷基化硫酸盐是通用的中间体，其可以通过本发明的方法进一步阐述。 特别地，公开了用环状硫酸盐将核苷和核苷类似物的2'，3'或5'-羟基位置烷基化以形成2'，3'或5'-烷基硫酸酯改性化合物的方法。 具有亲核试剂的2'，3'或5'-硫酸硫酸酯的置换提供了可用于合成具有改善的杂交亲和力和核酸酶抗性的寡聚化合物的2'，3'或5'- O修饰的核苷和核苷类似物。