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    Oligomeric compositions and methods
    23.
    发明申请
    Oligomeric compositions and methods 有权
    低聚组合物和方法

    公开(公告)号：US20060142232A1

    公开(公告)日：2006-06-29

    申请号：US11251564

    申请日：2005-10-13

    申请人： Garth Kinberger ,  Martin Maier ,  Richard Griffey ,  Eric Swazye

    发明人： Garth Kinberger ,  Martin Maier ,  Richard Griffey ,  Eric Swazye

    IPC分类号： A61K48/00

    CPC分类号： A61K47/62 ,  A61K47/549

    摘要： The activated oligomer compounds described herein are capable of forming bio-reversible covalent bonds with plasma proteins, in particular with human serum albumin. The plasma protein-oligomer complexes of the present invention exhibit enhanced cellular entry and significantly enhanced serum half-life.

    摘要翻译： 本文所述的活化的寡聚体化合物能够与血浆蛋白形成生物可逆共价键，特别是与人血清白蛋白形成。 本发明的血浆蛋白质 - 低聚物复合物表现出增强的细胞进入和显着增强的血清半衰期。

    Chimeric oligomeric compounds and their use in gene modulation
    26.
    发明申请
    Chimeric oligomeric compounds and their use in gene modulation 审中-公开
    嵌合寡聚化合物及其在基因调控中的应用

    公开(公告)号：US20050053976A1

    公开(公告)日：2005-03-10

    申请号：US10859825

    申请日：2004-06-03

    申请人： Brenda Baker ,  Anne Eldrup ,  Muthiah Manoharan ,  Balkrishen Bhat ,  Richard Griffey ,  Eric Swayze ,  Stanley Crooke

    发明人： Brenda Baker ,  Anne Eldrup ,  Muthiah Manoharan ,  Balkrishen Bhat ,  Richard Griffey ,  Eric Swayze ,  Stanley Crooke

    IPC分类号： A61K48/00 ,  C07H21/02 ,  C12Q1/68

    CPC分类号： A61K31/713

    摘要： Oligomer compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capble of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes at least one nucleotide comprising a chimeric organic composition. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide comprising a chimeric organic composition.

    摘要翻译： 提供包含第一和第二寡聚物的低聚物组合物，其中至少一部分第一寡聚体能够与至少一部分第二寡聚物杂交，至少一部分第一寡聚体与所选择的寡核苷酸杂交互补和杂交 靶核酸，并且所述第一或第二寡聚体中的至少一个包含至少一个包含嵌合有机组合物的核苷酸。 还提供寡聚物/蛋白质组合物，其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡聚体和至少一种包含至少一部分RNA诱导的沉默复合物（RISC）的蛋白质，其中至少一个核苷酸包含 嵌合有机组合物。

    Generation of virtual combinatorial libraries of compounds
    27.
    发明授权
    Generation of virtual combinatorial libraries of compounds 失效

    公开(公告)号：US06253168B1

    公开(公告)日：2001-06-26

    申请号：US09076405

    申请日：1998-05-12

    申请人： Richard Griffey ,  Eric Swayze

    发明人： Richard Griffey ,  Eric Swayze

    IPC分类号： G06G748

    CPC分类号： G06F19/709 ,  C40B50/02

    摘要： The present invention provides methods for the generation of virtual libraries of compounds. These compounds are generated in silico. The present invention encompasses methods for tracking the addition of fragments, use of reagents, and transformations performed. Further, methods for interfacing the information necessary to generate libraries of compounds with instrumentation that conducts the actual synthesis of the compounds are provided. Also provided are methods for the in silico docking of the library compounds to identified target molecules of interest.

    Oligomeric Compounds That Facilitate Risc Loading
    30.
    发明申请
    Oligomeric Compounds That Facilitate Risc Loading 审中-公开
    促进Risc加载的低分子化合物

    公开(公告)号：US20070275921A1

    公开(公告)日：2007-11-29

    申请号：US11569929

    申请日：2005-06-02

    申请人： Eric Swayze ,  Balkrishen Bhat ,  Richard Griffey ,  Thazha Prakash ,  Charles Allerson

    发明人： Eric Swayze ,  Balkrishen Bhat ,  Richard Griffey ,  Thazha Prakash ,  Charles Allerson

    IPC分类号： A61K31/7052 ,  A61P43/00 ,  C07H21/00

    CPC分类号： A61K31/7052

    摘要： The present invention provides double stranded compositions wherein one of the strands is useful in, for example, influencing the preferential loading the opposite strand into the RISC (or cleavage) complex. In particular, the present invention provides oligomeric compounds that comprise chemical modifications in at least one of the strands to drive loading of the opposite strand into the RISC (or cleavage) complex. Such modifications can be used to increase potency of duplex constructs that have been modified to enhance stability. Examples of chemical modifications that drive loading of the second strand include, but are not limited to, MOE (2′-O(CH2)2OCH3), 2′-O-methyl, -ethyl, -propyl, and —N-methylacetamide. Such modifications can be distributed throughout the strand, or placed at the 5′ and/or 3′ ends to make a gapmer motif on the sense strand. The activity of the 4′-thio gapmer RNA antisense strand can be improved by incorporating alternating MOE or MOE gapmer motif into the sense strand.

    摘要翻译： 本发明提供双链组合物，其中一条链可用于例如影响相对链优先加载到RISC（或切割）复合物中。 特别地，本发明提供了在至少一个链中包含化学修饰以驱动相反链加载到RISC（或切割）复合物中的低聚化合物。 可以使用这些修饰来增加经修饰以增强稳定性的双链构建体的效力。 驱动第二链的负载的化学修饰的实例包括但不限于MOE（2'-O（CH 2）2 OCH 3） ，2'-O-甲基， - 乙基， - 丙基和-N-甲基乙酰胺。 这样的修饰可以分布在整个链上，或者放置在5'和/或3'末端以在有义链上形成gapmer基序。 通过将交替的MOE或MOE gapmer基序并入有义链中，可以改善4'-硫代间隔RNA反义链的活性。