NA CHANNELS, DISEASE, AND RELATED ASSAYS AND COMPOSITIONS
    2.
    发明申请
    NA CHANNELS, DISEASE, AND RELATED ASSAYS AND COMPOSITIONS 有权
    NA通道,疾病和相关测定和组合物

    公开(公告)号:US20110230442A1

    公开(公告)日:2011-09-22

    申请号:US13059182

    申请日:2009-08-17

    CPC classification number: A61K31/4164 C07D209/14 C07D233/72 C07D317/26

    Abstract: Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.

    Abstract translation: 公开了分子及其合成,用于阻断门控离子通道如电压门控钠通道(VGSC)和前列腺电压钠通道(PVSC)。 这些抑制剂具有优异的阻断效能,例如置换与VGSC的位点2结合的放射性配体[3 H] -Batrachotoxin-B([3 H] -BTX-B)。 本发明的分子包含增加前列腺癌细胞(PC)中蛋白质结合位点的分子的结合亲和力的部分,其也是荧光的。 在一个实施方案中,本发明分子是可用于在疼痛,癫痫或前列腺癌中选择性地靶向过量或过度活跃的VGSC的抑制系统,从而抑制PC的​​增殖。 荧光部分还有助于药物在体外和体内生物系统中的筛选,跟踪和药效学研究。

    Na channels, disease, and related assays and compositions
    4.
    发明授权
    Na channels, disease, and related assays and compositions 有权
    Na通道,疾病和相关测定法和组合物

    公开(公告)号:US08816095B2

    公开(公告)日:2014-08-26

    申请号:US13059182

    申请日:2009-08-17

    CPC classification number: A61K31/4164 C07D209/14 C07D233/72 C07D317/26

    Abstract: Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.

    Abstract translation: 公开了分子及其合成,用于阻断门控离子通道如电压门控钠通道(VGSC)和前列腺电压钠通道(PVSC)。 这些抑制剂具有优异的阻断效能,例如置换与VGSC的位点2结合的放射性配体[3 H] -Batrachotoxin-B([3 H] -BTX-B)。 本发明的分子包含增加前列腺癌细胞(PC)中蛋白质结合位点的分子的结合亲和力的部分,其也是荧光的。 在一个实施方案中,本发明分子是可用于在疼痛,癫痫或前列腺癌中选择性地靶向过量或过度活跃的VGSC的抑制系统,从而抑制PC的​​增殖。 荧光部分还有助于药物在体外和体内生物系统中的筛选,跟踪和药效学研究。

    Storage and retrieval of richly typed hierarchical network models
    6.
    发明申请
    Storage and retrieval of richly typed hierarchical network models 有权
    丰富型分层网络模型的存储和检索

    公开(公告)号:US20070050399A1

    公开(公告)日:2007-03-01

    申请号:US11506665

    申请日:2006-08-18

    CPC classification number: G06F17/30607

    Abstract: A Composite Pattern with BLOB data types is used to model a hierarchical network, and includes a path-like construct for locating each component within the network model. Database procedures are used to efficiently search, modify and retrieve individual nodes from the network model using the database server's memory pool so that client applications are not required to retrieve and deserialize the entire Composite-BLOB hierarchy in order to make modifications or search for individual elements, thereby substantially reducing the transfer of data between the application layer and database. To avoid the need for dynamic memory restructuring during deserialization, the size required to store component data at each composite is stored when the composite is serialized, and during deserialization, the size is retrieved and used to obtain sufficient memory for the deserialized composite.

    Abstract translation: 具有BLOB数据类型的复合模式用于对分层网络建模,并且包括用于定位网络模型中的每个组件的路径样构造。 数据库过程用于使用数据库服务器的内存池从网络模型中有效地搜索,修改和检索单个节点,以便客户端应用程序不需要检索和反序列化整个Composite-BLOB层次结构,以便修改或搜索单个元素 ,从而显着减少应用层和数据库之间的数据传输。 为了避免在反序列化过程中需要动态内存重组,在复合数据序列化时存储每个复合数据组件数据所需的大小,在反序列化过程中,将检索大小并获取足够的反序列化复合存储空间。

Patent Agency Ranking