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    Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate
    31.
    发明授权
    Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate 有权
    取代的（S） - （2R，3R，5R）-3-羟基 - （5-嘧啶-1-基）四氢呋喃-2-基甲基芳基氨基磷酸酯

    公开(公告)号：US08889701B1

    公开(公告)日：2014-11-18

    申请号：US14051464

    申请日：2013-10-11

    申请人： Alla Chem, LLC

    发明人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Oleg Dmitrievich Mitkin

    IPC分类号： A01N43/54 ,  A61K31/505 ,  A61K45/06 ,  C07F9/6558 ,  A61K31/695 ,  A61K31/675

    CPC分类号： C07F9/65586 ,  A61K31/665 ,  A61K31/675 ,  A61K31/695 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  C07H19/067 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/393 ,  A61K2300/00

    摘要： The instant invention relates to a novel compound representing a substituted phosphoramidic acid—a (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 1 or a (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 2, or a pharmaceutically acceptable salt, a hydrate, a crystalline form or a stereoisomer thereof, as defined in the specification.The novel compound is used for a pharmaceutical composition with at least one pharmaceutically acceptable excipient as well as with an inosine 5 monophosphate dehydrogenase inhibitor, HCV protease NS3 inhibitor, HCV protease NS3/4A inhibitor, and RNA polymerase NS5A inhibitor. The novel compound is useful as a viral polymerase HCV NS5B inhibitor and can be used for treating a disease caused by hepatitis C virus (HCV).

    摘要翻译： 本发明涉及表示式1的取代的氨基磷酸-a（2R，3R，5R）-3-羟基 - （5-嘧啶-1-基）四氢呋喃-2-基）甲基芳基氨基磷酸酯的新化合物或 （2）的（S） - （2R，3R，5R）-3-羟基 - （5-嘧啶-1-基）四氢呋喃-2-基）甲基芳基氨基磷酸酯，或其药学上可接受的盐，水合物， 或其立体异构体，如说明书中所定义。 该新化合物用于具有至少一种药学上可接受的赋形剂以及肌苷5单磷酸脱氢酶抑制剂，HCV蛋白酶NS3抑制剂，HCV蛋白酶NS3 / 4A抑制剂和RNA聚合酶NS5A抑制剂的药物组合物。 该新型化合物可用作病毒聚合酶HCV NS5B抑制剂，可用于治疗丙型肝炎病毒（HCV）引起的疾病。

    NON-NATURAL MIC PROTEINS
    32.
    发明申请
    NON-NATURAL MIC PROTEINS 有权
    非天然麦芽糖蛋白

    公开(公告)号：US20140302072A1

    公开(公告)日：2014-10-09

    申请号：US14311130

    申请日：2014-06-20

    申请人： David W. MARTIN, JR. ,  Steven R. Williams

    发明人： David W. MARTIN, JR. ,  Steven R. Williams

    IPC分类号： C07K14/47

    CPC分类号： C07K14/473 ,  A61K38/00 ,  C07K14/70539 ,  C07K2318/00 ,  C07K2319/33 ,  Y02A50/389 ,  Y02A50/393

    摘要： This invention describes soluble, monovalent, non-natural protein molecules that can activate NK cells and certain T-cells to attack specific cellular target cells by attaching the NKG2D-binding portions of monovalent MICA or MICB protein, i.e. their α1-α2 platform domain, to the intended target cell specifically. The α1-α2 domain is contiguous with a heterologous α3 domain that has been genetically modified to bind directly or indirectly to the extracellular aspect of the target cell, thereby serving as the targeting domain. The genetic modification to create a non-natural and non-terminal targeting motif within the α3 domain can include a portion of an antibody, another protein molecule or portion thereof, a peptide, or a non-natural, modified α3 domain of a MIC protein.

    摘要翻译： 本发明描述了通过连接单价MICA或MICB蛋白（即它们的α1-α2平台结构域）的NKG2D结合部分可以激活NK细胞和某些T细胞以攻击特异性细胞靶细胞的可溶性，一价，非天然蛋白质分子， 具体到目的细胞。 α1-α2结构域与已经被遗传修饰的异源α3结构域连续，直接或间接地结合到靶细胞的细胞外方面，从而作为靶向结构域。 在α3结构域内产生非天然和非末端靶向基序的遗传修饰可以包括MIC蛋白质的一部分抗体，另一蛋白质分子或其部分，肽或非天然修饰的α3结构域 。

    COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES
    35.
    发明申请
    COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES 有权
    用于治疗病毒的组合物和方法

    公开(公告)号：US20140249178A1

    公开(公告)日：2014-09-04

    申请号：US14240583

    申请日：2012-08-23

    申请人： Eliezer Huberman

    发明人： Eliezer Huberman

    IPC分类号： A61K31/437

    CPC分类号： A61K31/437 ,  A61K31/44 ,  Y02A50/385 ,  Y02A50/393

    摘要： Substituted perhydro pyrrolopyridines and methods for their use in the treatment of HIV infections, AIDS, and AIDS-related diseases, and in the treatment of BVDV infections are described herein. Also, pharmaceutical compositions comprising the substituted perhydro pyrrolopyridines are useful for the treatment of HIV infections, AIDS, and AIDS-related diseases. The compositions include one or more carriers, diluents, or excipients, or a combination thereof.

    摘要翻译： 本文描述了取代的全氢吡咯并吡啶及其用于治疗HIV感染，AIDS和AIDS相关疾病以及用于治疗BVDV感染的方法。 此外，包含取代的全氟吡咯并吡啶的药物组合物可用于治疗HIV感染，AIDS和AIDS相关疾病。 组合物包括一种或多种载体，稀释剂或赋形剂，或其组合。

    3,7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE
    36.
    发明申请
    3,7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE 有权
    3,7-DIAMINO-10H-PHENOTHIAZINE SALTS及其使用

    公开(公告)号：US20140221359A1

    公开(公告)日：2014-08-07

    申请号：US14248730

    申请日：2014-04-09

    申请人： Wis Ta Laboratories Ltd.

    发明人： Claude Michel WISCHIK ,  Janet Elizabeth Rickard ,  Charles Robert Harrington ,  David Horsley ,  John Mervyn David Storey ,  Colin Marshall ,  James Peter Sinclair ,  Thomas Craven Baddeley

    IPC分类号： C07D279/20

    CPC分类号： C07D279/20 ,  A61K31/5415 ,  A61K49/0002 ,  A61K49/003 ,  A61K51/0465 ,  G01N33/6896 ,  G01N2800/2835 ,  Y02A50/393 ,  Y02A50/411

    摘要： Described are methods of prepraing reduced 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of formula: wherein: R1 and R9 are independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of HX1 and HX2 is independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These methods are particularly useful for producing stable reduced forms, and with high purity. The stability and purity are especially relevant for pharmaceutical compositions for the treatment of disease. The compounds are useful for treatment of e.g. tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs.

    摘要翻译： 描述了制备下式的还原的3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物的方法：其中：R 1和R 9独立地选自：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4烷基; R3NA和R3NB中的每一个独立地选自：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4烷基; R7NA和R7NB中的每一个独立地选自：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4烷基; HX1和HX2各自独立地是质子酸; 及其药学上可接受的盐，溶剂化物和水合物。 这些方法对于生产稳定的还原形式和高纯度特别有用。 稳定性和纯度与治疗疾病的药物组合物特别相关。 该化合物可用于治疗例如 tau病，如阿尔茨海默病，以及相应的氧化型硫堇药物的前药。