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12 条记录 (耗时 0.017 秒)

    Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate
    7.
    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。

    SUSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR USE THEREOF
    8.
    发明申请
    SUSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR USE THEREOF 审中-公开
    2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚，其使用方法

    公开(公告)号：US20130217703A1

    公开(公告)日：2013-08-22

    申请号：US13844825

    申请日：2013-03-16

    申请人： Alla Chem, LLC

    发明人： Alexandre Vasilievich IVACHTCHENKO ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko

    IPC分类号： C07D471/04

    CPC分类号： A61K31/437 ,  A61K31/444 ,  C07D471/04

    摘要： The present invention relates to a method of antagonizing a 5-HT6 serotonin receptor and simultaneously regulating Ca+2 ion homeostasis in a cell, comprising administering to the cell a compound of formula 1, or a pharmaceutically acceptable salt thereof, wherein: R1 is a C1-C5 alkyl; R2i is independently hydrogen, halogen, a C1-C3 alkyl, CF3, OCF3 or OCH3; i is 1, 2, 3 or 4; Ar is an unsubstituted phenyl or a substituted phenyl substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle with one or two nitrogen atoms in the heterocycle; and W is an ethylene group —CH2—CH2—, ethenyl group —CH═CH—, or ethynyl group —C≡C—. The invention also relates to new compounds selected from the group of compounds of the general formula 1, method for their preparation, pharmaceutical compositions and method for treating a cognitive disorder or neurodegenerative disease, or obesity in a subject in need thereof comprising administering an effective dose to the subject of a compound of formula 1 according to claim 1, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及一种拮抗5-HT 6 5-羟色胺受体并同时调节细胞中Ca 2+离子稳态的方法，包括向细胞施用式1化合物或其药学上可接受的盐，其中：R1为 C1-C5烷基; R2i独立地是氢，卤素，C1-C3烷基，CF3，OCF3或OCH3; 我是1，2，3或4; Ar是未取代的苯基或被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，取代的氨基或三氟甲基取代的取代的苯基; 或Ar是在杂环中具有一个或两个氮原子的取代或未取代的6元芳族杂环; W是亚乙基-CH 2 -CH 2 - ，乙烯基-CH = CH-或乙炔基-C = C-。 本发明还涉及选自通式1的化合物，其制备方法，用于治疗有需要的受试者的认知障碍或神经变性疾病或肥胖症的药物组合物和方法的新化合物，其包括施用有效剂量 涉及根据权利要求1的式1化合物或其药学上可接受的盐的主题。

    Pharmaceutical composition having improved flowability, medicinal agent, and method for producing and using same
    10.
    发明授权
    Pharmaceutical composition having improved flowability, medicinal agent, and method for producing and using same 有权
    具有改善的流动性的药物组合物，药剂及其制备和使用方法

    公开(公告)号：US09370576B2

    公开(公告)日：2016-06-21

    申请号：US14410584

    申请日：2013-07-05

    申请人： Alexandre Vasilievich Ivachtchenko ,  ALLA CHEM, LLC

    发明人： Alexandre Vasilievich Ivachtchenko ,  Alexandre Viktorovich Demin

    IPC分类号： A61K47/36 ,  A61K47/32 ,  A61K47/10 ,  A61K31/135 ,  A61K9/48 ,  A61J3/07

    CPC分类号： A61K47/36 ,  A61J3/074 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/135 ,  A61K47/10 ,  A61K47/32

    摘要： The invention relates to the field of pharmaceutics, in particular, to solid pharmaceutical composition comprising 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or pharmaceutically acceptable salt thereof, stabilizer, lubricant and filler; to method for preparation of pharmaceutical composition, to medicaments for immune suppression and treating multiple sclerosis. 2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol represents an immune modulator, which causes redistribution of lymphocytes from blood flow into secondary lymphoid tissue that leads to immune suppression. The invention provides uniform distribution of the active ingredient in the solid composition, high stability and improved flowability of the solid pharmaceutical composition. Due to the improved flowability the compositions suggested in the invention can be used on automated equipment.

    摘要翻译： 本发明涉及药物领域，特别涉及包含2-氨基-2- [2-（4-辛基苯基）乙基]丙烷-1,3-二醇或其药学上可接受的盐，稳定剂，润滑剂和 填料; 制备药物组合物的方法，用于免疫抑制和治疗多发性硬化症的药物。 2-氨基-2- [2-（4-辛基苯基）乙基]丙烷-1,3-二醇代表免疫调节剂，其引起淋巴细胞从血流重新分布到次级淋巴组织中，导致免疫抑制。 本发明提供固体组合物中活性成分的均匀分布，固体药物组合物的高稳定性和改善的流动性。 由于改进的流动性，本发明中提出的组合物可用于自动化设备。