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    Inhibitor for the formation of gamma-secretase complex
    1.
    发明授权
    Inhibitor for the formation of gamma-secretase complex 失效
    抑制剂形成γ-分泌酶复合物

    公开(公告)号：US08637274B2

    公开(公告)日：2014-01-28

    申请号：US12606792

    申请日：2009-10-27

    申请人： Yasuomi Urano ,  Takao Hamakubo ,  Tatsuhiko Kodama

    发明人： Yasuomi Urano ,  Takao Hamakubo ,  Tatsuhiko Kodama

    IPC分类号： C12N15/09

    CPC分类号： A61K31/22 ,  A61K31/366 ,  A61K31/401 ,  G01N2333/96425 ,  G01N2800/2821

    摘要： It is intended to provide an inhibitor for the formation of a γ-secretase complex which comprises a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator as the active ingredient; and use of a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator for producing the same. It is also intended to provide a method of screening a substance having an effect of inhibiting the formation of an active complex of γ-secretase which comprises assaying the activity of inhibiting cholesterol synthesis or quantifying cholesterol accumulated in lipid rafts in cells. It is also intended to provide a method of screening a cholesterol synthesis inhibitor, a protein geranylgeranylation regulator or an HMG-CoA reductase inhibitor which comprises assaying the effect of inhibiting the formation of an active complex of γ-secretase. Moreover, it is intended to provide a method of screening an effect of a test substance on γ-secretase which comprises measuring the distribution of constituents (niscastrin, APH-1, Pen-2 and so on) required by γ-secretase for the formation of its active complex in cells.

    摘要翻译： 旨在提供用于形成γ-分泌酶复合物的抑制剂，其包含胆固醇合成抑制剂或蛋白质香叶基香叶基化调节剂作为活性成分; 以及使用胆固醇合成抑制剂或蛋白质香叶基香叶基化调节剂来制备它们。 还旨在提供一种筛选具有抑制γ-分泌酶活性复合物形成的作用的物质的方法，其包括测定抑制胆固醇合成的活性或定量细胞中脂质筏中累积的胆固醇。 还旨在提供一种筛选胆固醇合成抑制剂，蛋白质香叶基香叶基调节剂或HMG-CoA还原酶抑制剂的方法，其包括测定抑制γ-分泌酶活性复合物形成的作用。 此外，旨在提供一种筛选测试物质对γ-分泌酶的作用的方法，其包括测量γ-分泌酶对于形成所需的成分（脑膜炎，APH-1，Pen-2等）的分布 其活性复合物在细胞中。

    Inhibitor for the Formation of Gamma-Secretase Complex
    2.
    发明申请
    Inhibitor for the Formation of Gamma-Secretase Complex 失效
    抑制剂形成γ-分泌酶复合物

    公开(公告)号：US20100093010A1

    公开(公告)日：2010-04-15

    申请号：US12606792

    申请日：2009-10-27

    申请人： Yasuomi Urano ,  Takao Hamakubo ,  Tatsuhiko Kodama

    发明人： Yasuomi Urano ,  Takao Hamakubo ,  Tatsuhiko Kodama

    IPC分类号： C12Q1/37 ,  C12Q1/25 ,  C12Q1/26

    CPC分类号： A61K31/22 ,  A61K31/366 ,  A61K31/401 ,  G01N2333/96425 ,  G01N2800/2821

    摘要： It is intended to provide an inhibitor for the formation of a γ-secretase complex which comprises a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator as the active ingredient; and use of a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator for producing the same. It is also intended to provide a method of screening a substance having an effect of inhibiting the formation of an active complex of γ-secretase which comprises assaying the activity of inhibiting cholesterol synthesis or quantifying cholesterol accumulated in lipid rafts in cells. It is also intended to provide a method of screening a cholesterol synthesis inhibitor, a protein geranylgeranylation regulator or an HMG-CoA reductase inhibitor which comprises assaying the effect of inhibiting the formation of an active complex of γ-secretase. Moreover, it is intended to provide a method of screening an effect of a test substance on γ-secretase which comprises measuring the distribution of constituents (niscastrin, APH-1, Pen-2 and so on) required by γ-secretase for the formation of its active complex in cells.

    摘要翻译： 旨在提供用于形成γ-分泌酶复合物的抑制剂，其包含胆固醇合成抑制剂或蛋白质香叶基香叶基化调节剂作为活性成分; 以及使用胆固醇合成抑制剂或蛋白质香叶基香叶基化调节剂来制备它们。 本发明还提供一种筛选具有抑制γ-分泌酶活性复合物形成的作用的物质的方法，该方法包括测定抑制胆固醇合成的活性或量化在细胞中积累的脂筏中的胆固醇。 本发明还旨在提供一种筛选胆固醇合成抑制剂，蛋白er牛儿基胆碱化调节剂或HMG-CoA还原酶抑制剂的方法，其包括测定抑制γ-分泌酶活性复合物形成的作用。 此外，旨在提供一种筛选测试物质对γ分泌酶的作用的方法，其包括测量γ-分泌酶对于形成所需的成分（脑膜炎，APH-1，Pen-2等）的分布 其活性复合物在细胞中。

    Inhibitor for the formation of y-secretase complex
    6.
    发明申请
    Inhibitor for the formation of y-secretase complex 审中-公开
    抑制剂形成γ-分泌酶复合物

    公开(公告)号：US20070161700A1

    公开(公告)日：2007-07-12

    申请号：US10584415

    申请日：2004-12-28

    申请人： Yasuomi Urano ,  Takao Hamakubo ,  Tatsuhiko Kodama

    发明人： Yasuomi Urano ,  Takao Hamakubo ,  Tatsuhiko Kodama

    IPC分类号： A61K31/401 ,  A61K31/366 ,  A61K31/22

    CPC分类号： A61K31/22 ,  A61K31/366 ,  A61K31/401 ,  G01N2333/96425 ,  G01N2800/2821

    摘要： It is intended to provide an inhibitor for the formation of a γ-secretase complex which comprises a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator as the active ingredient; and use of a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator for producing the same. It is also intended to provide a method of screening a substance having an effect of inhibiting the formation of an active complex of γ-secretase which comprises assaying the activity of inhibiting cholesterol synthesis or quantifying cholesterol accumulated in lipid rafts in cells. It is also intended to provide a method of screening a cholesterol synthesis inhibitor, a protein geranylgeranylation regulator or an HMG-CoA reductase inhibitor which comprises assaying the effect of inhibiting the formation of an active complex of γ-secretase. Moreover, it is intended to provide a method of screening an effect of a test substance on γ-secretase which comprises measuring the distribution of constituents (niscastrin, APH-1, Pen-2 and so on) required by γ-secretase for the formation of its active complex in cells.

    摘要翻译： 旨在提供用于形成γ-分泌酶复合物的抑制剂，其包含胆固醇合成抑制剂或蛋白质香叶基香叶基化调节剂作为活性成分; 以及使用胆固醇合成抑制剂或蛋白质香叶基香叶基化调节剂来制备它们。 还旨在提供一种筛选具有抑制γ-分泌酶活性复合物形成的作用的物质的方法，其包括测定抑制胆固醇合成的活性或定量细胞中脂质筏中累积的胆固醇。 还旨在提供一种筛选胆固醇合成抑制剂，蛋白质香叶基香叶基调节剂或HMG-CoA还原酶抑制剂的方法，其包括测定抑制γ-分泌酶活性复合物形成的作用。 此外，旨在提供一种筛选测试物质对γ-分泌酶的作用的方法，其包括测量γ-分泌酶对于形成所需的成分（脑膜炎，APH-1，Pen-2等）的分布 其活性复合物在细胞中。

    PTX3-GENE EXPRESSION INHIBITOR
    8.
    发明申请
    PTX3-GENE EXPRESSION INHIBITOR 审中-公开
    PTX3基因表达抑制剂

    公开(公告)号：US20080161348A1

    公开(公告)日：2008-07-03

    申请号：US11694288

    申请日：2007-03-30

    申请人： Shigeru MORIKAWA ,  Akashi Izumi ,  Takao Hamakubo ,  Tatsuhiko Kodama

    发明人： Shigeru MORIKAWA ,  Akashi Izumi ,  Takao Hamakubo ,  Tatsuhiko Kodama

    IPC分类号： A61K31/695 ,  A61K31/47

    CPC分类号： A61K31/404 ,  A61K31/22 ,  A61K31/365 ,  A61K31/40

    摘要： A method for suppressing expression of PTX3 gene, which comprises administering an effective amount of a compound, which is represented by the following formula (1): wherein R1 represents an organic group, X represents —CH2CH2— or —CH═CH—, and R2 represents a hydrogen atom or an alkyl group, or a lactone derivative thereof, or a salt thereof.According to the present invention, a PTX3 gene expression suppressing method useful for the treatment of autoimmune diseases, especially rheumatoid arthritis can be provided.

    摘要翻译： 一种抑制PTX3基因表达的方法，其包括给予有效量的由下式（1）表示的化合物：其中R 1表示有机基团，X表示-CH 2或2-CH 2 - 或-CH-CH-，R 2表示氢原子或烷基或其内酯衍生物， 或其盐。 根据本发明，可以提供用于治疗自身免疫性疾病，特别是类风湿性关节炎的PTX3基因表达抑制方法。