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    Method of screening insulin content enhancer
    1.
    发明申请
    Method of screening insulin content enhancer 审中-公开
    筛选胰岛素含量增强剂的方法

    公开(公告)号：US20050191612A1

    公开(公告)日：2005-09-01

    申请号：US10511549

    申请日：2003-09-10

    申请人： Takahide Ohishi ,  Tomonobu Koizumi

    发明人： Takahide Ohishi ,  Tomonobu Koizumi

    IPC分类号： A61P3/10 ,  C07K14/72 ,  G01N33/50 ,  G01N33/74 ,  C12Q1/00 ,  A61K38/28

    CPC分类号： G01N33/5008 ,  C07K14/723 ,  G01N33/502 ,  G01N33/5023 ,  G01N33/507 ,  G01N2333/726

    摘要： A screening tool for an agent for promoting insulin production and/or an agent for increasing insulin content, wherein the tool is a G protein-coupled receptor exhibiting an activity of promoting insulin production by activation, or a cell expressing the polypeptide, is disclosed. Further, a method for screening an agent for promoting insulin production and/or an agent for increasing insulin content, comprising the steps of bringing the cell or a cell membrane thereof into contact with a substance to be tested, and analyzing whether or not the polypeptide is activated, is disclosed. The screening tool and the screening method are useful in screening a substance which increases insulin content and prevents and/or treats diabetes. Furthermore, a novel agent for increasing insulin content comprising as an active ingredient a substance obtained by the screening, is disclosed.

    摘要翻译： 公开了用于促进胰岛素生成的试剂和/或增加胰岛素含量的试剂的筛选工具，其中该工具是表现出通过活化促进胰岛素产生的活性的G蛋白偶联受体或表达该多肽的细胞。 另外，用于筛选促进胰岛素生成的试剂的方法和/或用于增加胰岛素含量的试剂的方法，包括使细胞或其细胞膜与被检物质接触的步骤，以及分析多肽 被激活。 筛选工具和筛选方法可用于筛选增加胰岛素含量并预防和/或治疗糖尿病的物质。 此外，公开了一种用于增加胰岛素含量的新型药剂，其包含通过筛选获得的物质作为活性成分。

    Method for screening agents for the treatment of diabetes
    2.
    发明授权
    Method for screening agents for the treatment of diabetes 有权
    用于治疗糖尿病的筛选剂的方法

    公开(公告)号：US07662775B2

    公开(公告)日：2010-02-16

    申请号：US10975367

    申请日：2004-10-29

    申请人： Takahide Ohishi ,  Jun Takasaki ,  Mitsuyuki Matsumoto ,  Tetsu Saito ,  Masazumi Kamohara ,  Takatoshi Soga

    发明人： Takahide Ohishi ,  Jun Takasaki ,  Mitsuyuki Matsumoto ,  Tetsu Saito ,  Masazumi Kamohara ,  Takatoshi Soga

    IPC分类号： A61K38/00 ,  A61K51/00 ,  C07K1/00 ,  C07K14/00

    CPC分类号： C07K14/705 ,  A61K38/00 ,  C07K14/723

    摘要： The invention relates to a convenient screening tool for identifying an agent for treating diabetes. The screening tool is a G protein-coupled receptor, a variant of the G protein-coupled receptor, or a homolog of the G protein-coupled receptor, which promotes insulin secretion under a high glucose concentration by activation. The invention also relates to cells transformed with an expression vector comprising a polynucleotide encoding and expressing the screening tool. The invention provides a convenient screening method for identifying an agent for treating diabetes, pharmaceutical compositions comprising the agent, and a process for manufacturing the pharmaceutical composition.

    摘要翻译： 本发明涉及用于鉴定用于治疗糖尿病的药剂的方便的筛选工具。 筛选工具是G蛋白偶联受体，G蛋白偶联受体的变体或G蛋白偶联受体的同系物，其通过活化促进高葡萄糖浓度下的胰岛素分泌。 本发明还涉及用包含编码和表达筛选工具的多核苷酸的表达载体转化的细胞。 本发明提供了用于鉴定用于治疗糖尿病的药剂的方便的筛选方法，包含该药剂的药物组合物和用于制备该药物组合物的方法。

    Pyrimidine derivative condensed with a non-aromatic ring
    7.
    发明授权
    Pyrimidine derivative condensed with a non-aromatic ring 失效
    与非芳香环稠合的嘧啶衍生物

    公开(公告)号：US07947690B2

    公开(公告)日：2011-05-24

    申请号：US11577648

    申请日：2005-10-17

    申请人： Yasuhiro Yonetoku ,  Kenji Negoro ,  Kenichi Onda ,  Masahiko Hayakawa ,  Daisuke Sasuga ,  Takahiro Nigawara ,  Kazuhiko Iikubo ,  Hiroyuki Moritomo ,  Shigeru Yoshida ,  Takahide Ohishi

    发明人： Yasuhiro Yonetoku ,  Kenji Negoro ,  Kenichi Onda ,  Masahiko Hayakawa ,  Daisuke Sasuga ,  Takahiro Nigawara ,  Kazuhiko Iikubo ,  Hiroyuki Moritomo ,  Shigeru Yoshida ,  Takahide Ohishi

    IPC分类号： A61K31/519 ,  A61K31/497 ,  C07D495/04 ,  A61P3/10 ,  C07D487/04 ,  C07D471/04 ,  C07D239/72 ,  A61K31/517

    CPC分类号： C07D239/70 ,  C07D239/94 ,  C07D495/04

    摘要： The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.

    摘要翻译： 本发明提供由式（I）表示的稠合嘧啶化合物或其药学上可接受的盐：其中A表示环，其中所述环中至少一个碳原子任选被一个或多个选自以下的基团取代：低级烷基 ，-O-（低级烷基），卤素原子，羧基，-CO 2 - （低级烷基）和氨基甲酰基，R 1表示：（1）被至少三个卤素原子取代的苯基，其可以具有至少一个另外的取代基，或 （2）环丙基，环丁基，环戊基，环己基或环庚基，其各自任选被取代; 并且R 2表示由式（II）表示的基团或任选取代的环状氨基：其中R 21和R 22可以相同或不同，并且各自表示-H，低级烷基，低级烯基，低级炔基，环烷基，苯基，杂芳基， 芳族杂环基或-O-（低级烷基），其各自任选被取代。