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    Pyrimidine derivative condensed with a non-aromatic ring
    4.
    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。

    OXADIAZOLIDINEDIONE COMPOUND
    8.
    发明申请
    OXADIAZOLIDINEDIONE COMPOUND 审中-公开
    氧化杂环化合物

    公开(公告)号：US20100267775A1

    公开(公告)日：2010-10-21

    申请号：US12739501

    申请日：2008-10-22

    申请人： Kenji Negoro ,  Fumiyoshi Iwasaki ,  Kei Ohnuki ,  Toshio Kurosaki ,  Kazuyuki Tsuchiya ,  Kazuyuki Kuramoto ,  Shigeru Yoshida ,  Takatoshi Soga

    发明人： Kenji Negoro ,  Fumiyoshi Iwasaki ,  Kei Ohnuki ,  Toshio Kurosaki ,  Kazuyuki Tsuchiya ,  Kazuyuki Kuramoto ,  Shigeru Yoshida ,  Takatoshi Soga

    IPC分类号： A61K31/4439 ,  C07D271/07 ,  A61K31/4245 ,  A61P3/10 ,  C07D413/12

    CPC分类号： C07D271/06 ,  C07D271/07 ,  C07D413/12

    摘要： A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.

    摘要翻译： 具有GPR40受体激动作用的药剂，特别是可用作胰岛素促分泌剂的化合物或用于预防和/或治疗糖尿病的药剂。 本发明人已经研究了具有GPR40受体激动作用的化合物，证实了通过2-位的连接基与诸如苯基等取代基连接的具有苄基等取代基的恶二唑烷二酮化合物等 的恶二唑烷二酮环或其药学上可接受的盐具有优异的GPR40激动活性，从而完成了本发明。 恶二唑烷二酮化合物具有优异的胰岛素促分泌作用和抗高血糖作用，因此可用作胰岛素促分泌素或预防和/或治疗糖尿病的药剂。

    Oxadiazolidinedione Compound
    10.
    发明申请
    Oxadiazolidinedione Compound 有权
    恶二唑烷二酮化合物

    公开(公告)号：US20090186909A1

    公开(公告)日：2009-07-23

    申请号：US12298522

    申请日：2007-04-23

    申请人： Kenji Negoro ,  Fumiyoshi Iwasaki ,  Kei Ohnuki ,  Toshio Kurosaki ,  Yasuhiro Yonetoku ,  Norio Asai ,  Shigeru Yoshida ,  Takatoshi Soga

    发明人： Kenji Negoro ,  Fumiyoshi Iwasaki ,  Kei Ohnuki ,  Toshio Kurosaki ,  Yasuhiro Yonetoku ,  Norio Asai ,  Shigeru Yoshida ,  Takatoshi Soga

    IPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/4245 ,  C07D413/12 ,  C07D271/07

    CPC分类号： C07D271/06 ,  C07D271/07 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided.[Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.

    摘要翻译： 可以提供可用作药物的化合物，特别是胰岛素分泌促进剂或用于预防/治疗其中涉及GPR40的疾病如糖尿病等的化合物。 [解决方法]已经发现，恶二唑烷二酮化合物或其药学上可接受的盐，其特征在于具有通过在恶二唑烷二酮环的2位上的连接基与环状基团结合的苄基等取代基， 具有优异的GPR40激动作用。 此外，由于本发明的恶二唑烷二酮化合物显示出优异的胰岛素分泌促进作用和血糖降低作用，因此可用作胰岛素分泌促进剂或糖尿病的预防/治疗剂。