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    PHENYL PYRROLE DERIVATIVE CRYSTAL
    83.
    发明公开
    PHENYL PYRROLE DERIVATIVE CRYSTAL 审中-公开
    苯基吡咯衍生物晶体

    公开(公告)号：EP2703400A1

    公开(公告)日：2014-03-05

    申请号：EP12777084.0

    申请日：2012-04-26

    申请人： Daiichi Sankyo Company, Limited

    发明人： ONO, Makoto

    IPC分类号： C07D413/14 ,  A61K31/497 ,  A61P3/10

    CPC分类号： C07D413/14 ,  A61K31/497

    摘要： Provided is a monomethanesulfonate of a phenylpyrrole derivative, having superior glucokinase activating activity and demonstrating remarkably improved solubility, hygroscopicity and stability as well as superior oral absorption, and crystals thereof. The present invention provides (2S)-2-(3-{5-[(5S)-5-methyl-4,5-dihydro-1,3-oxazol-2-yl]-1H-pyrrol-2-yl}-5-{[5-(methylsulfonyl)pyrazin-2-yl]oxy}phenoxy)propan-1-ol monomethanesulfonate having superior glucokinase activating activity, crystals thereof, a pharmaceutical containing the same, and a preventive and/or therapeutic agent for diabetes and the like.

    摘要翻译： 本发明提供苯基吡咯衍生物的单甲磺酸盐，其具有优异的葡糖激酶活化活性，并显示出显着改善的溶解度，吸湿性和稳定性以及优异的口服吸收性及其晶体。 （2S）-2-（3- {5 - [（5S）-5-甲基-4,5-二氢-1,3-恶唑-2-基] -1H-吡咯-2-基} -5 - {[5-（甲基磺酰基）吡嗪-2-基]氧基}苯氧基）丙-1-醇单甲磺酸盐及其晶体，含有其的药物以及用于以下物质的预防和/或治疗剂 糖尿病等。

    AMINO GROUP-CONTAINING PYRROLIDINONE DERIVATIVE
    84.
    发明公开
    AMINO GROUP-CONTAINING PYRROLIDINONE DERIVATIVE 审中-公开
    氨基酸对苯二酚

    公开(公告)号：EP2674430A1

    公开(公告)日：2013-12-18

    申请号：EP12744844.7

    申请日：2012-02-06

    申请人： Daiichi Sankyo Company, Limited

    发明人： INAGAKI, Hiroaki ,  FUJISAWA, Tetsunori ,  ITOH, Masao ,  YOKOMIZO, Aki ,  TSUDA, Toshifumi ,  HIGUCHI, Saito ,  DAS, Biswajit ,  KATOCH, Rita ,  UPADHYAY, Dilip, J.

    IPC分类号： C07D413/14 ,  A61K31/538 ,  A61K31/5383 ,  A61P31/04 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00

    CPC分类号： C07D487/04 ,  A61K31/5383 ,  C07D241/44 ,  C07D265/36 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00 ,  Y02A50/475

    摘要： [Problems to be Solved by the Invention]
    To provide a drug having excellent antibacterial activity against Gram-positive bacteria and Gram-negative bacteria and also being excellent in terms of safety.
    [Means for Solving the Problems]
    A compound represented by the following formula (I) or a salt thereof:

    wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom
    m represents an integer 0, 1, or 2,
    n represents an integer 0 or 1
    Ar 1 represents a bicyclic heterocyclic group represented by the following formula:

    wherein A a represents a nitrogen atom or C-R a , A b represents a nitrogen atom or C-R b , and A c represents a nitrogen atom or C-R c , R a , R b , and R c independently represent a hydrogen atom or an alkyl group containing 1 to 6 carbon atoms,
    R 1 and R 2 independently represent a hydrogen atom, an alkoxy group containing 1 to 6 carbon atoms, a halogenoalkoxy group containing 1 to 6 carbon atoms, a halogen atom, or a cyano group,
    Ar 2 represents a bicyclic heterocyclic group represented by the following formulae:

    摘要翻译： 本发明要解决的问题提供对革兰氏阳性菌和革兰氏阴性细菌具有优异抗菌活性的药物，并且在安全性方面也是优异的。 解决问题的手段下述式（I）表示的化合物或其盐：其中R表示氢原子，羟基或卤素原子，m表示整数0,1或2，n表示 整数0或1 Ar 1表示由下式表示的双环杂环基：其中A a表示氮原子或CR a，A b表示氮原子或CR b，A c表示氮原子或CR c， R a，R b和R c独立地表示氢原子或含有1至6个碳原子的烷基，R 1和R 2独立地表示氢原子，含有1至6个碳原子的烷氧基，含卤素烷氧基 1至6个碳原子，卤素原子或氰基，Ar 2表示由下式表示的双环杂环基：