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    Process for producing thiophene compound and intermediate thereof
    1.
    发明授权
    Process for producing thiophene compound and intermediate thereof 有权
    制备噻吩化合物及其中间体的方法

    公开(公告)号：US08399685B2

    公开(公告)日：2013-03-19

    申请号：US12919394

    申请日：2009-02-27

    申请人： Kazufumi Yanagihara ,  Shingo Umezawa ,  Katsuaki Miyaji

    发明人： Kazufumi Yanagihara ,  Shingo Umezawa ,  Katsuaki Miyaji

    IPC分类号： C07D333/32

    CPC分类号： C07D333/32 ,  C07C319/14 ,  C07C327/32 ,  C07C323/56

    摘要： To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals.A 2-aryl acetate compound represented by the formula (1): wherein R1 is an aryl group or the like, R4 is a C1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

    摘要翻译： 提供一种生产2-芳基-3-羟基-4-取代的羰基噻吩化合物或其中间体的新方法，其用作制备药物和农药的中间体。 由式（1）表示的2-芳基乙酸酯化合物：其中R 1为芳基等，R 4为C 1-3烷基等，X为离去基，与硫代乙酸化合物 为了形成硫代乙酰基化合物（3），硫代乙酰基化合物（3）与乙烯基酮化合物反应形成γ-酮硫醚化合物（5），其在碱性条件下环化形成二氢噻吩化合物（6），并且 二氢噻吩化合物（6）通过使用氧化剂氧化，得到2-芳基-3-羟基-4-取代的羰基噻吩化合物（7）。

    Pyrazolone compounds and thrombopoietin receptor activator
    6.
    发明授权
    Pyrazolone compounds and thrombopoietin receptor activator 失效
    吡唑啉酮化合物和血小板生成素受体激活剂

    公开(公告)号：US08053453B2

    公开(公告)日：2011-11-08

    申请号：US10530482

    申请日：2003-10-09

    申请人： Katsuaki Miyaji ,  Norihisa Ishiwata ,  Takanori Nakamura

    发明人： Katsuaki Miyaji ,  Norihisa Ishiwata ,  Takanori Nakamura

    IPC分类号： A61K31/416 ,  A61K31/4152 ,  C07D231/36

    CPC分类号： C07D231/26

    摘要： A preventive, therapeutic or improving agent for diseases against which activation of the thrombopoietin receptor is effective or a platelet increasing agent, which contains a thrombopoietin receptor activator represented by the formula (1): wherein A is a C?2-14#191 aryl group, B is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, D is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, and E is a C?2-14#191 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the activator or a solvate thereof, as an active ingredient.

    摘要翻译： 含有血小板生成素受体活化剂的有效的血栓生成素受体有效的疾病或血小板增多剂的预防，治疗或改善剂，其含有由式（1）表示的血小板生成素受体激活剂：其中A为C 2-14-1491芳基 基团，B为氢原子，C 1-6 1-6烷基，被一个或多个氟原子取代的C 1-3-3＃191烷基或C 2-14-1419芳基，D为 氢原子，C 1-6 1-6烷基，被一个或多个氟原子取代的C 1-3-3＃191烷基或C 2-14-1419芳基，E是C 1〜 2-14＃191芳基，活化剂的互变异构体，前药或药学上可接受的盐作为活性成分。