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    METHOD FOR PRODUCING C-GLYCOSIDE DERIVATIVE AND SYNTHETIC INTERMEDIATE THEREOF
    4.
    发明公开
    METHOD FOR PRODUCING C-GLYCOSIDE DERIVATIVE AND SYNTHETIC INTERMEDIATE THEREOF 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES C-GLYKOSIDDERIVATS UND SYNTHETISCHES ZWISCHENPRODUKTDAFÜR

    公开(公告)号：EP2105442A1

    公开(公告)日：2009-09-30

    申请号：EP07850951.0

    申请日：2007-12-20

    申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

    发明人： KOMENOI, Kousuke ,  NAKAMURA, Atsushi ,  KASAI, Makoto ,  IMAMURA, Masakazu ,  SHIRAKI, Ryota ,  NAKANISHI, Keita

    IPC分类号： C07D409/10 ,  A61K31/381 ,  A61P3/10 ,  C07D333/54

    CPC分类号： C07D409/10 ,  C07D333/54

    摘要： The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.

    摘要翻译： 本发明提供一种可以以高产率和低成本生产符合环境保护并且在工业上可应用的C-糖苷衍生物的方法。 C-糖苷衍生物可用于治疗和预防糖尿病如胰岛素依赖性糖尿病（1型糖尿病），非胰岛素依赖型糖尿病（2型糖尿病）等，以及各种糖尿病相关疾病，包括胰岛素抵抗性疾病和 肥胖。

    CHOLINE SALT CRYSTAL OF AZULENE COMPOUND
    5.
    发明公开
    CHOLINE SALT CRYSTAL OF AZULENE COMPOUND 审中-公开
    苯胺类化合物的CHOLINE盐晶体

    公开(公告)号：EP1908757A1

    公开(公告)日：2008-04-09

    申请号：EP06767927.4

    申请日：2006-07-06

    申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

    发明人： IMAMURA, Masakazu ,  SUZUKI, Takayuki ,  MURAKAMI, Takeshi ,  NAKANISHI, Keita ,  UEBAYASHI, Hiroshi ,  NAKAMURA, Haruka ,  YUDA, Masamichi ,  AMENOMIYA, Naoko ,  AWAMURA, Yuuji ,  TOMIYAMA, Hiroshi

    IPC分类号： C07D309/10 ,  A61K31/351 ,  A61P3/10 ,  C07C215/90

    CPC分类号： C07C215/90 ,  C07D309/10

    摘要： A choline salt crystal of (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-D-glucitol which shows an endothermic peak at 194 to 198°C as measured by differential scanning calorimetry (DSC analysis) and shows main peaks at about 2θ (°) 5.58, 14.72, 16.80, 17.82, 21.02, and 22.46 as measured by X-ray powder diffraction. Thus, a crystal of an azulene compound can be produced which is in a single crystal form, has a constant quality, can be produced with good reproducibility, can be provided stably as a crystal of an drug substance for use in the preparation of a pharmaceutical and is excellent in storage stability.

    摘要翻译： （1S）-1,5-脱水-1- [5-（甘菊环-2-基甲基）-2-羟基苯基] -D-葡萄糖醇的胆碱盐晶体在194〜198℃显示出吸热峰， 差示扫描量热法（DSC分析），并且显示通过X射线粉末衍射测量的在约2θ（°）5.58,14.72,16.80,17.82,21.02和22.46处的主峰。 因此，可以制造单晶形式的az化合物晶体，其具有恒定的品质，可以以良好的再现性生产，可以作为用于制备药物的药物晶体稳定地提供 储存稳定性优异。