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。