公开(公告)号：EP2042498A1

公开(公告)日：2009-04-01

申请号：EP07790741.8

申请日：2007-07-13

申请人： Astellas Pharma Inc.

发明人： HAMADA, Noritaka ,  MIZOGUCHI, Ryo ,  SANO, Kuniyuki ,  SAKAIDA, Takaaki ,  AWAMURA, Yuji ,  IWAKAWA, Yu ,  TOBE, Takahiko ,  SUGANE, Takashi

IPC分类号： C07D401/14 ,  A61K31/4439 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D413/14

摘要： Object
Provided are β-form crystal, γ-form crystal, and α-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance.
Means for Resolution
A solving means includes β-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150°C according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2θ(°), and the like. Selected Figure

摘要翻译： 提供的对象为苯并恶二唑衍生物的β型晶体，γ型晶体和α型晶体，其中可以以高重复性获得具有足够品质的均匀晶体，并且它们可以随时作为药物晶体供应使用 在制造医药品时，特别适用于工业生产中的大量合成，几乎不显示吸湿性并且具有特别优异的耐光性。 解决方案的手段解决手段包括4- [3-异丙基-5-（6-苯基-3-吡啶基）-4H-1,2,4-三唑-4-基] -2,1-二甲基 - 3-苯并恶二唑根据差示扫描量热计分析（DSC分析）在145至150℃显示吸热峰，并显示在9.8,11.1,12.8,13.3,17.1,20.2,21.2和22.3处的X射线粉末衍射峰 2θ（°）等。 选定图