C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 309/10 (2006.01) A61K 31/351 (2006.01) A61P 3/10 (2006.01) C07C 215/90 (2006.01)
Patent
CA 2614545
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 2.theta.(~) 5.58, 14.72, 16.80, 17.82, 21.02 and 22.46 as measured by powder X ray diffraction. Thus, a crystal of an azulene compound can be produced which is in the form of a single crystal, has a fixed quality, can be produced with good reproducibility, can be provided stably as a crystal of an active substance for use in the preparation of a pharmaceutical and is excellent in storage stability.
L'invention concerne un cristal de sel de choline de (1S)-1,5-anhydro-1-[5-(azulèn-2-ylméthyl)-2-hydroxyphényl]-D-glucitol présentant un pic endothermique à une température comprise entre 194 °C et 198 °C sur la base d'une analyse calorimétrique différentielle (analyse ACD) et des pics principaux sur une échelle 2.theta.(°) à 5,58, 14, 72, 16,80, 17,82, 21,02 et 22,46 environ, sur la base d'une analyse par diffraction de rayons X sur poudres. L'invention permet ainsi de produire un cristal d'un composé d'azulène sous forme de monocristal, possédant une qualité fixe, pouvant être produit en série, fourni de façon stable sous forme de cristal d'une substance active, utilisé dans la préparation d'un produit pharmaceutique, et possédant une excellente stabilité de conservation.
Amenomiya Naoko
Awamura Yuuji
Imamura Masakazu
Murakami Takeshi
Nakamura Haruka
Astellas Pharma Inc.
Dennison Associates
Kotobuki Pharmaceutical Co. Ltd.
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