C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 277/34 (2006.01) A61K 31/426 (2006.01)
Patent
CA 2351727
The invention relates to type A crystal of 5-[{6-(2-fluorobenzyl)oxy-2- naphthyl}methyl]-2,4-thiazolidinedione characterized to have characteristic absorption peaks (2.theta.) at 11.5°~0.3°, 14.5°~0.2°, 16.2°~0.3°, 17.0°~0.3°, 17.7°~0.2°, 18.6°~0.3°, 19.1°~0.2°, 21.3°~0.4°, 22.4°~0.5°, 25.7°~0.5° and 28.3°~0.5° in a powder X-ray diffraction pattern, and also to a method for preparation thereof, and a pharmaceutical composition comprising the same. The crystal is excellent in stability, and has advantages in handling, storage, and pharmaceutical preparation. The invention also relates to type B, C and D crystals of said compound.
L'invention concerne un cristal de type A de 5-[{6-(2-fluorobenzyl)oxy-2-naphthyl}méthyl]-2,4-thiazolidinedione caractérisé par des pics d'absorption typiques de (2 theta ) à 11,5 DEG +/-0,3 DEG , 14,5 DEG +/-0,2 DEG , 16,2 DEG +/-0,3 DEG , 17,0 DEG +/-0,3 DEG , 17,7 DEG +/-0,2 DEG , 18,6 DEG +/-0,3 DEG , 19,1 DEG +/-0,2 DEG , 21,3 DEG +/-0,4 DEG , 22,4 DEG +/-0,5 DEG , 25,7 DEG +/-0,5 DEG et 28,3 DEG +/-0,5 DEG dans un diagramme de diffraction des rayons X. L'invention traite aussi d'un procédé de préparation de ce cristal, et d'une composition pharmaceutique le comprenant. Le cristal présente une excellente stabilité, et de nombreux avantages en matière de manipulation, de stockage et de préparation pharmaceutique. L'invention a aussi pour objet des cristaux B, C et D dudit composé.
Maruyama Akira
Masuda Katsuhiko
Oe Takayuki
Ueno Hiroaki
Kirby Eades Gale Baker
Mitsubishi Chemical Corporation
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