C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/06 (2006.01) A61K 31/454 (2006.01) A61P 25/28 (2006.01)
Patent
CA 2580119
An amorphous object of (3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4- (4~methyl-1H-imidazol-1-yl)benzylidene]piperidine-2-one, which is represented by the formula (1) and has A.beta.-production inhibitory activity. The amorphous object has such satisfactory properties that it has excellent solubility, is stable, does not readily become a crystalline form, and has low hygroscopicity. It is hence suitable for use in pharmaceutical preparations.
La présente invention a pour objet une forme amorphe de la (3E)-1-[(1S)-1-(4-fluorophényl)éthyl]-3-[3-méthoxy-4-(4-méthyl-1H-imidazol-1-yl)benzylidène]pipéridine-2-one, de formule (1) qui présente un effet inhibiteur de la production de A.beta.. Ladite forme amorphe présente une excellente solubilité, est stable, ne se transforme pas spontanément en une forme cristalline, et se révèle faiblement hygroscopique. Elle est donc adaptée à une utilisation dans des préparations pharmaceutiques.
Doi Eriko
Ito Koichi
Kushida Ikuo
Eisai R. & D. Management Co. Ltd.
Smart & Biggar
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