C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/02 (2006.01) A61K 31/7056 (2006.01) A61P 3/10 (2006.01)
Patent
CA 2725230
The present invention provides a novel form of 3-(3-{4-[3-(.beta.-D-gluco- pyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)- 2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3- (.beta.-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3- methylphenoxy}- propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.
L'invention concerne une nouvelle forme de 3-(3-{4-[3-(ß-D-glucopyranosyl-oxy)-5-isopropyl-1H-pyrazole-4-ylméthyl]-3-méthylphénoxy}propylamino)-2,2-diméthyl-propionamide qui présente une stabilité au stockage améliorée. Le dihydrate d'hémifumarate de 3-(3-{4-[3-(ß-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazole-4-ylméthyl]-3-méthyl-phénoxy}propylamino)-2,2-diméthylpropionamide est utile en tant que matériau de départ pharmaceutique car il présente une excellente stabilité au stockage. En outre, il présente une cristallinité extrêmement favorable ; et il convient à la production industrielle car il peut être purifié par des procédés simples.
Takeuchi Hideki
Tsuru Eiji
Kirby Eades Gale Baker
Kissei Pharmaceutical Co. Ltd.
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