Vitreous form
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsNorio Ohnishi, Osamu Aoki, Atsuo Ohike, Kazuto Okimoto, Hiroshi Ishikuro
Life of this patent
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Abstract
This invention relates to a vitreous form of 8-(3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline (FR173657). This vitreous form has good solid stability and, therefor, is useful for producing and supplying FR173657 products whose quality is stable enough to be suitable for medicines.
Claims13
A vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline.
A vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline, which is obtained by heating an amorphous form, crystalline form, or a mixture thereof of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)-acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline or its solvate at a temperature not lower than its melting point, followed by cooling it.
A vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline, of which endothermic peak top due to glass transition appears at around 126 to 128° C. in the differential scanning calorimetry (DSC;
- heating rate:
- 10° C./minute).
A vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline, which does not crystallize partially or fully, or does not decompose under long-term storage.
A process for preparing the vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline, which comprises heating an amorphous form, crystalline form, or a mixture thereof of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline or its solvate at a temperature not lower than its melting point, followed by cooling it.
Dependencies are inferred from the claim text.