A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/55 (2006.01) A61K 9/08 (2006.01) A61K 9/48 (2006.01) A61K 47/10 (2006.01) A61K 47/34 (2006.01) A61P 25/06 (2006.01)
Patent
CA 2662748
Liquid formulations comprising the compound 1-[1-({[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]amino}carbonyl)piperidin-4-yl]-2-oxo-1,2-dihydroimidazo[4,5-b]pyridin-3-ide have surprisingly improved bioavailability and stability in comprising polyethylene glycol, Tween (polysorbate 80), Cremophor® EL (polyoxyl 35 castor oil), propylene glycol, and optionally water, and may be filled into soft or hard gelatin capsules useful for treating conditions including migraine headache and cluster headache.
L'invention porte sur des formulations liquides qui renferment le composé 1-[1-({[(3R,6S)-6-(2,3-difluorophényl)-2-oxo-1-(2,2,2-trifluoroéthyl)azepan-3-yl]amino}carbonyl)pipéridin-4-yl]-2-oxo-1,2-dihydroimidazo[4,5-b]pyridin-3-ide. Les formulations de l'invention possèdent une biodisponibilité et une stabilité étonnament améliorées, en ce qu'elles comprennent du polyéthylène glycol, du Tween (polysorbate 80), du Cremophor® EL (polyoxyle 35-huile de ricin), du propylène glycol et, facultativement, de l'eau, et peuvent être placées dans des capsules de gélatine souple ou dure afin de traiter des troubles, parmi lesquels les maux de tête et les céphalées vasculaires de Horton.
Alani Laman L.
Breslin David
Jahansouz Hossain
Stellabott Joyce
Thompson Karen
Merck & Co. Inc.
Merck Sharp & Dohme Corp.
Norton Rose Canada S.e.n.c.r.l.,s.r.l./llp
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