Piperidin-2,6-dione pamoate salts and their use for the...

A - Human Necessities – 61 – K

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A61K 31/451 (2006.01) A61P 25/00 (2006.01) C07D 211/88 (2006.01)

Patent

CA 2495377

Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl- 4,4dimethylpiperidin-2,6-diones (1) and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5dimethoxyphenyl)-3-(3- dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine2,6-dione pamoate.

La présente invention concerne de nouveaux pamoates de certains 3-phényl-3-diméthylaminoalkyl-4,4diméthylpipéridin-2,6-diones (1), et certains de leurs solvates pharmacologiquement admis, ces pamoates et solvates ne donnant pas lieu à perte de poids ni modification hépaticytaire chez le rat. Cela a permis de limiter à des niveaux marginalement efficaces les doses d'hydrochlorures correspondant dans le traitement ou la prophylaxie de troubles affectifs en liaison avec le stress tels que l'anxiété, la dépression, la migraine et l'apnée du sommeil. Les pamoates préférés sont celui du 3(3,5diméthoxyphényl)-3-(3-diméthylaminopropyl)-4,4-diméthylpiperidine-2,6-dione, et plus particulièrement celui du 3(3-méthoxyphényl)-3-(3-diméthylaminopropyl)-4,4-diméthylpipéridine-2,6-dione.

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