C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/88 (2006.01) A61K 31/45 (2006.01) A61P 25/22 (2006.01) A61P 25/24 (2006.01)
Patent
CA 2459009
Novel bisulphate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4- dimethylpiperidin-2,6-diones 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 bisulphate salts are 3(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4- dimethylpiperidine-2,6-dione bisulphate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione bisulphate.
L'invention concerne des nouveaux sels d'hydrogénosulfate de certains 3-phényl-3-diméthylaminoalkyle-4,4-diméthylpipéridine-2,6-diones et des solvates pharmaceutiquement acceptables de ces composés. Ces sels sont dépourvus d'une perte de poids et de changements d'hépatocytes chez le rat, ce qui limite les valeurs efficaces marginaux des doses cliniques autorisées des chlorhydrates correspondants dans les traitement ou la prophylaxie des troubles affectifs en rapport avec le stress tels que l'anxiété, la dépression, les migraines, et des apnées du sommeil. Les sels d'hydrogénosulfate utilisés de préference sont 3(3,5-dimethoxyphényle)-3-(3-diméthylaminopropyle)-4,4-diméthylpiperidine-2,6-dione hydrogénosulphate et, notamment, 3(3-méthoxyphényle)-3-(3-diméthylaminopropyle)-4,4-diméthylpiperidine-2,6-dione hydrogénosulphate.
Prestwick Pharmaceuticals Inc.
Sim & Mcburney
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