Hydroxybenzoate salts of metanicotine compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 213/46 (2006.01) A61K 31/4406 (2006.01)

Patent

CA 2584448

Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine- type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z- metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.

Selon la présente invention, des patients susceptibles de souffrir ou souffrant d'états ou de troubles, tels que des troubles du système nerveux central, sont traités par administration de compositions qui renferment des sels d'hydroxybenzoate de composés de type E-métanicotine. La formation de sels d'hydroxybenzoate de composés de type E-métanicotine est également utilisée dans la purification des composés E-métanicotine, à mesure que les sels d'hydroxybenzoate tendent à se cristalliser à l'extérieur, il ne reste alors que des impuretés, comme des composés Z-métanicotine et des composés, dont la liaison double a migré dans la solution. Si cela est souhaité, les sels d'hydroxybenzoate peuvent être convertis soit en base libre (E-métanicotine), soit en une autre forme de sel acceptable pharmaceutiquement.

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