Mono-lysine salts of azole compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 405/14 (2006.01) A61K 31/4196 (2006.01) A61K 31/427 (2006.01) A61P 31/04 (2006.01) C07C 229/26 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2606185

Mono-lysine salts of triazole compounds having a secondary or tertiary hydroxy group are provided. More particularly, the new water-soluble triazole antifungal mono-lysine salt compounds, or solvates thereof, are provided having the general formula I: wherein A in formula I represents the non- hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group. R and R1 in formula I can each be a hydrogen atom or an alkyl group having one to six carbon atoms. The novel water-soluble azole compounds are useful for the treatment of fungal infections and can be administered orally, topically and parenterally.

L'invention concerne des sels mono-lysines de composés triazoles possédant un groupe hydroxy secondaire ou tertiaire. Plus spécifiquement, l'invention concerne de nouveaux composés de sels mono-lysines antifongiques hydrosolubles, ou des solvates de ceux-ci, représentés par la formule générale (I), dans laquelle A représente la partie non hydroxy d'un composé antifongique triazole du type contenant un groupe hydroxyle secondaire ou tertiaire, R et R1 peuvent chacun représenter un atome d'hydrogène ou un groupe alkyle possédant de un à six atomes de carbone. Ces nouveaux composés azoles hydrosolubles sont utiles dans le traitement d'infections fongiques et peuvent être administrés par voie orale, de façon topique ou de façon parentérale.

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