Although several azole compounds are currently used for systemic mycoses, none of them completely fulfills the necessary clinical requirements of efficacy against major systemic mycoses including disseminated aspergillosis, safety, and availability in oral or parenteral formulations. Demand for parenterally formulated azole compounds for the treatment of serious systemic mycoses is increasing. Most of the azole compounds on the market as well as under development are highly lipophilic molecules that make parenteral formulation difficult.
The present invention relates to novel water soluble azole compounds useful for the treatment of systemic mycoses and suitable for both oral and particularly parenteral administration, a process for their manufacture, antifungal compositions containing them and a method for treating mycoses.
More particularly, the present invention refers to compounds of formula (I), 
wherein
Q is a 3H-imidazole or 1,2,4-triazole derivative with antifungal activity which is linked to the remainder of the compound of formula (I) by a nitrogen in the azole;
R1 is hydrogen or alkyl;
R2 is hydrogen, alkyl, alkylcarbonyloxyalkyl, alkoxycarbonyl, alkylcarbonyl, mono- or dialkylaminoalkylcarbonyloxyalkyl;
R3 is alkylaminoalkyl, alkylcarbonyl, alkylcarbonyloxyalkyl, alkylaminoalkylcarbonyloxyalkyl, hydrogen, acylalkylaminoalkyl, alkyl, hydroxyalkyl, aminoalkyl, alkylcarbonylaminoalkyl, alkylcarbonylalkylaminoallkyl, alkoxycarbonylalkylaminoalkyl, alkoxycarbonylaminoalkyl, optionally substituted phenyl, optionally substituted pyridin-2-yl or optionally substituted 5-or 6-membered cycloalkyl, acylaminoalkyl, alkylaminoalkylacyloxyalkyl or
the group (R2, R3)Nxe2x80x94 may form an optionally substituted pyrrolidine, pyrrolidone or piperidine; and
Xxe2x88x92 is a pharmaceutically acceptable anion,
as well as pharmaceutically acceptable salts, hydrates or solvates of the compounds of formula (I).
USPTO Backgrounds
USPTO Backgrounds