Water soluble azoles as broad-spectrum antifungals

The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; n is 1...

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Hauptverfasser: L. MEERPOEL, L.J.J. BACKX, L.J.E. VAN DER VEKEN
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; n is 1, 2 or 3; Y is O, S or NR ; R represents hydrogen, aryl, Het , or an optionally substituted C1-6alkyl; each R independently represents hydrogen or C1-6alkyl; or in case R and R are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het is the same as Het and may also be piperazinyl, homopiperazinyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl; R represents hydrogen or C1-4alkyl; R represents hydrogen or C1-4alkyl; or R and R taken together form a bivalent radical of formula -N=CH- (i), -CH=N- (ii), -CH=CH-(iii), wherein one hydrogen atom in the radicals (i) and (ii) may be optionally be replaced and up to two hydrogen atoms in radical (iii) may optionally be replaced; D represents a trisubstituted (1,3-dioxolane or tetrahydrofuran) derivative; as antifungals; their processes for preparation, compositions containing them and their use as a medicine.