Water soluble azoles as broad-spectrum antifungals

本发明涉及式(I)其N-氧化物型、药学上可接受的加成盐和立体化学异构体形式的新型化合物；其中L代表式(a)、(b)、(c)、(d)、(e)或(f)的基团；其中各Alk独立代表任选取代的C#-[1-6]链烷二基；n为1、2或3；Y为O、S或NR#+[2]；R#+[1]代表芳基、Het#+[1]或任选取代的C#-[1-6]烷基；R#+[2]代表氢；或在R#+[1]和R#+[2]连于同一氮原子的情况下，它们可一起构成杂环基；或它们可一起构成叠氮基；各R#+[3]独立代表氢、羟基或C#-[1-4]烷氧基；芳基代表苯基、萘基、1，2，3，4-四氢萘基、茚基或2，3-二氢化茚基；各所述芳基团可任选被取代；Het#+[1]代表任选取代的单环或双环的杂环基；Het#+[2]与Het#+[1]相同，且均可以是哌嗪基、高哌嗪基、1，4-二氧杂环己烷基、吗啉基、硫代吗啉基；R#+[6]代表氢或C#-[1-4]烷基；R#+[7]代表氢或C#-[1-4]烷基；或R#+[6]和R#+[7]一起构成式-N＝CH-(i)、-CH＝N-(ii)、-CH＝CH-(iii)、-CH#-[2]-CH#-[2]-(iv)的二价基团，其中在基团(i)和(ii)中的一个氢原子可被C#-[1-4]烷基取代，在基团(iii)和(iv)中的一个或多个氢原子可以被C#-[1-4]烷基取代；D代表三取代的四氢呋喃衍生物；本发明涉及作为抗真菌药的所述化合物；还涉及它们的制备方法、包含它们的组合物以及它们作为药物的用途。∴∴∴∴ 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.