Antifungal 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones
申请人:JANSSEN PHARMACEUTICA N.V.
公开号:EP0402989A2
公开(公告)日:1990-12-19
4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones of formula
wherein
Q is CH or N;
Y is a radical of formula
R¹ is C₅₋₇cycloalkyl or mono-, di-, tri-, tetra- or pentahaloC₁₋₄alkyl; and
R² is C₁₋₆alkyl, C₅₋₇cycloalkyl or mono-, di-, tri-, tetra- or pentahaloC₁₋₄alkyl,
the acid addition salts and stereoisomeric forms thereof; said compounds having antifungal properties. Pharmaceutical compositions containing such compounds as an active ingredient; methods of preparing said compounds and pharmaceutical compositions.
式中的 4-[4-[4-[4-[[2-(2,4-二氟苯基)-2-(1H-偶氮啉甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]-1-哌嗪基]苯基]三唑酮和咪唑啉酮
其中
Q 是 CH 或 N;
Y 是式中的基团
R¹ 是 C₅₋₇环烷基或单、二、三、四或五卤 C₁₋₄烷基;以及
R² 是 C₁₋₆烷基、C₅₋₇环烷基或单、二、三、四或五卤 C₁₋₄烷基、
酸加成盐及其立体异构形式;所述化合物具有抗真菌特性。含有此类化合物作为活性成分的药物组合物;制备所述化合物和药物组合物的方法。