申请人:Kaken Pharmaceutical Co., Ltd.
公开号:EP3351533A1
公开(公告)日:2018-07-25
Provided is a compound showing excellent antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof:
wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C=O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.
本发明提供了一种化合物,该化合物对毛癣菌具有极佳的抗真菌活性,而毛癣菌是表皮真菌病的主要致病微生物,该化合物对毛癣菌引起的疾病具有极高的疗效。一种由式(I)代表的双芳基衍生物或其盐:
其中环 A 是任选取代的苯基,或任选取代的 5 或 6 元环杂芳基(环 A 可进一步缩合形成任选取代的融合环);Q 是 CH2、C=O、NH、O、S 或类似物;X1、X2 和 X3 是 CR1 或 N;Y 是 CH 或 N;Z 是 CR2b 或 N;R2a 和 R2b 各为氢原子、卤素原子、任选取代的 C1-C6 烷基、C1-C6 卤代烷基或类似基团;R2a 和 R2b 可与其键合的碳原子一起形成任选取代的碳环或任选取代的杂环。