申请人:Schering Corporation
公开号:US05039676A1
公开(公告)日:1991-08-13
This invention relates to tri- and tetra-substituted-oxetanes, e.g. (.+-.)-cis- and (.+-.)-trans-2-[(4-(4-isopropylpiperazin-1-yl)phenoxy)methyl]-4-(2,4-dihal ophenyl)-4-[1H-1,2,4-triazol-1-yl)-methyl]oxetane and tri- and tetra-substituted-tetrahydrofurans, e.g. (.+-.)-cis- and (.+-.)-trans-1-[4-[[2-(2,4-dihalophenyl)tetrahydro-2-[(1H-azol-1-yl)methyl ]-5-furanylmethoxy]phenyl]-4-yl-1-substituted piperazine-3-one and related derivatives which exhibit antifungal and antiallergy activities, pharmaceutical composition thereof, methods of their use in treating or preventing susceptible fungal infections and allergic reactions in a host including warm-blooded animals such as humans.
该发明涉及三取代和四取代氧杂环戊烷,例如(.+-.)-顺式和(.+-.)-反式-2-[(4-(4-异丙基哌嗪-1-基)苯氧基)甲基]-4-(2,4-二卤苯基)-4-[1H-1,2,4-三唑-1-基)-甲基]氧杂环戊烷和三取代和四取代四氢呋喃,例如(.+-.)-顺式和(.+-.)-反式-1-[4-[[2-(2,4-二卤苯基)四氢-2-[(1H-唑-1-基)甲基]-5-呋喃基氧基]苯基]-4-基-1-取代哌嗪-3-酮及相关衍生物,这些化合物具有抗真菌和抗过敏活性,以及它们的药物组合物、在治疗或预防宿主中如温血动物(包括人类)中易感染的真菌感染和过敏反应的方法。