申请人:Hoffmann-La Roche Inc.
公开号:US05214046A1
公开(公告)日:1993-05-25
The compound of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 individually is hydrogen, lower alkyl or lower alkenyl or together signify straight-chain alkylene with 2 to 4 carbon atoms, R.sup.3 is hydrogen, halogen or lower alkyl, Q is alkylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and each of Y and Y' individually is a direct bond or the group --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--, the group R.sup.1 R.sup.2 N--Q--O-- is attached to the 3- or 4 -position of ring A and the symbol R designates that the ring to which it is attached is unsubstituted or is substituted with at least one substitutent selected from the group consisting of halogen, trifluoromethyl, cyano, nitro, lower alkyl and lower alkoxy, and their pharmaceutically acceptable acid addition salts can be used for the control or prevention of fungal infections, especially of topical or systemic infections which are caused by pathogenic fungi, and for the manufacture of antifungally-active medicaments. The compounds of formula I have not only a pronounced antifungal activity, but they also exhibit synergistic effects in combination with other known antifungally-active substances which inhibit sterol biosynthesis such as ketoconazole and terbinafine.
该化合物的化学式为##STR1##,其中R.sup.1和R.sup.2分别为氢、低碳烷基或低碳烯基,或者一起表示具有2至4个碳原子的直链烷基;R.sup.3为氢、卤素或低碳烷基;Q为具有4至11个碳原子且两个自由价键之间至少有4个碳原子的烷基,或者具有4至11个碳原子且两个自由价键之间至少有4个碳原子的烯基;Y和Y'中的每一个都是直接键或基团--CH.sub.2 --、--CH.sub.2 CH.sub.2 --、--CH.dbd.CH--或--C.tbd.C--;基团R.sup.1 R.sup.2 N--Q--O--连接到环A的3-或4-位置,符号R表示其连接的环未被取代或者被取代至少一个取代基,该取代基可从卤素、三氟甲基、氰基、硝基、低碳烷基和低碳烷氧基组成的群体中选择,且它们的药学上可接受的酸盐可用于控制或预防由致病真菌引起的真菌感染,特别是局部或全身感染,用于制造具有抗真菌活性的药物。化合物I的化学式不仅具有明显的抗真菌活性,而且与其他已知抑制固醇生物合成的抗真菌活性物质(如酮康唑和特比萘芬)结合时还表现出协同效应。