申请人:The United States of America as represented by the Secretary of the Army
公开号:US04659708A1
公开(公告)日:1987-04-21
The subject 8-[6-(N-heterocyclic-substituted)hexylamino]-6-methoxy lepidine erivatives have the formula: ##STR1## wherein Z represents methyl or, together with the two contiguous carbon atoms, the benzo moiety of a benzopiperazinyl derivative when Y is --N(R')--, n is an integer from 0 to 2; Y represents --O--, --S--, --S(O)--, --S(O).sub.2 --, and --N(R')--; R' represents hydrogen, alkyl, lower alkyl, R" substituted lower alkyl, cycloalkyl, aryl, sulfonyl, saturated 1,4-diazepinyl, lower alkyl N-cyanocarboximidothioate, or --C(O)R'"; R" represents at least one of hydroxy, alkoxy, aralkoxy, amino, lower alkyl substituted amino, phenyl, halogenated phenyl, or sufonyl; and R'" represents lower alkyl, alkoxy, aralkoxy, amino, lower alkyl substituted amino or aryl substituted amino; and pharmaceutically acceptable salts thereof. These derivatives afford improvement in means for the chemotherapy of leishmaniasis when administered parenterally or orally to infected animals.
主题8-[6-(N-杂环取代)己基氨基]-6-甲氧基莱匹啶衍生物的公式如下:##STR1## 其中Z代表甲基或与相邻的两个碳原子一起,当Y为--N(R')--时,苯并哌嗪衍生物的苯并基;n是0到2的整数;Y代表--O--,--S--,--S(O)--,--S(O).sub.2--和--N(R')--;R'代表氢,烷基,低烷基,R"取代的低烷基,环烷基,芳基,磺酰基,饱和的1,4-二氮杂环基,低烷基N-氰基羧酰亚硫酸酯或--C(O)R' ";R"代表羟基,烷氧基,芳基烷氧基,氨基,取代的低烷基氨基,苯基,卤代苯基或磺酰基;R'"代表低烷基,烷氧基,芳基烷氧基,氨基,取代的低烷基氨基或取代的芳基氨基;以及其药学上可接受的盐。当通过口服或注射给感染动物时,这些衍生物可以提供治疗利什曼病的改进方法。