申请人:The United States of America as represented by the Secretary of the Army
公开号:US04209519A1
公开(公告)日:1980-06-24
The subject 8-amino-6-methoxy lepidine derivatives have the formula: ##STR1## wherein, R represents an --alkylene (tertiary) amine, --alkylene-NH.sub.2, (N-alkylsubstituted piperadyl amino)-alkylene-, --alkylene-(tertiary) amine or --alkylene-N-heterocyclic; R.sub.1, represents an alkoxy, alkyl, halogenated alkyl, alkenyl, aryloxy, halogen or hydrogen radical; R.sub.2 represents an alkyl, halogenated alkyl or aryloxy; n represents integers 3, 4, 5, 6 or 7; and pharmaceutically acceptable salts thereof wherein the salt forming acid or acid-hydrate is organic or inorganic. These derivatives afford improvement in means for the chemotherapy of leishmaniasis. Presence of a basic sidechain attachment at position 8- provides means for enhancement of the effectiveness of such compounds, which may be administered parenterally or orally to infected animals.
主题8-氨基-6-甲氧基乙啶衍生物的化学式为:##STR1##其中,R代表--烷基(三级)胺,--烷基-NH.sub.2,(N-烷基取代哌啶基氨基)-烷基,--烷基-(三级)胺或--烷基-N-杂环;R.sub.1代表烷氧基,烷基,卤代烷基,烯基,芳氧基,卤素或氢基;R.sub.2代表烷基,卤代烷基或芳氧基;n代表整数3、4、5、6或7;以及其药学上可接受的盐,其中形成盐的酸或酸水合物是有机的或无机的。这些衍生物改进了利什曼病化疗的手段。在位置8处存在一种碱性侧链附着物,可提供增强这类化合物效果的手段,这些化合物可以通过注射或口服给受感染的动物。