申请人:Sterling Drug Inc.
公开号:US04104385A1
公开(公告)日:1978-08-01
Compounds useful as schistosomicidal agents are cyclic alkylidenyl N-[6-(R.sub.3 R.sub.4 N)-4(or 5)-R.sub.5 -3-pyridazinyl]aminomethylenemalonates (I), where R.sub.3 R.sub.4 N is lower-tertiary-amino and R.sub.5 is hydrogen or lower-alkyl, are prepared by reacting 3-amino-6-(R.sub.3 R.sub.4 N)-4(or 5)-R.sub.5 -pyridazine (III) with cyclic alkylidenyl .alpha.-(lower-alkoxymethylene)malonate (IV) or by heating equimolar quantities of III, tri-(lower-alkyl) orthoformate and cyclic alkylidenyl malonate (V). Also shown is cyclic isopropylidenyl N-(6-methylamino-3-pyridazinyl)aminomethylenemalonate, a schistosomicidal agent, and its preparation. Also shown are schistosomicidal compositions comprising as active component a schistosomicidally effective cyclic alkylidenyl N-[6-(R.sub.3 R.sub.4 N)-4(or 5)-R.sub.5 -3-pyridazinyl]aminomethylenemalonate (I) or cyclic isopropylidenyl N-(6-methylamino-3-pyridazinyl)aminomethylenemalonate (II) or salt thereof and a method for the treatment of schistosomiasis which comprises administering to a host infected with schistosomes a schistosomicidally effective amount of said active component.
用作血吸虫杀虫剂的化合物为环烷基亚亚乙基基 N-[6-(R.sub.3 R.sub.4 N)-4(或5)-R.sub.5 -3-吡啶啉基]氨基甲基丙二酸酯(I),其中 R.sub.3 R.sub.4 N 为次级亚胺基,R.sub.5 为氢或次烷基,通过将 3-氨基-6-(R.sub.3 R.sub.4 N)-4(或5)-R.sub.5 -吡啶啉(III)与环烷基亚亚乙基基 .alpha.-(次烷氧基甲基)丙二酸酯(IV)反应或通过加热 III、三-(次烷基)正甲酸酯和环烷基亚亚乙基基丙二酸酯(V)的等摩尔量来制备。还展示了环异丙亚亚乙基基 N-(6-甲基氨基-3-吡啶啉)氨基甲基丙二酸酯,一种血吸虫杀虫剂,以及其制备方法。还展示了包含作为活性成分的血吸虫杀虫效果的环烷基亚亚乙基基 N-[6-(R.sub.3 R.sub.4 N)-4(或5)-R.sub.5 -3-吡啶啉基]氨基甲基丙二酸酯(I)或环异丙亚亚乙基基 N-(6-甲基氨基-3-吡啶啉)氨基甲基丙二酸酯(II)或其盐的血吸虫杀虫组合物,以及一种治疗血吸虫病的方法,包括向感染血吸虫的宿主施用所述活性成分的血吸虫杀虫效果量。