申请人:American Cyanamid Company
公开号:US04689324A1
公开(公告)日:1987-08-25
Novel 10,10-Dihydro-10-[(substituted carbonyl)imino]-10-phenyl-10H-phenoxaphines of the formula: ##STR1## wherein A is selected from the group consisting of hydrogen and COOR.sub.1, where, when A is hydrogen the compound is in the form of a water soluble salt HnX, where n is an integer 1 or 2 and X is selected from the group consisting of sulfate, trefluoroacetate, bromide and chloride and R.sub.1 is selected from the group consisting of straight or branched chain alkyl(C.sub.1 -C.sub.4), alkenyl(C.sub.2 -C.sub.4), alkynyl(C.sub.2 -C.sub.4), cycloalkyl(C.sub.3 -C.sub.6), cycloalkyl(C.sub.3 -C.sub.6)methyl, benzyl, pyridylmethyl or which tetrahydro-3-furanyl; methods for using these compounds for effecting diuresis, treating hypertension and edema and lowering plasma renin activity in mammals; pharmaceutical compositions of matter containing these compounds and processes for their preparation.
新颖的10,10-二氢-10-[(取代羰基)亚胺基]-10-苯基-10H-苯氧杂苯的化学式为:##STR1##其中A从羟基和COOR.sub.1组成的群体中选择,当A为氢时,该化合物以水溶性盐HnX的形式存在,其中n是整数1或2,X从硫酸盐、三氟乙酸盐、溴化物和氯化物组成的群体中选择,R.sub.1从直链或支链烷基(C.sub.1 -C.sub.4)、烯基(C.sub.2 -C.sub.4)、炔基(C.sub.2 -C.sub.4)、环烷基(C.sub.3 -C.sub.6)、环烷基(C.sub.3 -C.sub.6)甲基、苄基、吡啶甲基或四氢-3-呋喃基组成的群体中选择;使用这些化合物实现利尿、治疗高血压和水肿以及降低哺乳动物血浆肾素活性的方法;包含这些化合物的药物组合物和其制备过程。