申请人:E. R. Squibb & Sons, Inc.
公开号:US04654355A1
公开(公告)日:1987-03-31
7-Oxabicycloheptane substituted amide-thioamide prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 0 to 4; A is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; n is 1 to 5; Q is --CH.dbd.CH--, --CH.sub.2 --, ##STR2## or a single bond; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, --CH.sub.2 OH, ##STR3## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; p is 1 to 4; R.sup.1 is H or lower alkyl; q is 1 to 12; R.sup.2 is H or lower alkyl; and R.sup.3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aralkyloxy, amino, alkylamino, or arylamino. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
提供了具有结构式 ##STR1## 的7-Oxabicycloheptane取代酰胺-硫酰胺前列腺素类似物,其中m为0至4; A为--CH.dbd.CH--或--CH.sub.2 CH.sub.2 --; n为1至5; Q为--CH.dbd.CH--, --CH.sub.2 --, ##STR2## 或单键; R为CO.sub.2 H,CO.sub.2 alkyl,CO.sub.2 alkali metal,CO.sub.2 polyhydroxyamine salt,--CH.sub.2 OH,##STR3## 其中R.sup.4和R.sup.5相同或不同,分别为H,低碳基,羟基,低烷氧基或芳基,至少一个R.sup.4和R.sup.5不是羟基和低烷氧基; p为1至4; R.sup.1为H或低碳基; q为1至12; R.sup.2为H或低碳基; R.sup.3为H,低碳基,低烯基,低炔基,芳基,芳基烷基,低烷氧基,芳基氧基,氨基,烷基氨基或芳基氨基。这些化合物是心血管药物,例如用于治疗血栓性疾病。