申请人:E. R. Squibb & Sons, Inc.
公开号:US04734424A1
公开(公告)日:1988-03-29
Bicycloheptane substituted amide 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, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S-, aryl-S-, arylalkyl-S-, ##STR4## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
提供了具有结构式##STR1##的双环庚烷取代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烷基,CO.sub.2碱金属,CO.sub.2多羟胺盐,--CH.sub.2 OH,##STR3##其中R.sup.4和R.sup.5相同或不同,为H,低烷基,羟基,低烷氧基或芳基,R.sup.4和R.sup.5中至少有一个不是羟基和低烷氧基;p为1至4;R.sup.1为H或低烷基;q为1至12;R.sup.2为H或低烷基;R.sup.3为H,低烷基,低烯基,低炔基,芳基,芳基烷基,低烷氧基,芳氧基,芳基烷氧基,氨基,烷基氨基,芳基氨基,芳基烷基氨基,低烷基-S-,芳基-S-,芳基烷基-S-,##STR4##(其中n'为0,1或2),烷基氨基烷基,芳基氨基烷基,芳基烷基氨基烷基,烷氧基烷基,芳氧基烷基或芳基烷氧基。这些化合物是心血管药物,例如,在治疗血栓性疾病中有用。