申请人:American Cyanamid Company
公开号:US04703130A1
公开(公告)日:1987-10-27
Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein W is selected from the group consisting of methyl and phenyl optionally substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and phenyl; r, n, m and a are integers such that the expression r+(n+1)m+a is also an integer and has a value of 3 to 20; r is greater than or equal to 2; n is greater than or equal to 2; m is greater than or equal to zero and a is greater than or equal to zero; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer 2-12 and the moiety --(CHR).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4-7; in either the racemic or optically active forms.
描述具有以下公式的降压磷酸衍生物:##STR1## 其中W从由甲基和苯组成的基团中选择,该基团可以选择性地被C.sub.1 -C.sub.3烷基,C.sub.1 -C.sub.3烷氧基和苯基取代;r、n、m和a是整数,使得表达式r+(n+1)m+a也是整数,并且其值为3到20;r大于或等于2;n大于或等于2;m大于或等于零且a大于或等于零;T从氢和##STR2## 中选择,其中R.sub.1从氢,C.sub.1 -C.sub.4支链或直链烷基,C.sub.1 -C.sub.4支链或直链烷氧基和C.sub.1 -C.sub.4支链或直链烷基氨基组成的基团中选择;Q是从--(CH.sub.2).sub.p --和--(CHR).sub.p --中选择的二价基团,其中p是整数2-12,而基团--(CHR).sub.p --代表一个被一个或多个C.sub.1 -C.sub.10烷基或苯基取代的烷基链;Z从##STR3## 中选择,其中R.sub.2可以相同也可以不同,并且从氢和C.sub.1 -C.sub.4支链或直链烷基中选择,q是一个整数从4-7;可以是消旋的或光学活性形式。