申请人:Alza Corporation
公开号:US04055593A1
公开(公告)日:1977-10-25
Novel alkyl diethers of prostaglandins of the formula; ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.6 are hydrogen when Y is a single bond and R.sub.2 and R.sub.6 are absent when Y is a double bond; R.sub.3 is keto, ##STR2## R.sub.4 is hydrogen or ##STR3## R'.sub.9 is hydrogen or lower alkyl; R'.sub.10 is lower alkyl; R'.sub.11 is lower alkyl; Z.sub.1 is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; Z.sub.2 is trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; X is a single bond or a double bond and X is a single bond when R.sub.4 and R.sub.5 are hydrogen; Y is a single bond or a double bond; n is 1 to 5, m is 0 to 4; and the non-toxic salts. The prostaglandin ethers possess valuable pharmacological properties as modifiers of smooth muscle activity, gastric secretion, blood pressure, lipolysis and the reproductive system. The compounds also induce labor and menses and they can be used for the relief of asthma and nasal congestion. The compounds are also useful as platelet anti-clumping agents and for the inhibition of peptic ulcers.
公式为:##STR1##其中R.sub.1是氢或较低的烷基;当Y为单键时,R.sub.2和R.sub.6是氢,当Y为双键时,R.sub.2和R.sub.6不存在;R.sub.3是酮,##STR2##R.sub.4是氢或##STR3##R'.sub.9是氢或较低的烷基;R'.sub.10是较低的烷基;R'.sub.11是较低的烷基;Z.sub.1是顺式或反式--CH.dbd.CH--或--CH.sub.2 CH.sub.2 --;Z.sub.2是反式--CH.dbd.CH--或--CH.sub.2 CH.sub.2 --;X是单键或双键,当R.sub.4和R.sub.5为氢时,X是单键;Y是单键或双键;n为1至5,m为0至4;以及非毒性盐。这些前列腺素醚具有有价值的药理学特性,可以作为平滑肌活性、胃分泌、血压、脂肪分解和生殖系统的调节剂。这些化合物还能诱导分娩和月经,可以用于缓解哮喘和鼻塞。这些化合物还可用作血小板抗凝聚剂和抑制消化性溃疡的药物。