申请人:The United States of America as represented by the Secretary of the
公开号:US05366997A1
公开(公告)日:1994-11-22
There are disclosed cardiovascularly active compounds possessing antihypertensive properties, and pharmaceutical compositions containing these agents and a method of treating cardiovascular disorders with the compounds. The active components of the pharmaceutical compositions are compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from straight chain and branched chain alkyl and olefinic groups, which may be unsubstituted or substituted; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a heterocyclic group; and R.sub.3 is a pharmaceutically acceptable organic group selected from alkyl and olefinic groups which may be unsubstituted or substituted, acyl, a sulfonyl, sulfinyl, sulfenyl, carbonate, or carbamate derivative; or R.sub.3 is a group of the formula--(CH.sub.2).sub.n ONN(O)NR.sub.1 R.sub.2, wherein n is 2-8, and R.sub.1 and R.sub.2 are as described above. Novel compounds are disclosed wherein at least one of R.sub.1, R.sub.2 and R.sub.3 is an olefinic group or heteroatom-substituted straight or branched chain alkyl or olefinic group. Novel methods of synthesizing the compounds are also disclosed.
本发明揭示了具有降压作用的心血管活性化合物,以及含有这些药物的制药组合物和使用这些化合物治疗心血管疾病的方法。制药组合物的活性成分是式I的化合物,其中R.sub.1和R.sub.2分别选择直链和支链烷基和烯烃基,可以是未取代或取代的;或者R.sub.1和R.sub.2与它们结合的氮原子形成杂环基团;R.sub.3是从可以是未取代或取代的烷基和烯烃基,酰基,磺酰基,亚磺酰基,碳酸酯或氨基甲酸酯衍生物中选择的药用可接受的有机基团;或者R.sub.3是公式-(CH.sub.2).sub.n ONN(O)NR.sub.1 R.sub.2的基团,其中n为2-8,R.sub.1和R.sub.2如上所述。还揭示了新的化合物,其中至少有一个R.sub.1,R.sub.2和R.sub.3是烯烃基或杂原子取代的直链或支链烷基或烯烃基。还揭示了新的合成这些化合物的方法。