申请人:Leo Pharmaceutical Products Ltd.
公开号:US04082851A1
公开(公告)日:1978-04-04
The invention relates to a series of new compounds, salts thereof and to methods for the preparation of the compounds which have the general formula ##STR1## in which R.sub.1 stands for an unsubstituted or substituted phenoxy, phenylthio, benzyl, phenylsulfinyl, or anilino radical; R.sub.2 stands for a -YR.sub.2 ' radical, in which Y represents -O-, -S-, or -NH-, and R.sub.2 ' represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or -alkynyl; or methyl or ethyl substituted with phenyl, furyl, thienyl or pyridyl; R.sub.3 and R.sub.4 which can be the same or different, and unsubstituted or substituted, stand for hydrogen or for a straight or branched C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl or -alkynyl radical, a C.sub.5 -C.sub.7 -cycloalkyl, a phenyl, or a 5-, 6- or 7-membered heterocyclic ring system containing not more than two hetero atoms selected from the group consisting of oxygen, sulphur and nitrogen, or for a C.sub.1 -C.sub.3 alkyl radical substituted with phenyl or with a 5-, 6- or 7-membered heterocyclic ring system containing not more than two hetero atoms selected from the group consisting of oxygen, sulphur and nitrogen; and R.sub.4 furthermore stands for a lower carbalkoxy radical, a C.sub.1 -C.sub.6 alkanoyl radical, or a benzoyl radical; and Salts thereof with pharmaceutically acceptable acids. The compounds of the invention possess a pronounced diuretic and/or saluretic activity with a very low excretion of potassium ions. The low toxicity also makes the present compounds particularly valuable in human and veterinary practice.
本发明涉及一系列新化合物及其盐,并涉及制备该化合物的方法,其具有以下通式:
其中,R1代表未取代或取代的苯氧基、苯
硫基、苄基、苯基亚磺酰基或
苯胺基基团;R2代表-YR2'基团,其中Y代表-O-、-S-或-NH-,R2'代表C1-C6烷基、C2-C6烯基或-炔基;或者被苯基、
呋喃基、
噻吩基或
吡啶基取代的甲基或乙基;R3和R4可以相同或不同,未取代或取代,代表氢或直链或支链C1-C8烷基、C2-C8烯基或-炔基、C5-C7环烷基、苯基或不超过两个来自氧、
硫和氮的杂原子的5、6或7元杂环环系统,或被苯基或不超过两个来自氧、
硫和氮的杂原子的5、6或7元杂环环系统取代的C1-C3烷基;R4还代表较低的羰基烷氧基基团、C1-C6烷酰基基团或苯甲酰基基团;以及与药学上可接受的酸形成的盐。本发明化合物具有明显的利尿和/或利盐作用,且
钾离子的排泄非常低。低毒性也使得本发明化合物在人类和兽医实践中特别有价值。