申请人:Ciba-Geigy Corporation
公开号:US04517184A1
公开(公告)日:1985-05-14
The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an alkylene or alkylidene radical having a maximum of 5 carbon atoms, n represents O or 1, R.sub.2 and R.sub.3 each represents, independently of the other, hydrogen, lower alkyl, lower alkoxy or halogen, and A represents the radical O-R.sub.4, wherein R.sub.4 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.5 and R.sub.6 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.5 and R.sub.6 are bonded to one another and, together with the adjacent nitrogen atom, represent unsubstituted or lower alkyl-substituted tetra- or hexa-methyleneimino or 4-morpholinyl, to salts of compounds of the formula I in which A represents OR.sub.4 wherein R.sub.4 is hydrogen, with bases, and to acid addition salts of compounds of the formula I in which the radical R.sub.1 has a basic character, and to pharmaceutical compositions that contain them. The novel substances exhibit diuretic and, in addition, uricosuric activity and may be administered, according to the invention, preferably in the form of appropriate pharmaceutical compositions, to mammals for the treatment of oedema and hypertension.
该发明涉及公式I的新型苯二氧杂环己烯衍生物,其中R.sub.1代表未取代或取代的芳香或杂芳基团,alk代表最多具有5个碳原子的烷基或烷基亚甲基基团,n代表O或1,R.sub.2和R.sub.3分别代表,独立于其他,氢、较低的烷基、较低的烷氧基或卤素,A代表基团O-R.sub.4,其中R.sub.4代表氢或未取代或取代的脂肪或芳基脂肪基团,或A代表基团,其中R.sub.5和R.sub.6分别代表,独立于其他,氢或较低烷基,或R.sub.5和R.sub.6与彼此结合,并且与相邻的氮原子一起代表未取代或较低烷基取代的四氢或六亚甲基亚基或4-吗啉基,该发明还涉及公式I中A代表OR.sub.4的化合物的盐,其中R.sub.4为氢,与碱,以及公式I中基团R.sub.1具有碱性质的化合物的酸盐,以及含有它们的药物组合物。这些新物质具有利尿和尿酸排泄活性,并且根据该发明,它们可以以适当的药物组合物的形式优选地用于治疗水肿和高血压的哺乳动物。