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.
本发明涉及一种新的苯二氧杂环衍生物,其化学式为I,其中R1代表未取代或取代的芳香或杂芳基团,烷基代表最多具有5个碳原子的烷基或烷基亚甲基基团,n代表O或1,R2和R3分别独立地代表氢、低烷基、低烷氧基或卤素,A代表OR4基团,其中R4代表氢或未取代或取代的脂肪或脂肪芳香族碳氢基团,或A代表式中的基团,式中R5和R6分别独立地代表氢或低烷基,或R5和R6相互结合,并与相邻的氮原子一起代表未取代或低烷基取代的四亚甲基或六亚甲基亚胺基或4-吗啉基,以及化合物的盐,其中A代表OR4,其中R4为氢,与碱形成的酸盐,以及化学式I中基团R1具有碱性特征的化合物的酸加成盐以及含有这些化合物的制药组合物。这些新物质表现出利尿和尿酸排泄活性,并且可以按照本发明的方法,优选以适当的制药组合物的形式给哺乳动物用于治疗水肿和高血压。