申请人:Meiji Seika Kaisha Ltd.
公开号:US04083850A1
公开(公告)日:1978-04-11
Novel compounds useful as hypotensive agents are presented having the general formula I ##STR1## wherein R.sub.1 represents a lower aliphatic acyl group, a straight or branched chain alkyl or alkenyl group or an aralkyl group of the general formula ##STR2## wherein R.sub.2 represents hydrogen, a lower alkyl group or a halogen atom. Furthermore, new therapeutic compositions of matter are also described incorporating the above novel 3-substituted-2(1H)pyridone-6-carboxylic acids (I) as an active ingredient with carriers and showing uses as hypotensive agents. These new compounds of the formula I are prepared either by reacting D-glucaro-.delta.-lactam or its salt with an acid anhydride or by reacting 3-hydroxy-2(1H)pyridone-6-carboxylic acid with an acyl anhydride or alkyl halide, aralkyl halide and an alkenyl halide.
具有一般式I的有用降压剂的新化合物被提出,其中R.sub.1代表较低的脂肪酰基,直链或支链烷基或烯基或一般式的芳基 ##STR2## 其中R.sub.2代表氢,较低的烷基或卤素原子。此外,还描述了包含上述新的3-取代-2(1H)吡啶酮-6-羧酸(I)作为活性成分的新治疗组合物,其中含有载体,并显示用作降压剂的用途。这些具有式I的新化合物可以通过将D-葡糖醛-δ-内酯或其盐与酸酐反应,或者通过将3-羟基-2(1H)吡啶酮-6-羧酸与酰酐或烷基卤化物、芳基卤化物和烯基卤化物反应来制备。