申请人:Daiichi Seiyaku Co., Ltd.
公开号:US04136188A1
公开(公告)日:1979-01-23
2-SUBSTITUTED-1,3-DIAZACYCLIC COMPOUNDS OF THE FORMULA: ##STR1## wherein R.sub.1 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; R.sub.2 represents a hydrogen atom, a lower alkoxycarbonyl group, an aliphatic acyl group or an aromatic acyl group, the aromatic ring of which may have one or more substituents selected from a halogen atom, a lower alkyl group, a lower alkoxy group, an acyl group and an acyloxy group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or an aralkyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group or an aryl group; R.sub.6 represents a cyclohexyl group, a pyridyl group or a phenyl group which may have a substituent selected from a halogen atom, a lower alkyl group and a lower alkoxy group; A represents -N.dbd., an -N(lower alkyl)- group or a methylene group; n represents an integer of from 2 to 4, and a dotted line indicates that a double bond is optional; salts of such derivatives; and the method for preparing such compounds and their salts; the compounds and their salts having a distinct anti-diabetic activity in humans and animals.
2-取代-1,3-二氮杂环化合物的化学式如下:##STR1## 其中R.sub.1代表氢原子、卤原子、低碳基或低氧基基团;R.sub.2代表氢原子、低碳氧羰基团、脂肪族酰基团或芳香族酰基团,芳香环可能具有一个或多个取代基,选自卤原子、低碳基、低氧基、酰基和酰氧基;R.sub.3代表氢原子、低碳基、低羟基碳基或芳基碳基;R.sub.4代表氢原子、低碳基或芳基;R.sub.6代表环己基、吡啶基或苯基,可能具有一个取代基,选自卤原子、低碳基和低氧基;A代表-N.dbd.、-N(低碳基)-基团或亚甲基基团;n表示2到4之间的整数,虚线表示双键是可选的;这些衍生物的盐;以及制备这种化合物及其盐的方法;这些化合物及其盐在人类和动物中具有明显的抗糖尿病活性。