申请人:Richter Gedeon Vegyeszeti Gyar Rt.
公开号:US03989701A1
公开(公告)日:1976-11-02
New compounds of the general formula (I) ##SPC1## wherein R.sub.1 and R.sub.2 each is a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, or R.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, and R.sub.3 is hydrogen or an acyl group derived from a C.sub.1.sub.-18 carboxylic acid. The compounds are prepared by reducing the corresponding nitro compounds of the general formula (II) ##SPC2## and optionally acylating the obtained product. The compounds of the general formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.
通式(I)的新化合物:##SPC1##其中,R.sub.1和R.sub.2分别是饱和或不饱和的直链或支链烷基,芳基烷基,饱和或不饱和的环烷基或芳基,或R.sub.1和R.sub.2与相邻的氮原子一起形成带有或不带有进一步的氧或氮杂原子的取代或未取代的杂环基;R.sub.3是氢或来源于C.sub.1.sub.-18羧酸的酰基。该化合物的制备方法是还原通式(II)的相应硝基化合物:##SPC2##并可选择性地酰化所得的产物。通式(I)的化合物及其酸加合物和季铵盐主要在诱导肝微粒体酶方面具有活性,但它们还具有有价值的退烧活性和与抗抑郁药物相似的麻醉药物致死率增加效应。