申请人:Richter Gedeon Vegyeszeti Gyar Rt.
公开号:US04224325A1
公开(公告)日:1980-09-23
The invention relates to compounds of general formula ##STR1## wherein R.sup.1 stands for a hydrogen atom or a C.sub.1-6 alkyl-, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, R.sup.2 stands for a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a nitro or an --NR.sup.5 R.sup.6 group, wherein R.sup.5 and R.sup.6 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl or a C.sub.2-4 hydroxyalkyl group, R.sup.3 stands for a hydrogen atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, a chlorine atom or a hydroxyl, amino or methoxy group, R.sup.4 stands for a carbamoyl, a cyano or an --NR.sup.7 --NHR.sup.8 group, wherein R.sup.7 and R.sup.8 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.1-4 alkoxycarbonyl or an --NR.sup.9 R.sup.10 group, wherein R.sup.9 and R.sup.10 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-5 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl, a phenyl or a benzyl group, or --NR.sup.9 R.sup.10 may represent a morpholine, piperidine or piperazine ring, and their pharmaceutically acceptable acid-addition salts. Furthermore, the invention relates to a process for preparing these compounds. The novel compounds of general formula I have valuable pharmacological properties. Thus they show a considerable hypotensive effect and are capable to inhibit enzymes regulating the catabolism of prostaglandins.
本发明涉及一般式##STR1##的化合物,其中R.sup.1代表氢原子或C.sub.1-6烷基,C.sub.2-4羟基烷基,C.sub.3-6环烷基或苯基,R.sup.2代表氢、氟、氯或溴原子或C.sub.1-6烷基,C.sub.2-4羟基烷基,硝基或--NR.sup.5 R.sup.6基团,其中R.sup.5和R.sup.6可能具有相同或不同的含义,分别代表氢原子或C.sub.1-4烷基或C.sub.2-4羟基烷基,R.sup.3代表氢原子或C.sub.1-6烷基,C.sub.2-4羟基烷基,C.sub.3-6环烷基或苯基,氯原子或羟基,氨基或甲氧基,R.sup.4代表氨基甲酰基,氰基或--NR.sup.7 --NHR.sup.8基团,其中R.sup.7和R.sup.8可能具有相同或不同的含义,分别代表氢原子或C.sub.1-4烷基,C.sub.2-4羟基烷基,C.sub.1-4烷氧羰基或--NR.sup.9 R.sup.10基团,其中R.sup.9和R.sup.10可能具有相同或不同的含义,分别代表氢原子或C.sub.1-5烷基,C.sub.2-4羟基烷基,C.sub.3-6环烷基,苯基或苄基,或--NR.sup.9 R.sup.10可以表示吗啡啶,哌啶或哌嗪环,并且它们的药学上可接受的酸盐。此外,本发明涉及一种制备这些化合物的方法。一般式I的新化合物具有有价值的药理特性。因此,它们表现出显著的降压作用,并能够抑制调节前列腺素分解代谢的酶。