申请人:Ferrer Internacional, S.A.
公开号:US04883797A1
公开(公告)日:1989-11-28
Derivatives of piperazine having the general formula ##STR1## wherein R.sub.1 is benzhydryl or cinnamyl and R.sub.2 is selected from the group consisting of ##STR2## --(CH.sub.2).sub.3 --R.sub.8, --CH.sub.2 NHR.sub.9, --CH.sub.2 NH.sub.2 and --COR.sub.10 ; wherein R.sub.3 is hydrogen, chloromethyl, (4-benzhydryl-1-piperazinyl) methyl, 4-morpholinylmethyl or 1-piperidinylmethyl, R.sub.4 is hydrogen, chloromethyl or carbethoxy, R.sub.5 and R.sub.6 taken together are an oxygen atom or the radical --O--(CH.sub.2).sub.2 --O--, R.sub.7 is methyl, phenyl or 2-thienyl, R.sub.8 is 4-morpholinyl, 1-piperidinyl or 4-benzhydryl-1-piperazinyl, R.sub.9 is 2-oxo-1- (pyrrolidinyl) acetyl, 2-hydroxybenzoyl or 4-sulfamoylbenzoyl, R.sub.10 is 2-oxo-1-(pyrrolidinyl)methyl or 4-sulfamoylphenyl and X is oxygen or NH; as well as methods for making the same and their use in a pharmaceutical composition is proposed. The compounds have cardiovascular properties and increasing effects on cerebral flow.
Piperazine的衍生物具有以下一般公式:其中R.sub.1是苯甲基或肉桂基,R.sub.2选自以下组合:--(CH.sub.2).sub.3 --R.sub.8, --CH.sub.2 NHR.sub.9, --CH.sub.2 NH.sub.2和--COR.sub.10;其中R.sub.3是氢、氯甲基、(4-苯甲基-1-哌嗪基)甲基、4-吗啉基甲基或1-哌啶基甲基,R.sub.4是氢、氯甲基或羰乙氧基,R.sub.5和R.sub.6一起是氧原子或基团--O--(CH.sub.2).sub.2 --O--,R.sub.7是甲基、苯基或2-噻吩基,R.sub.8是4-吗啉基、1-哌啶基或4-苯甲基-1-哌嗪基,R.sub.9是2-氧代-1-(吡咯啉基)乙酰基、2-羟基苯甲酰基或4-磺酰基苯甲酰基,R.sub.10是2-氧代-1-(吡咯啉基)甲基或4-磺酰基苯基,X是氧或NH;并提出了制备这些化合物的方法以及它们在制药组合物中的用途。这些化合物具有心血管特性和增加对脑血流的影响。