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    • 6. 发明授权
    • 1,4-Disubstituted piperazines having dopaminergic activity
    • 具有多巴胺能活性的1,4-二取代哌嗪
    • US4874765A
    • 1989-10-17
    • US41206
    • 1987-04-22
    • Erzsebet LapisEdit TothBela KissJozsef TorleyEva PalosiIstvan HajduLaszlo SzpornyDora GrooIstvan Laszlovszky
    • Erzsebet LapisEdit TothBela KissJozsef TorleyEva PalosiIstvan HajduLaszlo SzpornyDora GrooIstvan Laszlovszky
    • C07D295/08A61K31/495A61P25/00A61P25/24A61P25/26C07D295/088C07D295/18C07D295/185C07D295/10
    • C07D295/185C07D295/088
    • The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and stand for hydrogen or halogen or a trihalomethyl, lower alkyl, lower alkoxy, nitro, hydroxyl, aralkyloxy or an 1-(2-propenyl-4-piperazinyl) group;R.sub.5 stands for hydrogen or a C.sub.1-4 alkyl group;R.sub.6 represents a C.sub.3-6 alkyl, alkenyl, alkynyl group or a ##STR2## group, wherein R.sub.7 means a C.sub.2-5 alkyl, alkenyl or alkinyl group; andis 2 or 3,with the provisos that:R.sub.6 is different from isopropyl, n-butyl and isobutyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2;R.sub.6 is different from isopropyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2; or when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-methyl group and n is 2; andR.sub.6 is different from propionyl group when R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen and n means 2.The compounds of the general formula (I) are therapeutically useful for the treatment of diseases arising from a hypofunction of the dopaminergic system.
    • 本发明涉及通式(I)的新的1,4-二取代哌嗪衍生物,其药学上可接受的酸加成盐和季铵盐,含有它们的药物组合物及其制备方法。 在通式(I)中,R 1,R 2,R 3和R 4相同或不同,代表氢或卤素或三卤代甲基,低级烷基,低级烷氧基,硝基,羟基,芳烷氧基或1- (2-丙烯基-4-哌嗪基)基团; R5代表氢或C1-4烷基; R6表示C3-6烷基,烯基,炔基或者IMAGE基团,其中R7表示C2-5烷基,烯基或炔基; 并且为2或3,条件是:当R 2,R 3,R 4和R 5代表氢时,R 6不同于异丙基,正丁基和异丁基,R 1表示2-氯且n为2; 当R2,R3,R4和R5代表氢时,R6不同于异丙基,R1表示2-氯,n是2; 或当R2,R3,R4和R5代表氢时,R1表示2-甲基,n表示2; 当R 1,R 2,R 3,R 4和R 5为氢且n表示2时,R 6与丙酰基不同。通式(I)的化合物可治疗用于治疗多巴胺能系统功能低下的疾病。