申请人:Novo Nordisk A/S
公开号:US05276035A1
公开(公告)日:1994-01-04
A disubstituted piperazine compound having the formula ##STR1## wherein R.sup.1 is halogen, methoxy, C.sub.1-6 -alkyl or trifluoromethyl, and R.sup.2 is methyl or substituted C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl, where substituents may be hydroxy-, keto- or oximino-groups in any position leading to a stable tertiary amine; or R.sup.2 is a straight or branched C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl, which in any position may be substituted as above, but is terminally substituted with one of the following groups: cyano, optionally C.sub.1-4 -alkoxy-substituted C.sub.1-4 -alkoxy, dimethoxy, optiontionally substituted phenoxy, phosphonic acid, thienyl, furyl, oxazoline, isoxazole, oxadiazole, where the optional substitution is represented by C.sub.1-6 -alkyl or phenyl, provided that when cyano is the only substituent in R.sup.2, R.sup.2 must contain at least four carbon atoms, and pharmaceutically acceptable acid addition salts thereof. The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.
一种二取代哌嗪化合物,其化学式为##STR1##其中R.sup.1为卤素、甲氧基、C.sub.1-6-烷基或三氟甲基,R.sup.2为甲基或取代的C.sub.1-8-烷基、C.sub.3-8-烯基或C.sub.3-8-环烷基,取代基可以是羟基、酮基或肟基,位于任何位置导致稳定的三级胺;或者R.sup.2为直链或支链的C.sub.1-8-烷基或C.sub.3-8-烯基,在任何位置可以如上述取代,但末端取代为以下之一的基团:氰基、可选的C.sub.1-4-烷氧基取代的C.sub.1-4-烷氧基、二甲氧基、可选取代的苯氧基、膦酸、噻吩基、呋喃基、噁唑啉、异噁唑啉、噁二唑啉,其中可选的取代由C.sub.1-6-烷基或苯基表示,但当氰基是R.sup.2中唯一的取代基时,R.sup.2必须至少含有四个碳原子,并且其药学上可接受的酸盐。这些化合物在治疗涉及多巴胺缺乏的精神障碍中是有用的。