申请人:Duphar International Research B.V.
公开号:US06225312B1
公开(公告)日:2001-05-01
The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1 is hydrogen or fluoro; R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3 and R4 independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2 and serotonin 5-HT1A receptors.
这项发明涉及一组具有有趣药理特性的新哌嗪和哌啶化合物。已经发现,具有以下式(a)的化合物具有这些特性:其中A代表一个由5-7个环原子组成的杂环基团,其中来自O、N和S的1-3个杂原子存在;R1为氢或氟;R2为C1-4-烷基、C1-4-烷氧基或氧代基,p为0、1或2;Z代表碳或氮,当Z为氮时,虚线为单键,当Z为碳时,为单键或双键;R3和R4独立地为氢或C1-4-烷基;n的值为1或2;R5为卤素、羟基、C1-4-烷氧基或C1-4-烷基,q为0、1、2或3;Y为苯基、呋喃基或噻吩基,这些基团可以被羟基、卤素、C1-4-烷氧基、C1-4-烷基、氰基、氨基甲酰基、单或双C1-4-烷基氨基甲酰基等1-3个取代基取代;以及它们的盐对多巴胺D2和5-羟色胺5-HT1A受体均表现出高亲和力。