申请人:H. Lundbeck A/S
公开号:US06031099A1
公开(公告)日:2000-02-29
Piperidine compounds having the general formula (I), ##STR1## wherein R.sup.1 is (a) a group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, phenyl, cycloalkylalkyl, cycloalkenylalkyl, phenylalkyl or diphenylalkyl linked to the piperidyl N-atom through an at least 2-membered spacer group; or (b) a group having general formula (II), ##STR2## wherein X is CHR.sup.10, O, S, SO, SO.sub.2 or NR.sup.10, Z.sup.1 is CH.sub.2, O, or S; Z.sup.2 and Z.sup.3 are independently (CH.sub.2).sub.n, n being 0 or 1, O or S or Z.sup.1 and Z.sup.2 may together represent a group --CH.dbd.CH--; or when Z.sup.3 is (CH.sub.2).sub.n wherein n is 0, Z.sup.1 and Z.sup.2 may together represent a 3-membered divalent group; show potent sigma receptor activity. Furthermore they show effect in animal models indicative of anxiolytic properties. Accordingly they are useful as medicines for the treatment of anxiety, psychosis, epilepsy, convulsion, movement disorders, motor disturbances, amnesia, cerebrovascular diseases, senile demential of the Alzheimer type or Parkinson's disease.
具有一般式(I)的哌啶化合物,其中R1是(a)由烷基,烯基,环烷基,环烯基,苯基,环烷基烷基,环烯基烷基,苯基烷基或二苯基烷基组成的基团,通过至少2个成员的间隔基团与哌啶N原子连接;或(b)具有一般式(II)的基团,其中X是CHR10,O,S,SO,SO2或NR10,Z1是CH2,O或S;Z2和Z3独立地是(CH2)n,n为0或1,O或S或Z1和Z2可以一起表示一个--CH=CH--基团;或当Z3是(CH2)n,其中n为0时,Z1和Z2可以一起表示一个3个成员的双价基团;显示出强大的σ受体活性。此外,它们在动物模型中表现出具有抗焦虑特性的效果。因此,它们可用作治疗焦虑症,精神病,癫痫,惊厥,运动障碍,遗忘症,脑血管疾病,阿尔茨海默病或帕金森病的药物。