Dimeric piperidine, tetrahydropyridine and piperazine derivatives
    11.
    发明授权
    Dimeric piperidine, tetrahydropyridine and piperazine derivatives 失效
    二聚哌啶,四氢吡啶和哌嗪衍生物

    公开(公告)号:US5830896A

    公开(公告)日:1998-11-03

    申请号:US484361

    申请日:1995-06-07

    摘要: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (1), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalklyl, or X is CR.sup.8--R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.sub.2, CH.sub.2 OCH.sub.2, CH.sub.2 SCH.sub.2, CH.dbd.CH--O, or CH.dbd.CH--S; and Z.sup.2 is O, S or (CH.sub.2).sub.p, p being 0 or 1; are potent sigma receptor ligands thus being useful as drugs for the treatment of anxiety, psychosis, epilepsy, convulsion, movement disorders, motor disturbances, amnesia, cerebrovascular diseases, senile demential of the Alzheimer tpe or Parkinson's disease.

    摘要翻译: 本发明涉及具有通式(1)的二聚4-苯基哌啶,4-苯基-1,2,3,6-四氢吡啶或4-苯基哌嗪化合物或二聚螺环哌啶化合物,其中 n为1-5; R1至R4是取代基; R5和R6各自为氢或烷基或一起形成乙烯或丙烯桥; X是O,S,SO,SO2,CO或(CH2)m,m是0或1,X是NR7,R7是H,烷基,环烷基,环烷基烷基,苯基或苯基烷基,或X是CR8-R9,其中 R8和R9选自羟基和R7定义的取代基; 和(i)Z1是取代基,Z2是(CH2)p,其中p是0; Y为N,C或CH; (ii)Z1和Y通过单键连接在一起,从而形成螺环结; 在这种情况下,Y是C; Z1是O,S,(CH2)q,q是1,2或3,或Z1是CH2O,CH2S,CH2CH2O,CH2CH2S,CH = CH,CH = CHCH2,CH2OCH2,CH2SCH2,CH = CH-O或CH = CH-S; Z2为O,S或(CH2)p,p为0或1; 是有效的西格玛受体配体,因此可用作治疗焦虑,精神病,癫痫,惊厥,运动障碍,运动障碍,遗忘症,脑血管疾病,阿尔茨海默病或帕金森病老年痴呆症的药物。

    Dimeric piperidine, tetrahydropyridine and piperazine derivatives
    12.
    发明授权
    Dimeric piperidine, tetrahydropyridine and piperazine derivatives 失效
    二聚哌啶,四氢吡啶和哌嗪衍生物

    公开(公告)号:US5684012A

    公开(公告)日:1997-11-04

    申请号:US486740

    申请日:1995-06-07

    摘要: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.sub.2, CH.sub.2 OCH.sub.2, CH.sub.2 SCH.sub.2, CH.dbd.CH--O, or CH.dbd.CH--S; and Z.sup.2 is O, S or (CH.sub.2).sub.p, p being 0 or 1; are potent sigma receptor ligands thus being useful as drags 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.

    摘要翻译: 本发明涉及具有通式(I)的二聚4-苯基哌啶,4-苯基-1,2,3,6-四氢吡啶或4-苯基哌嗪化合物或二聚螺环哌啶化合物,其中 n为1-5; R1至R4是取代基; R5和R6各自为氢或烷基或一起形成乙烯或丙烯桥; X是O,S,SO,SO 2,CO或(CH 2)m,是0或1,X是NR 7,R 7是H,烷基,环烷基,环烷基烷基,苯基或苯基烷基,或X是CR 8 R 9,其中R 8和 R9选自羟基和R7定义的取代基; 和(i)Z1是取代基,Z2是(CH2)p,其中p是0; Y为N,C或CH; (ii)Z1和Y通过单键连接在一起,从而形成螺环结; 在这种情况下,Y是C; Z1是O,S,(CH2)q,q是1,2或3,或Z1是CH2O,CH2S,CH2CH2O,CH2CH2S,CH = CH,CH = CHCH2,CH2OCH2,CH2SCH2,CH = CH-O或CH = CH-S; Z2为O,S或(CH2)p,p为0或1; 是有效的西格玛受体配体,因此可用作治疗焦虑,精神病,癫痫,惊厥,运动障碍,运动障碍,遗忘症,脑血管疾病,阿尔茨海默氏型老年痴呆症或帕金森病的药物。