Method of treating psychoses
    2.
    发明授权
    Method of treating psychoses 失效
    治疗精神病的方法

    公开(公告)号:US5238945A

    公开(公告)日:1993-08-24

    申请号:US876040

    申请日:1992-04-30

    IPC分类号: A61K31/445

    CPC分类号: A61K31/445

    摘要: Disclosed is a method of treating psychoses in human beings, comprising the step of administering an effective amount of the compound, ##STR1## or a pharmaceutically acceptable salt thereof, to a patient in need thereof.Said compound selectively blocks dopamine neurones in the ventral tegmental area of the brain, substantially without blocking the dopamine neurones in the substantia nigra pars compacta and, therefore, is free from the extrapyramidal side effects of common neuroleptics.

    摘要翻译: 公开了一种治疗人类精神病的方法,包括向有需要的患者施用有效量的化合物“IMAGE”或其药学上可接受的盐的步骤。 所述化合物选择性地阻断脑的腹侧被盖区域中的多巴胺神经元,基本上不阻塞黑质微结构中的多巴胺神经元,因此没有普通神经安定药物的锥体束外副作用。

    Process for the preparation of methanol
    5.
    发明授权
    Process for the preparation of methanol 有权
    甲醇制备方法

    公开(公告)号:US06881759B2

    公开(公告)日:2005-04-19

    申请号:US10806443

    申请日:2004-03-23

    摘要: The present invention is a novel process for methanol production in a liquid phase reactor from a synthesis gas comprising of hydrogen, carbon dioxide and carbon monoxide. The liquid phase reactor contains a solid catalyst suspended in methanol. In this innovation, methanol acts both as a product and as a suspension medium for the catalyst. The new innovation exploits the condensing conditions for methanol production. By operating at condensing conditions, the methanol partial pressure at equilibrium is higher than the boiling pressure of methanol at the given temperature. Hence the produced methanol of the equilibrium composition condenses creating the potential of more gas to be converted. Since equilibrium is not a limiting factor, high conversions can be obtained.

    摘要翻译: 本发明是由氢,二氧化碳和一氧化碳组成的合成气体在液相反应器中生产甲醇的新方法。 液相反应器含有悬浮在甲醇中的固体催化剂。 在这项创新中,甲醇既作为产品又作为催化剂的悬浮介质。 新的创新利用甲醇生产的冷凝条件。 通过在冷凝条件下操作,平衡时的甲醇分压高于在给定温度下甲醇的沸腾压力。 因此,产生的平衡组合物的甲醇会凝结,从而产生更多的待转化气体的潜力。 由于平衡不是限制因素,因此可以获得高转化率。

    Dimeric piperidine, tetrahydropyridine and piperazine derivatives
    6.
    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
    7.
    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。

    Dimeric piperidine, tetrahydropyridine and piperazine derivatives
    10.
    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:US5837707A

    公开(公告)日:1998-11-17

    申请号:US467760

    申请日:1995-06-06

    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, 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 drugs 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,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CR8R9,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,阿尔茨海默氏型老年痴呆症或帕金森病的药物。