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    Piperidine derivatives having anxiolytic effect
    2.
    发明授权
    Piperidine derivatives having anxiolytic effect 失效
    具有抗焦虑作用的哌啶衍生物

    公开(公告)号：US06207677B1

    公开(公告)日：2001-03-27

    申请号：US09391290

    申请日：1999-09-07

    申请人： Ejner K. Moltzen ,  Jens Kristian Perregaard

    发明人： Ejner K. Moltzen ,  Jens Kristian Perregaard

    IPC分类号： A61K31438

    CPC分类号： C07D221/20 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D417/12 ,  C07D491/10 ,  C07D495/10

    摘要： Piperidine compounds having the general formula (I), wherein R1 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), wherein X is CHR10, O, S, SO, SO2 or NR10, Z1 is CH2, O, or S; Z2 and Z3 are independently (CH2)n, n being 0 or 1, O or S or Z1 and Z2 may together represent a group —CH═CH—; or when Z3 is (CH2)n wherein n is 0, Z1 and Z2 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.

    摘要翻译： 具有通式（I）的哌啶化合物，其中R 1是（a）通过至少2个碳原子连接到哌啶基N原子上的烷基，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， 元间隔基; 或（b）具有通式（II）的基团，其中X是CHR 10，O，S，SO，SO 2或NR 10，Z 1是CH 2，O或S; Z2和Z3独立地为（CH2）n，n为0或1，O或S或Z1，Z2可以一起表示基团-CH = CH-; 或当Z 3为（CH 2）n，其中n为0时，Z 1和Z 2可以一起表示3元二价基团; 显示出有效的σ受体活性。 此外，它们在指示抗焦虑性质的动物模型中显示出效果。 因此，它们可用作治疗焦虑，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
    3.
    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：US6090808A

    公开(公告)日：2000-07-18

    申请号：US73884

    申请日：1998-05-06

    申请人： Jens Perregaard ,  John W. Stenberg ,  Ejner K. Moltzen

    发明人： Jens Perregaard ,  John W. Stenberg ,  Ejner K. Moltzen

    IPC分类号： C07D295/06 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61P9/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/26 ,  A61P25/28 ,  C07D20060101 ,  C07D211/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/20 ,  C07D211/44 ,  C07D211/54 ,  C07D211/70 ,  C07D211/72 ,  C07D211/74 ,  C07D213/04 ,  C07D221/20 ,  C07D241/02 ,  C07D241/04 ,  C07D241/06 ,  C07D295/073 ,  C07D295/13 ,  C07D295/135 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10 ,  C07D491/20

    CPC分类号： C07D295/135 ,  C07D211/18 ,  C07D295/13 ,  C07D491/10

    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，阿尔茨海默氏型老年痴呆症或帕金森病的药物。

    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：US5837707A

    公开(公告)日：1998-11-17

    申请号：US467760

    申请日：1995-06-06

    申请人： Jens Perregaard ,  John W. Stenberg ,  Ejner K. Moltzen

    发明人： Jens Perregaard ,  John W. Stenberg ,  Ejner K. Moltzen

    IPC分类号： C07D295/06 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61P9/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/26 ,  A61P25/28 ,  C07D20060101 ,  C07D211/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/20 ,  C07D211/44 ,  C07D211/54 ,  C07D211/70 ,  C07D211/72 ,  C07D211/74 ,  C07D213/04 ,  C07D221/20 ,  C07D241/02 ,  C07D241/04 ,  C07D241/06 ,  C07D295/073 ,  C07D295/13 ,  C07D295/135 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10 ,  C07D491/20

    CPC分类号： C07D295/135 ,  C07D211/18 ,  C07D295/13 ,  C07D491/10

    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。

    Dimeric piperidine, tetrahydropyridine and piperazine derivatives
    8.
    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：US5658921A

    公开(公告)日：1997-08-19

    申请号：US354280

    申请日：1994-12-12

    申请人： Jens Perregaard ,  John W. Stenberg ,  Ejner K. Moltzen

    发明人： Jens Perregaard ,  John W. Stenberg ,  Ejner K. Moltzen

    IPC分类号： C07D295/06 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61P9/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/26 ,  A61P25/28 ,  C07D20060101 ,  C07D211/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/20 ,  C07D211/44 ,  C07D211/54 ,  C07D211/70 ,  C07D211/72 ,  C07D211/74 ,  C07D213/04 ,  C07D221/20 ,  C07D241/02 ,  C07D241/04 ,  C07D241/06 ,  C07D295/073 ,  C07D295/13 ,  C07D295/135 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10 ,  C07D491/20 ,  C07D519/00

    CPC分类号： C07D295/135 ,  C07D211/18 ,  C07D295/13 ,  C07D491/10

    摘要： The subject invention describes Novel dimer 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having the general Formula I: ##STR1## wherein n is 1-5;R.sup.1 to R.sup.4 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulfonyl, C.sub.1-6 alkyl- or di-(C.sub.1-6 alkyl)amino, cyano, trifluoromethyl, nitro, trifluoromethylthio or trifluoromethylsulfonyloxy; R.sup.5 and R.sup.6 are independently hydrogen, or C.sub.1-6 alkyl;X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, or X is NR.sup.7, R.sup.7 being H, C.sub.1-6 alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are independently selected from the group consisting of hydroxy and the substituents defined under R.sup.7, any phenyl group being optionally substituted with one or more substituents selected from halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulfonyl, C.sub.1-6 alkyl or di(C.sub.1-6 alkyl)amino, cyano, trifluoromethyl or trifluoromethylthio; andZ.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; andZ.sup.2 is O, S or (CH.sub.2).sub.p, p being 0 or 1, with the proviso that Z.sup.1 may not be O, S or (CH.sub.2).sub.q, wherein q is 1 when Z.sup.2 is (CH.sub.2).sub.p wherein p is 0;or an acid addition salt thereof. These compounds are potent sigma receptor ligands thus being useful for the treatment of anxiety, psychosis, epilepsy, convulsion, movement disorders, motor disturbances, amnesia, cerebrovascular diseases senile dementia of the Alzheimer type or Parkinson's disease.

    摘要翻译： 本发明描述了具有通式I的新型二聚体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 是1-5; R 1至R 4独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，羟基，C 1-6烷硫基，C 1-6烷基磺酰基，C 1-6烷基 - 或二 - （C 1-6烷基）氨基，氰基 ，三氟甲基，硝基，三氟甲硫基或三氟甲基磺酰氧基; R 5和R 6独立地是氢或C 1-6烷基; X是O，S，SO，SO2，CO或（CH2）m，m是0或1，或X是NR7，R7是H，C1-6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独立地选自羟基和R7定义的取代基，任何苯基任选被一个或多个选自以下的取代基取代：卤素，C 1-6烷基，C 1-6烷氧基，羟基，C 1 -C 6烷氧基， 6烷硫基，C 1-6烷基磺酰基，C 1-6烷基或二（C 1-6烷基）氨基，氰基，三氟甲基或三氟甲硫基; Z1为O，S，（CH2）q，q为1,2或3，或Z1为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，条件是Z1不为O，S或（CH2）q，其中当Z2为（CH2）p时，q为1，其中p为0 ; 或其酸加成盐。 这些化合物是有效的西格玛受体配体，因此可用于治疗焦虑，精神病，癫痫，惊厥，运动障碍，运动障碍，遗忘症，脑血管疾病老年痴呆型老年痴呆症或帕金森病。

    1,2,3-Triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists
    9.
    发明授权
    1,2,3-Triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists 失效
    可用作乙酰胆碱激动剂的1,2,3-三唑和四唑取代的哌啶或四氢吡啶化合物

    公开(公告)号：US4866077A

    公开(公告)日：1989-09-12

    申请号：US209994

    申请日：1988-06-22

    申请人： Klaus P. Bogeso ,  Klaus G. Jensen ,  Ejner K. Moltzen ,  Henrik Pedersen

    发明人： Klaus P. Bogeso ,  Klaus G. Jensen ,  Ejner K. Moltzen ,  Henrik Pedersen

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P21/00 ,  A61P25/02 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D401/04 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention relates to novel compounds of the following formula, where the dotted line designates an optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,2,4- or 1,3,4-oxadiazole;R.sup.1 is selected from hydrogen, lower alkyl, optionally substituted with phenyl which may be substituted with halogen, lower alkyl, or lower alkoxy, or a group R.sup.6 --CO--NH--CH.sub.2 -- or R.sup.6 --O--CO--, wherein R.sup.6 is lower alkyl, branched or unbranched, or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy, or lower acyloxy;R.sup.2 and R.sup.3 are the same or different, each representing hydrogen, lower alkyl, cycloalkyl (3-6 C-atoms), lower alkenyl, lower alkadienyl, lower alkynyl, optionally substituted with hydroxy, halogen or phenyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy; R.sup.2 and R.sup.3 may further, respectively, be selected from trifluoromethyl or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy or lower acyloxy, or R.sup.2 and R.sup.3 may, respectively, be a group OR.sup.7 or SR.sup.7 wherein R.sup.7 is defined as R.sup.2 or R.sup.3, andif "het" includes 2 or more carbon atoms, R.sup.4 and R.sup.5 are the same or different, and each is defined as R.sup.2 or R.sup.3, and if "het" includes only one carbon atom, there is only one substituent, R.sup.4, on the heterocyclic ring, and R.sup.4 is defined as R.sup.2 or R.sup.3,as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.