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    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：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
    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：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。

    3-[4-[4-substituted-1-piperazinyl]-1-butyl]-1H-2,3-dihydroindoles
    13.
    发明授权
    3-[4-[4-substituted-1-piperazinyl]-1-butyl]-1H-2,3-dihydroindoles 失效
    3- [4- [4-取代-1-哌嗪基] -1-丁基] -1H-2,3-二氢吲哚

    公开(公告)号：US5002948A

    公开(公告)日：1991-03-26

    申请号：US456938

    申请日：1989-12-26

    申请人： Jens Perregaard ,  John W. Stenberg

    发明人： Jens Perregaard ,  John W. Stenberg

    IPC分类号： A61K31/495 ,  A61P9/00 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D209/14 ,  C07D209/34 ,  C07D231/56 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12

    CPC分类号： C07D405/12 ,  C07D209/14

    摘要： The present invention relates to novel piperazinylbutylindoles, -indazoles, the corresponding 2,3-dihydro derivatives and 2-indolones which have been found to have central serotonin activity with preference for the serotonin 5-HT.sub.lA receptor.Compared to the anxiolytic drug buspirone, and other clinically investigated compounds such as ipsapirone and gepirone, most of the present compounds have lower efficacy at the 5-HT.sub.lA receptor which implies less side effects related to activation of the receptors.The invention also includes acid addition salts, methods of preparation, pharmacetical compositions and method of treating CNS disorders occuring in anxiety, depression, aggression and in alcohol abuse, or in states of disease related to the cardiovascular, gastrointestinal and renal systems, by administering the aforementioned derivatives.Separation and use of the stereo isomers of the 2,3-dihydro derivatives and 2-indolones are also part of this invention.

    Process for the preparation of hydrogen and synthesis gas
    15.
    发明申请
    Process for the preparation of hydrogen and synthesis gas 有权
    氢气和合成气的制备方法

    公开(公告)号：US20050108941A1

    公开(公告)日：2005-05-26

    申请号：US10989306

    申请日：2004-11-17

    申请人： Poul Nielsen ,  Jens Perregaard

    发明人： Poul Nielsen ,  Jens Perregaard

    IPC分类号： B01J23/80 ,  C01B3/02 ,  C01B3/32 ,  C01B3/40 ,  C01B3/42

    CPC分类号： C01B3/323 ,  C01B3/326 ,  C01B2203/0233 ,  C01B2203/1076 ,  C01B2203/1223 ,  Y02P20/52

    摘要： Process for production of synthesis gas comprising carbon monoxide, carbon dioxide and hydrogen by reforming of methanol including the steps of: (a) introducing methanol in liquid phase into a reactor containing a solid methanol reforming catalyst suspended in a liquid phase of methanol and water; (b) reacting the liquid phase of methanol and water in presence of the suspended catalyst at a pressure and temperature, where methanol is maintained in the liquid phase; and (c) withdrawing from the reactor a gas phase of synthesis gas being produced during reaction of the liquid methanol and water phase.

    摘要翻译： 包括以下步骤生产包括一氧化碳，二氧化碳和氢的合成气的方法包括以下步骤：（a）将液相中的甲醇引入到悬浮在甲醇和水的液相中的固体甲醇重整催化剂的反应器中; （b）在甲醇保持在液相的压力和温度下，在悬浮催化剂存在下使甲醇和水的液相反应; 和（c）从反应器中取出在液体甲醇和水相反应期间产生的合成气的气相。

    Dimeric piperidine, tetrahydropyridine and piperazine derivatives
    16.
    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。