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    Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites
    1.
    发明申请
    Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 有权
    具有对多巴胺-D2受体和5-羟色胺再摄取位点的亲和力的组合的四氢吡啶-4-基吲哚

    公开(公告)号：US20060122206A1

    公开(公告)日：2006-06-08

    申请号：US11294657

    申请日：2005-12-06

    申请人： Roelof Hes ,  Pieter Smid ,  Cornelis Kruse ,  Martinus Tulp

    发明人： Roelof Hes ,  Pieter Smid ,  Cornelis Kruse ,  Martinus Tulp

    IPC分类号： A61K31/513 ,  C07D403/14

    CPC分类号： C07D401/14

    摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.

    摘要翻译： 本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和 涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 本发明涉及下式的新的四氢吡啶-4-基吲哚。 和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3） ，烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3）， 或A和Z一起形成饱和或（部分）不饱和的5或6元环，其可被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳 ，硫氮。

    New phenylpiperazines
    4.
    发明申请
    New phenylpiperazines 有权
    新的苯基哌嗪

    公开(公告)号：US20060293313A1

    公开(公告)日：2006-12-28

    申请号：US11450323

    申请日：2006-06-12

    申请人： Roelof Hes ,  Johannes Van der Heijden ,  Cornelis Kruse ,  Tipker Jacobus ,  Martinus Tulp ,  Gerben Visser ,  Bernard Van Vliet

    发明人： Roelof Hes ,  Johannes Van der Heijden ,  Cornelis Kruse ,  Tipker Jacobus ,  Martinus Tulp ,  Gerben Visser ,  Bernard Van Vliet

    IPC分类号： A61K31/5415 ,  A61K31/538 ,  A61K31/496 ,  C07D417/14 ,  C07D413/14 ,  C07D405/14 ,  C07D403/14

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.

    摘要翻译： 本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D 2 O受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与 多巴胺能和/或血清素能系统如焦虑障碍，抑郁症，帕金森病和精神分裂症。 本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R 5和R 6独立地是H或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）2 - ，其中p的值为3 -5和R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或吲哚基的第7位上的R 6（R 7）表示 - （CH 2）2 - 其中q具有2-4，及其盐。

    TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES
    5.
    发明申请
    TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES 有权
    具有多巴胺D2受体和丝氨酸蛋白酶重复位点的亲和力组合的四氢吡啶并[4-YL]吲哚

    公开(公告)号：US20070066634A2

    公开(公告)日：2007-03-22

    申请号：US11294657

    申请日：2005-12-06

    申请人： Roelof van Hes ,  Pieter Smid ,  Cornelis Kruse ,  Martinus Tulp

    发明人： Roelof van Hes ,  Pieter Smid ,  Cornelis Kruse ,  Martinus Tulp

    IPC分类号： A61K31/513 ,  C07D403/14

    CPC分类号： C07D401/14

    摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6- membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.

    摘要翻译： 本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和 涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 本发明涉及下式的新的四氢吡啶-4-基吲哚。 和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3） ，烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3）， 或A和Z一起形成饱和或（部分）不饱和的5-或6-元环，其可以被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳 ，硫氮。