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    Diazabicyclononyl oxadiazole compounds and their use as nicotinic acetylcholine receptor modulators
    1.
    发明授权
    Diazabicyclononyl oxadiazole compounds and their use as nicotinic acetylcholine receptor modulators 有权
    二氮杂双环壬基恶二唑化合物及其作为烟碱乙酰胆碱受体调节剂的用途

    公开(公告)号：US08946412B2

    公开(公告)日：2015-02-03

    申请号：US13516350

    申请日：2010-12-16

    申请人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Østergaard Nielsen ,  Tino Dyhring ,  Philip K. Ahring

    发明人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Østergaard Nielsen ,  Tino Dyhring ,  Philip K. Ahring

    IPC分类号： A61K31/551 ,  A61K51/04 ,  C07D471/08

    CPC分类号： C07D471/08 ,  A61K51/0468

    摘要： This invention relates to diazabicyclononyl oxadiazolyl derivatives, which are found to-be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Ar1 represents a pyrrolyl group, optionally substituted with alkyl or halo-alkyl.

    摘要翻译： 本发明涉及二氮杂双环壬基恶二唑基衍生物，其被发现是烟碱乙酰胆碱受体的调节剂。 由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。 Ar1表示吡咯基，任选被烷基或卤代烷基取代。

    Diazabicyclic aryl derivatives as cholinergic receptor modulators
    2.
    发明授权
    Diazabicyclic aryl derivatives as cholinergic receptor modulators 失效
    二氮杂双环芳基衍生物作为胆碱能受体调节剂

    公开(公告)号：US08236793B2

    公开(公告)日：2012-08-07

    申请号：US12633505

    申请日：2009-12-08

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Tino Dyhring Jørgensen ,  Daniel B Timmermann

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Tino Dyhring Jørgensen ,  Daniel B Timmermann

    IPC分类号： A61K31/55 ,  C07D243/10

    CPC分类号： C07D471/08

    摘要： This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

    摘要翻译： 本发明涉及新的二氮杂双环芳基衍生物，其在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂中被发现是胆碱能配体。 由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

    NOVEL COMPOUNDS
    4.
    发明申请
    NOVEL COMPOUNDS 审中-公开
    新型化合物

    公开(公告)号：US20120004257A1

    公开(公告)日：2012-01-05

    申请号：US13173178

    申请日：2011-06-30

    申请人： Dan Peters ,  Gordon Munro ,  Elsebet Østergaard Nielsen

    发明人： Dan Peters ,  Gordon Munro ,  Elsebet Østergaard Nielsen

    IPC分类号： A61K31/46 ,  A61P25/04 ,  A61P25/24 ,  C07D451/06 ,  A61P25/00

    CPC分类号： C07D451/06

    摘要： The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

    摘要翻译： 本申请公开了新颖的8-氮杂 - 双环[3.2.1]辛-3-基氧基）色烯-2-酮衍生物及其作为单胺神经递质再摄取抑制剂的用途。 在其它方面，申请公开了这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

    NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES USEFUL AS MODULATOR OF NICOTINIC ACETYLCHOLINE RECEPTORS
    6.
    发明申请
    NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES USEFUL AS MODULATOR OF NICOTINIC ACETYLCHOLINE RECEPTORS 失效
    新的1,4-二氮杂双环[3.2.2]有用的作为非线性乙酰胆碱受体的调节剂的NONYL OXADIAZOLYL衍生物

    公开(公告)号：US20110105478A1

    公开(公告)日：2011-05-05

    申请号：US12921922

    申请日：2009-03-09

    申请人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Østergaard Nielsen ,  Eva Dam Christoffersen

    发明人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Østergaard Nielsen ,  Eva Dam Christoffersen

    IPC分类号： A61K31/551 ,  C07D487/08 ,  A61P25/00 ,  A61P25/28 ,  A61P25/24 ,  A61P25/18 ,  A61P3/04 ,  A61P25/16 ,  A61P29/00 ,  A61P1/00 ,  A61P11/06 ,  A61P17/10

    CPC分类号： C07D471/08

    摘要： This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

    摘要翻译： 本发明涉及1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物的新型N-氧化物及其在制备药物组合物中的用途。 发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体。 由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

    NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
    7.
    发明申请
    NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
    新型4-苄氧基 - 四氢吡啶衍生物及其作为单胺神经递质抑制剂的用途

    公开(公告)号：US20110053984A1

    公开(公告)日：2011-03-03

    申请号：US12921030

    申请日：2009-02-27

    申请人： Dan Peters ,  John Paul Redrobe ,  Elsebet Østergaard Nielsen

    发明人： Dan Peters ,  John Paul Redrobe ,  Elsebet Østergaard Nielsen

    IPC分类号： A61K31/445 ,  C07D211/46 ,  A61P25/00 ,  A61P29/00 ,  A61P13/00 ,  A61P15/00

    CPC分类号： C07D211/46

    摘要： This invention relates to novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydrogen or C1-6-alkyl; Rb and Rc independent of each other represent a phenyl group, which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano, C1-6-alkoxy and methylenedioxo; R′, R″, R′″ and R″″ independent of each other represent C1-6-alkyl; and with the proviso that the compound is not 4-benzhydryloxy-1,2,2,6,6-pentamethyl-piperidine, useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

    摘要翻译： 本发明涉及式（I）的新型4-二苯甲氧基 - 四烷基 - 哌啶衍生物，其任何立体异构体或其立体异构体的任何混合物或其N-氧化物或其药学上可接受的盐，其中R a表示氢或C 1 -6-烷基; Rb和Rc彼此独立地表示苯基，该苯基任选被一个或多个独立地选自卤素，三氟甲基，三氟甲氧基，氰基，C 1-6 - 烷氧基和亚甲基二氧基的取代基取代; R'，R“，R”“和R”“彼此独立地表示C 1-6 - 烷基; 并且条件是该化合物不是4-二苯甲基氧基-1,2,2,6,6-五甲基哌啶，其可用作单胺神经递质再摄取抑制剂。 在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。