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    N-OXIDES OF 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
    132.
    发明申请
    N-OXIDES OF 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开
    1,4-二氮杂双环[N，N-二氧化物] [3.2.2] NONYL PYRIMIDINYL衍生物有用的非线性乙酰胆碱受体配体

    公开(公告)号：US20120004214A1

    公开(公告)日：2012-01-05

    申请号：US13145287

    申请日：2010-01-20

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

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

    IPC分类号： A61K31/551 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P3/00 ,  A61P3/04 ,  A61P25/16 ,  A61P25/00 ,  A61P25/22 ,  A61P25/08 ,  A61P3/10 ,  A61P25/14 ,  A61P9/06 ,  A61P21/00 ,  A61P9/10 ,  A61P15/06 ,  A61P1/12 ,  A61P11/06 ,  A61P15/10 ,  A61P9/12 ,  A61P29/00 ,  A61P17/00 ,  A61P17/10 ,  A61P1/00 ,  A61P1/04 ,  A61P25/30 ,  A61P25/34 ,  A61P25/36 ,  A61P25/32 ,  C07D487/08

    CPC分类号： C07D471/06

    摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives 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. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy.

    摘要翻译： 本发明涉及新的1,4-二氮杂 - 双环[3.2.2]壬基嘧啶基衍生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。 式（I）其立体异构体或其药学上可接受的盐的立体异构体或其混合物或其药学上可接受的盐，其中Ar表示吲哚基，该吲哚可以任选地被一个或多个取代基取代，所述取代基选自卤素，三氟甲基，三氟甲氧基，氰基，硝基 ，氨基，烷基，羟基和烷氧基。

    NOVEL N-OXIDES OF FURANYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE
    133.
    发明申请
    NOVEL N-OXIDES OF FURANYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE 审中-公开
    新戊氧基 - 二氮杂双环十二烷衍生物的新型N-氧化物及其医药用途

    公开(公告)号：US20110319397A1

    公开(公告)日：2011-12-29

    申请号：US13145998

    申请日：2010-01-25

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

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

    IPC分类号： A61K31/551 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P3/04 ,  A61P25/16 ,  A61P25/14 ,  A61P1/00 ,  A61P29/00 ,  A61P15/00 ,  A61P15/06 ,  A61P1/04 ,  A61P1/12 ,  A61P25/36 ,  A61P25/34 ,  C07D413/14

    CPC分类号： C07D471/08

    摘要： This invention relates to novel N-oxides of certain furanyl-oxadiazolyl-diazabicyclononane derivatives 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 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： 本发明涉及某些呋喃基 - 恶二唑基 - 二氮杂双环壬烷衍生物的新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和单胺受体和转运蛋白的调节剂。 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。

    3-Substituted quinuclidines and their use
    139.
    发明申请
    3-Substituted quinuclidines and their use 审中-公开
    3-取代的奎宁和它们的用途

    公开(公告)号：US20080132704A1

    公开(公告)日：2008-06-05

    申请号：US12004022

    申请日：2007-12-20

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring Jorgensen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring Jorgensen

    IPC分类号： C07D453/02

    CPC分类号： C07D453/02

    摘要： This invention relates to novel 3-substituted quinuclidine 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3-取代的奎宁环衍生物，其被发现是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。 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。