1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as modulator of nicotinic acetylcholine receptors
    91.
    发明授权
    1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as modulator of nicotinic acetylcholine receptors 失效
    可用作烟碱乙酰胆碱受体调节剂的1,4-二氮杂双环[3.2.2]壬基恶二唑基衍生物

    公开(公告)号:US08106042B2

    公开(公告)日:2012-01-31

    申请号:US12921922

    申请日:2009-03-09

    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。

    Aryl ureido benzoic acid derivatives and their use
    97.
    发明授权
    Aryl ureido benzoic acid derivatives and their use 失效
    芳基脲基苯甲酸衍生物及其用途

    公开(公告)号:US07521480B2

    公开(公告)日:2009-04-21

    申请号:US10535683

    申请日:2003-11-10

    摘要: This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

    摘要翻译: 本发明涉及可用作离子型GluR5受体的选择性和非竞争性拮抗剂的新型芳基脲基苯甲酸衍生物。 由于其生物学活性,本发明的芳基脲基衍生物被认为可用于治疗对天冬氨酸或谷氨酸受体的调节有反应的疾病。 此外,本发明提供了根据本发明使用的化合物,以及包含化合物的药物组合物,以及治疗对天冬氨酸或谷氨酸受体的调节作用的疾病或病症或病症的方法。

    Indolyl-oxadiazolyl-diazabicyclononane derivatives and their medical and diagnostical use
    98.
    发明授权
    Indolyl-oxadiazolyl-diazabicyclononane derivatives and their medical and diagnostical use 有权
    吲哚基 - 恶二唑基 - 二氮杂双环壬烷衍生物及其医疗和诊断用途

    公开(公告)号:US08778928B2

    公开(公告)日:2014-07-15

    申请号:US13145979

    申请日:2010-01-25

    IPC分类号: C07D413/14 A61K31/551

    摘要: This invention relates to novel indolyl-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: 本发明涉及新的吲哚基 - 恶二唑基 - 二氮杂双环壬烷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。