Single pot process for producing (Z)-azabicyclo oxime ethers
    12.
    发明授权
    Single pot process for producing (Z)-azabicyclo oxime ethers 失效
    用于生产(Z) - 氮杂双环肟醚的单罐方法

    公开(公告)号:US6121459A

    公开(公告)日:2000-09-19

    申请号:US355227

    申请日:1999-12-23

    CPC分类号: C07D487/08 C07D453/02

    摘要: Biologically active O-substituted azabicyclo oximes having the Z configuration may be isolated simply, without chromatographic separation, and in high yield and Z/E purity through the coupling of a 1-azabicyclo-3-one with an O-substituted hydroxylamine in acidic aqueous solution and conversion of E-configured isomer to Z-isomer without requiring purification or separation. Neutralization and subsequent isolation of the free base followed by precipitation of the salt allows separation of the Z-isomer with high Z/E purity.

    摘要翻译: PCT No.PCT / US97 / 23872 Sec。 371 1999年12月23日第 102(e)1999年12月23日PCT 1997年12月29日PCT PCT。 出版物WO98 / 32758 日期1998年7月30日具有Z构型的生物活性O-取代的氮杂双环肟可以简单地分离,无色谱分离,通过1-氮杂双环-3-酮与O- 在酸性水溶液中取代羟胺,并将E构型异构体转化为Z-异构体,无需纯化或分离。 中和并随后分离游离碱,随后沉淀盐允许以高Z / E纯度分离Z-异构体。

    Substituted tetrazoles and derivatives thereof acting at muscarinic
receptors
    14.
    发明授权
    Substituted tetrazoles and derivatives thereof acting at muscarinic receptors 失效
    作用于毒蕈碱受体的取代的四唑及其衍生物

    公开(公告)号:US5200419A

    公开(公告)日:1993-04-06

    申请号:US526423

    申请日:1990-05-21

    IPC分类号: C07D453/02

    CPC分类号: C07D453/02

    摘要: Substituted tetrazoles and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.

    摘要翻译: 描述了取代的四唑及其衍生物,以及其制备方法及其药物组合物,其可用作中枢作用毒蕈碱药,并且可用作治疗疼痛的止痛剂,作为睡眠辅助剂和用于治疗 老年性痴呆,老年痴呆症,亨廷顿氏舞蹈症,迟发性运动障碍,运动过度,躁狂症或类似脑功能不全的症状,特征在于脑乙酰胆碱生成或释放的症状。

    Diphenylmethylene piperidines
    16.
    发明授权
    Diphenylmethylene piperidines 失效
    二苯基亚甲基哌啶

    公开(公告)号:US4540780A

    公开(公告)日:1985-09-10

    申请号:US500344

    申请日:1983-06-02

    摘要: Novel chemical compounds which are diphenylmethylene piperidine compounds are provided, as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. The compounds have both anticholinergic and antidopaminergic properties, and are useful as antiemetic, antihistamine, pulmonary, antiallergy, and antispasmodic agents.

    摘要翻译: 提供了作为二苯基亚甲基哌啶化合物的新型化合物,以及其制备方法,包含该化合物的药物组合物,以及以剂型形式使用该化合物的方法。 该化合物具有抗胆碱能药和抗癌剂能力,可用作止吐药,抗组胺药,肺,抗过敏药和解痉药。