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6 条记录 (耗时 0.022 秒)

    New imidazopyridines as serotonergic 5-HT3 antagonists
    1.
    发明公开
    New imidazopyridines as serotonergic 5-HT3 antagonists 失效
    咪唑并吡啶al-serotonergische 5-HT3拮抗剂。

    公开(公告)号：EP0504679A1

    公开(公告)日：1992-09-23

    申请号：EP92103862.6

    申请日：1992-03-06

    申请人： G.D. Searle & Co.

    发明人： Becker, Daniel P. ,  Flynn, Daniel L. ,  Moormann, Alan Edward ,  Nosal, Roger ,  Villamil, Clara I.

    IPC分类号： C07D519/00 ,  C07D471/04 ,  A61K31/435

    CPC分类号： C07D471/04

    摘要： The imidazopyridines of formula
    wherein Ar represents a radical of the formula

    Z represents a radical of the formula

    The compounds are seterotonergic 5-HT₃ antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT₃ receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utillity as enhancers of nasal absoption of bioactive compounds.

    摘要翻译： 下式的咪唑并吡啶其中Ar表示式CHEM> Z的基团表示下式的基团。化合物是稳定性能的5-HT 3拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑，精神病，抑郁症（特别是伴有焦虑症的抑郁症），认知障碍，药物滥用依赖和戒断，胃肠蠕动窒息（包括食管反流，消化不良，胃潴留，肠易激惹） 综合征），化疗引起的呕吐和内脏痛。 此外，本发明的化合物可以发现作为生物活性化合物鼻吸收的增强剂。

    New meso-azacyclic aromatic acid amides and esters as novel serotonergic agents
    3.
    发明公开
    New meso-azacyclic aromatic acid amides and esters as novel serotonergic agents 失效
    咔唑che che che che che che。。。。。。。。。。。。。。。。

    公开(公告)号：EP0504680A1

    公开(公告)日：1992-09-23

    申请号：EP92103863.4

    申请日：1992-03-06

    申请人： G.D. Searle & Co.

    发明人： Becker, Daniel P. ,  Flynn, Daniel L. ,  Moormann, Alan Edward ,  Nosal, Roger ,  Villamil, Clara I.

    IPC分类号： C07D487/04 ,  C07D487/08 ,  C07D471/08 ,  A61K31/40 ,  A61K31/435 ,  A61K31/55 ,  A61K31/53 ,  A61K31/505 ,  A61K31/415

    CPC分类号： C07D471/08 ,  C07D487/04 ,  C07D487/08

    摘要： The meso-azacyclic aromatic acid amides and esters of formula

    where Ar represents a radical of the formula:

    X is NH od O; and Z represents a radical of the formula:

    are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrom, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT₃ receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT₃ reseptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

    摘要翻译： 内消旋 - 氮杂环芳香酰胺和式的酯，其中Ar表示下式的基团：其中X是O， Z表示下式的基团：可用于治疗中枢神经系统和胃肠动力障碍，例如胃食管反流，非溃疡性消化不良，胃排空迟缓，肠梗阻，肠易激综合征等。 此外，本发明的化合物可用作5-羟色胺5-HT 3受体的拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗剂的拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑，精神病，抑郁症（特别是伴有焦虑症的抑郁症），认知障碍，药物滥用依赖和/或戒断，肠易激综合征，化疗药物引起的呕吐和内脏痛 。 此外，本发明的化合物可用作生物活性化合物的鼻吸收增强剂。