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    • 9. 发明授权
    • Piperidine derivative
    • 哌啶衍生物
    • US08377967B2
    • 2013-02-19
    • US12864878
    • 2008-11-20
    • Kunihiko HigashiuraTakashi OginoTaizo ItoHiroyuki Iwatsuki
    • Kunihiko HigashiuraTakashi OginoTaizo ItoHiroyuki Iwatsuki
    • A61K31/4535C07D409/02A61P37/08
    • C07D495/04C07D409/04C07D497/04
    • The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.
    • 本发明提供了具有优异的组胺受体拮抗作用的化合物哌啶衍生物,其可用作药物组合物,特别是抗组胺药的活性成分。 本发明的哌啶衍生物具有有效的组胺受体拮抗作用。 此外,本发明的化合物即使在小鼠口服给药化合物的脑受体结合试验中也显示低脑转移,因此该化合物具有减轻中枢神经系统中的副作用的优选性质,例如嗜睡。 本发明的哌啶衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药例如嗜睡是非常有用的。