BENZOPYRAN DERIVATIVES
    98.
    发明公开
    BENZOPYRAN DERIVATIVES 有权
    苯并吡喃衍生物

    公开(公告)号:EP1222183A1

    公开(公告)日:2002-07-17

    申请号:EP00975868.1

    申请日:2000-10-16

    CPC分类号: C07D311/24 C07D311/30

    摘要: Benzopyran derivatives (I) (R = phenyl, alkoxycarbonyl, alkylcarbonyl, CONH2, CONH(alkyl), CON(alkyl)2, CN or alkoxycarbonylamino; R2 = alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R4 and R5 independently = H, halogen, polyfluoroalkyl, polyfluoroalkoxy, CN or CONH2; n is 0, 1 or 2; but if R = Ph and both of R4 and R5 = H or hologen atoms, then R2 = polyfluoroalkoxy or CF3SO2O) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and, in particular, with high selectivity for the α1-adrenergic receptor as compared to the 5-HT1A receptor. This activity profile suggests the use of these benzopyran derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side-effects associated with hypotensive activity.