ISOXAZOLECARBOXAMIDE DERIVATIVES

摘要

Isoxazolecarboxamide derivatives (I) (R=alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R1 and R2 independently =H, halogen, polyfluoroalkoxy or alkoxy; R3 = one or more substituents selected from H, halogen, alkyl, alkox y, NO2, NH2, NHacyl, CN, alkoxycarbonyl, carboxamido; R4 = H, alkyl or aralkyl; an n is 0, 1 or 2) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and high selectivity toward the .alpha.la adrenergic receptor with respect to the 5-HTlA receptor. This activity profile suggests the use of these derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without sid e effects associated with hypotensive activity being present.