1-Subst-pyrazol-5-ones - with diuretic saluretic, antihypertensive and antithrombotic activity

摘要

Cpds. of formula (I) and their acid-addn. salts (where R is H, NH2; R' is H, alkyl, alkenyl, aryl, aralkyl; X is -CH2-CH2- opt. substd. on one or both C-atoms by alkyl and opt. attached to the gp. R2 by an O or S atom; or X is -CH2:CH:CH- in which each C-atom may be substd. by alkyl; or X is opt. substd. methylene provided that when R is NH2, R' is not H; R2 is aryl opt. substd. by one or two halo, CF3, alkyl, alkenyl, alkoxy, or R2 is substd. by one alkylamino, CN, -OCF3, NO2, -CONH2, -SO2NH2 or the gp. SOn-alkyl where n is 0, 1 or 2, and also opt. substd. by one or two alkyl, alkenyl, alkoxy, halo, CF3; or two of the substits. of the aryl gp. R2 may form a 5 to 7-membered opt. satd. ring opt. contg. one or two O or S-atoms) have diuretic saluretic, antihypertensive and antithrombotic activity. Oral doses of 3mg/kg are effective in dogs. Dosage is pref. 0.1-10mg/kg/day parenterally and 0.5-100mg/kg/day orally.