Pyrazolo-benzodiazepine derivs. - used esp. for lowering uric acid levels

摘要

Pyrazole derivs. of formula (I) and their physiologically tolerable salts are new: In (I), R1 is H or, on any available ring position >=1, same or different, 1-4C alkyl, alkoxy or alkylthio, halo, CF3, NO2, COOH, 1-4C alkoxy-carbonyl, di(1-4C) alkylamino or amidino; R2 and R3 are 1-4C alkyl, 5-7C cycloalkyl, benzyl or phenyl, the last opt. substd. by r1; and R3 can also be H; R4 and R5 are H, 1-4C alkyl (opt. substd. by 1-4C-dialkylamino, COOH, 1-4C alkoxycarbonyl or CN), or the gp. CO (CH2)nR6; n = 0-2. R6 is Cl, 1-4C alkoxy (opt. substd. by di(1-4C)alkylamino); or when n = O, it is NH2, opt. acylated or alkylated hydrazino; R6 may also be Nr7R8; R7 and R8 are H, 1-6C alkyl (opt. substd. by OH and/or mono- or di-(1-4C) alkylamino) or together they complete a 5-8 membered ring opt. having a further O, S or N atom (the N opt. substd. by 1-4C alkyl, which can be substd. by OH, ethylenedioxy or trimethylenedioxy or phenyl). (I) esp. have uricosuric and uricostatic activities, sometimes associated with a diuretic effect. They also have analgesic, antiphlogistic, antidepressant and cardiac/circulatory (esp. antiarrhythmic) activities.