Title: Pyrazol-5-ones

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Abstract: Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##SPC1## Or a pharmaceutically acceptable nontoxic salt thereof wherein R is hydrogen, lower alkyl or amino; R.sup.1 is lower alkyl, alkenyl of 2 to 4 carbon atoms, monoaryl or monoaralkyl unsubstituted or substituted in the aryl moiety by 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, halogen, nitro, cyano and trifluoromethyl; X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl; Y is a direct bond, oxygen or sulphur, provided that when X is methylene, Y is a direct bond; and Z is aryl unsubstituted or nuclear substituted by: A. 3 halogens; B. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, cycloalkyl of 5 to 7 carbon atoms and cycloalkenyl of 5 to 7 carbon atoms; C. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2; D. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, halogen, and trifluoromethyl; E. dilower alkylamino, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, or dilower alkylsulphamyl wherein the nitrogen atom is a member of 5-, 6- or 7-membered heterocyclic ring or said ring which contains oxygen as an additional ring member; or F. a fused, saturated or unsaturated 5-, 6- or 7-membered ring or said ring which additionally contains 1 or 2 oxygen atoms or 1 sulphur atom, With a pharmaceutically acceptable nontoxic inert diluent or carrier. The compositions are preferably administered orally or parenterally and in the latter case, sterile or isotonic aqueous solutions are preferred.


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