Pyrazol-5-ones

US4288446A · kind A · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Eike Moller · Wuppertal, DE
• Karl Meng
• Egbert Wehinger
• Harald Horstmann

Key dates

• Filing date: Dec 12, 1979
• Grant date: Sep 8, 1981
• Expiry date: Dec 12, 1999

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D231/20
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

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: ##STR1## or a pharmaceutically acceptable nontoxic salt thereof wherein R is hydrogen, lower alkyl or amino; PA0 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; PA0 Y is a direct bond, oxygen or sulphur, provided that when X is methylene wherein 1 hydrogen atom is substituted by alkyl of 1 to 4 carbon atoms, Y is a direct bond; PA0 Z is aryl of 6 to 10 carbon atoms unsubstituted or substituted by: PA1 (a) 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, and alkenoxy of 2 to 4 carbon atoms; PA1 (b) lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl,lower alkylsulphamyl, dilower alky…