Pyrazol-5-ones

US4032646A · kind A · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

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

Key dates

• Filing date: Sep 4, 1975
• Grant date: Jun 28, 1977
• Expiry date: Sep 4, 1995

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; PA1 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; PA1 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; PA1 Y is a direct bond, oxygen or sulphur, provided that when X is methylene, Y is a direct bond; and PA1 Z is aryl unsubstituted or nuclear substituted by: PA2 A. 3 halogens; PA2 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 alkenox…