The Boots Company Plc

Malcolm F Sim

Kenneth J Nichol

David B Yates

Roy V Davies

Norman William Bristow

James Fraser

Peter E Macey

Raymond Parkinson

A method for the treatment of heart failure in a mammal comprises the administration to the mammal of a quinolone of the general formula I, ##STR1## wherein m is 0 or 1; n is 0, 1 or 2; and R is hydrogen, halo, methyl or trifluoromethyl. A preferred method of the invention comprises the treatment of chronic heart failure in a mammal by the oral administration of a quinolone of formula I. Preferred compounds of formula I are 7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone and 1-methyl-3-methylsulphonylmethyl-4-quinolone.

Method of treating heart disease

Compositions which contain a quinolone compound of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is lower alkyl optionally substituted by hydroxy or C.sub.1-4 alkoxycarbonyl; allyl; propynyl or phenyl- lower alkyl in which the phenyl ring is optionally substituted by 1 or 2 C.sub.1-4 alkoxy groups; R.sub.2 is C.sub.1-4 alkyl with the proviso that when n is 0, R.sub.2 is methyl; and R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, halo, trifluoromethyl or lower alkylthio show antihypertensive activity. Compounds of general formula ##STR2## in which n, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as described above are novel subject to the following provisos (a) when R.sub.3, R.sub.4 and R.sub.4 and R.sub.5 are hydrogen R.sub.2 is methyl and R.sub.1 is lower alkyl, R.sub.1 contains more than one carbon atom, and

4-Quinolinones having antihypertensive activity

Therapeutic activity, and in particular the ability to induce diuresis or saluresis, has been discovered in 4-hydroxy- or 4-mercapto-2-aryl-1,2-dihydrophthalazine-1-acetic acids, the tautomers of these namely 4-oxo or thio-2-aryl-1,2-tetrahydrophthalazine-1-acetic acids, and in the ester and alcohol derivatives of the acids, and in the acyl derivatives of the 4-hydroxy or mercapto compounds and in the 3-alkyl derivatives of the 4-oxo or thio compounds. Therapeutic compositions and methods using the compounds are described, as also are novel compounds.

Therapeutic agents

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Woodborough, United Kingdom

Malcolm F Sim