4-Quinolinones having antihypertensive activity
AssigneeThe Boots Company PLC
InventorsRoy V. Davies, James Fraser, Kenneth J. Nichol, Raymond Parkinson, Malcolm F. Sim, David B. Yates
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AssigneeThe Boots Company PLC
InventorsRoy V. Davies, James Fraser, Kenneth J. Nichol, Raymond Parkinson, Malcolm F. Sim, David B. Yates
Estimating the term…
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 (b) when R.sub.3 and R.sub.4 are hydrogen, R.sub.5 is hydrogen or 7-methyl, and R.sub.1 is ethyl, R.sub.2 contains more than one carbon atom. The specification describes and claims methods of making the compounds and novel intermediates used in such methods.
Quinolone compounds of the general formula ##STR12## wherein n is 0, 1 or 2;
Quinolone compounds of the general formula ##STR13## wherein n is 0, 1 or 2;
7-Fluoro-1-methyl-3-methylsulphinyl-4-quinolone.
Therapeutic compositions suitable for antihypertensive use which comprise as an active ingredient an antihypertensive amount of a quinolone compound of the general formula ##STR14## wherein n is 0, 1 or 2;
Quinolone compounds of the general formula ##STR16## wherein n is 0, 1 or 2, R.sub.2 is C.sub.1-4 alkyl 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, with the proviso that, when R.sub.3, R.sub.4 and R.sub.5 are hydrogen, R.sub.2 contains more than 1 carbon atom.
A method of treating hypertension in a hypertensive warm blooded animal which comprises administering to the hypertensive animal a therapeutically effective amount of a quinolone compound of the formula ##STR17## wherein n is 0, 1, or 2;
Dependencies are inferred from the claim text.