Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1986-06-13
1988-09-20
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546153, 546155, 546156, 560 46, 548485, 562453, 564 86, 564194, C07D21536, A61K 3147
Patent
active
047726148
ABSTRACT:
Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease.
With the exception of the three compounds 1-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimethoxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel.
Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.
REFERENCES:
patent: 4302460 (1981-11-01), Davies et al.
patent: 4442109 (1984-04-01), Davies et al.
patent: 4447435 (1984-05-01), Davies et al.
patent: 4552884 (1985-11-01), Sim et al.
patent: 4659718 (1987-04-01), Davies et al.
Derwent Abstract 23901V for Japan Patent No. 49-13185 (2/5/74).
Yanagisawa et al., Chem. Pharm. Bull. 21(5), pp. 1080-1089 (1973).
Liebigs Annalen Der Chemie (1978) pp. 617-626.
Davies Roy V.
Fraser James
Nichol Kenneth J.
Bernhardt E.
Daus Donald G.
The Boots Company
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