Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-06-25
1989-08-08
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546156, 546153, A61K 3147, C07D21556
Patent
active
048552917
ABSTRACT:
Quinolones of the formula I ##STR1## in which the dotted line between positions 2 and 3 of the quinolone ring represents an optional bond; R is hydrogen or lower alkyl; R.sub.1 is lower alkyl; and R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, halo, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, trifluoromethyl, cyano, fluorinated lower alkoxy, phenyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, lower alkylthio, halo and trifluoromethyl, the group --OAr or the group --S(O).sub.n Ar in which Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, lower alkylthio, halo and trifluoromethyl and n is 0, 1 or 2, or the group --NR.sub.5 R.sub.6 or the N-oxide thereof in which R.sub.5 and R.sub.6, which may be the same or different, are lower alkyl or, together with the nitrogen atom to which they are attached, form a 5-7 membered ring optionally containing an additional hetero atom selected from oxygen, nitrogen and sulphur have utility as antihypertensive agents.
Novel quinolones are those of the above-defined formula I, provided that (a) when the optional 2,3-bond is present R.sub.1 is methyl and R is hydrogen, at least one of R.sub.2, R.sub.3 and R.sub.4 is other than hydrogen and (b) when the optional 2,3-bond is present, R is lower alkyl and R.sub.3 and R.sub.4 are hydrogen, R.sub.2 is other than hydrogen or lower alkoxy.
Pharmaceutical compositions comprising a novel quinolone of the above formula I together with a pharmaceutically acceptable carrier are described and claimed.
Processes for preparing the novel quinolones are also described.
REFERENCES:
patent: 4302460 (1981-11-01), Davies et al.
patent: 4442109 (1984-04-01), Davies
patent: 4450167 (1984-05-01), LeMartret et al.
patent: 4596807 (1986-06-01), Crosby
patent: 4610991 (1986-09-01), Bailey
patent: 4659718 (1987-04-01), Davies et al.
patent: 4671959 (1987-06-01), Warren et al.
patent: 4772614 (1988-09-01), Davies et al.
patent: 4786644 (1988-11-01), Glamrowski et al.
Nakanishi et al., Derwent Abstract for Japanese Patent, (vol. 8), #44/12143, (6/2/69).
Kozello et al., Pharmaceutical Chemistry Journal, (Khimiko-Farmatsevticheski Zhurnal), vol. 5, pp. 21-22, (1971).
Erickson et al., J. of Med. Chem., vol. 22, pp. 816-823, (1979).
"Medicinal Chemistry", (2nd Ed.), Alfred Berger, Editor, Interscience Publishers (N.Y.), p. 43, (1960).
Abstract for EP 70767, (7/17/81).
Abstract for EP 40573, (11/25/81).
Abstract for JP 54/88276, (7/13/79).
Abstract for BE 814843, (11/12/74).
Abstract for FR 2193822, (3/29/74).
Abstract for DT 1908548, (11/5/70).
Abstract for FR 2532314, (3/2/84).
Abstract for JP 58/148817, (9/15/83).
Abstract for JP 58/148861, (9/5/83).
Abstract for BE 892148, (8/16/82).
Beinhardt E.
Daus Donald G.
The Boots Company PLC
LandOfFree
1,4dihydroquinoline-3-carboxamides does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 1,4dihydroquinoline-3-carboxamides, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1,4dihydroquinoline-3-carboxamides will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-905727