US4442109A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-Methylthiomethyl-and 3-methylsulfinylmethyl-4-quinolinones useful for treating hypertension
Assignee: Boots Co PLC
•
Filing: 1981-09-21
•
Granted: 1984-04-10
•
Expires: 2001-09-21
Abstract
Abstract Novel quinolones of the general formula <IMAGE> wherein n is 0, 1 or 2; R1 is C1-4 alkyl; and R3 is hydrogen, C1-4 alkyl, methoxy, methylthio, halo or trifluoromethyl. These compounds have antihypertensive activity and may be used for treating hypertension in mammals. The quinolones are administered in novel therapeutic compositions comprising a quinolone of the above general formula together with a pharmaceutically acceptable carrier. Processes for making the novel quinolones are described.
Inventors
- 👤 Roy V. Davies
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 19:50
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/16; C07D215/20; C07D215/22; C07D215/233; C07D215/18; C07D215/24; C07D215/26; C07D215/36; C07D215/48; C07D215/54; C07D215/56
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
24 words
A quinolone of the formula ##STR11## wherein n is 0 or 1 and R 3 is hydrogen, 7-chloro, 7-fluoro, 7-trifluoromethyl, 6-fluoro, 7-methyl, or 7-bromo.
Claim 2
Dependent Claim
24 words
A quinolone of the formula ##STR11## wherein n is 0 or 1 and R 3 is hydrogen, 7-chloro, 7-fluoro, 7-trifluoromethyl, 6-fluoro, 7-methyl, or 7-bromo.
Claim 3
Dependent Claim
36 words
A quinolone of the formula ##STR12## wherein (a) n is 0 and R 3 is hydrogen, 7-fluoro, 7-trifluoromethyl, 7-methyl, 7-bromo, or 6-fluoro, or (b) n is 1 and R 3 is hydrogen, 7-fluoro, 7-methyl, or 6-fluoro.
Claim 4
Dependent Claim
36 words
A quinolone of the formula ##STR12## wherein (a) n is 0 and R 3 is hydrogen, 7-fluoro, 7-trifluoromethyl, 7-methyl, 7-bromo, or 6-fluoro, or (b) n is 1 and R 3 is hydrogen, 7-fluoro, 7-methyl, or 6-fluoro.
Claim 5
Dependent Claim
12 words
A quinolone as claimed in claim 2 wherein R 3 is hydrogen.
Claim 6
Dependent Claim
30 words
A quinolone of the general formula ##STR13## wherein (a) n is 0 and R 3 is chloro, or (b) n is 1 and R 3 is chloro, bromo, or trifluoromethyl.
Claim 7
Dependent Claim
30 words
A quinolone of the general formula ##STR13## wherein (a) n is 0 and R 3 is chloro, or (b) n is 1 and R 3 is chloro, bromo, or trifluoromethyl.
Claim 8
Dependent Claim
7 words
Compound of claim 4 which is 7-chloro-1-methyl-3-methylthiomethyl-4-quinolone.
Claim 9
Dependent Claim
7 words
Compound of claim 4 which is 7-chloro-1-methyl-3-methylsulphinylmethyl-4-quinolone.
Claim 10
Dependent Claim
7 words
Compound of claim 4 which is 7-bromo-1-methyl-3-methylsulphinylmethyl-4-quinolone.
Claim 11
Dependent Claim
7 words
Compound of claim 4 which is 1-methyl-3-methylsulphinylmethyl-7-trifluoromethyl-4-quinolone.
Claim 12
Dependent Claim
38 words
Therapeutic compositions which comprise an antihypertensive effective amount of a quinolone of the formula ##STR14## wherein (a) n is 0 and R 3 is chloro, or (b) n is 1 and R 3 is chloro, bromo, or trifluoromethyl.
Claim 13
Dependent Claim
38 words
Therapeutic compositions which comprise an antihypertensive effective amount of a quinolone of the formula ##STR14## wherein (a) n is 0 and R 3 is chloro, or (b) n is 1 and R 3 is chloro, bromo, or trifluoromethyl.
Claim 14
Dependent Claim
12 words
A therapeutic composition as claimed in claim 9 in unit dosage form.
Claim 15
Dependent Claim
17 words
A therapeutic composition as claimed in claim 10 in the form of a tablet, capsule, or suppository.
Claim 16
Dependent Claim
17 words
A therapeutic composition as claimed in claim 9 wherein n is 0 and R 3 is chloro.
Claim 17
Dependent Claim
17 words
A therapeutic composition as claimed in claim 9 wherein n is 1 and R 3 is chloro.
Claim 18
Dependent Claim
17 words
A therapeutic composition as claimed in claim 9 wherein n is 1 and R 3 is bromo.
Claim 19
Dependent Claim
17 words
A therapeutic composition as claimed in claim 9 wherein n is 1 and R 3 is trifluoromethyl.
Claim 20
Independent Claim
50 words
A method of treating hypertension in a hypertensive mammal which comprises administering to the hypertensive mammal a therapeutically effective amount of a quinolone of the formula ##STR15## wherein (a) n is 0 and R 3 is chloro, or (b) n is 1 and R 3 is chloro, bromo, or trifluoromethyl.
Claim 21
Independent Claim
50 words
A method of treating hypertension in a hypertensive mammal which comprises administering to the hypertensive mammal a therapeutically effective amount of a quinolone of the formula ##STR15## wherein (a) n is 0 and R 3 is chloro, or (b) n is 1 and R 3 is chloro, bromo, or trifluoromethyl.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-04-10 | 1987-10-10 | 1988-04-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-04-10 | 1991-10-10 | 1992-04-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-04-10 | 1995-10-10 | 1996-04-10 | $7700.00 | Window Closed / Lapsed |