US4439436A
Expired / Lapsed
US
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1,3-Dioxolo(4,5-G)quinoline compounds
Assignee: STWB Inc
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Filing: 1982-08-04
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Granted: 1984-03-27
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Expires: 2002-08-04
Abstract
Abstract Novel 5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acids substituted in the 5-position by lower-alkylamino or di-lower-alkylamino, useful as antibacterial agents, are prepared from 8-hydroxy-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid or a lower-alkyl ester thereof via a series of novel intermediates.
Inventors
- 👤 Mark P. Wentland
- 👤 Denis M. Bailey
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 07:48
CPC Classifications
C; C07; C07D; C07D491/00; C07D491/02; C07D491/04; C07D491/056; A; A61; A61P; A61P31/00; A61P31/04
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
60 words
A compound of the formula ##STR9## where R is hydrogen or alkyl of 1-3 carbon atoms; R' is hydrogen, formyl, alkyl of 1-3 carbon atoms, or alkoxycarbonyl where the alkyl moiety of the latter group is identical with R; and R" is hydrogen or lower-alkyl; or an alkali metal salt or N-methylglucamine salt of a compound where R" is hydrogen.
Claim 2
Dependent Claim
60 words
A compound of the formula ##STR9## where R is hydrogen or alkyl of 1-3 carbon atoms; R' is hydrogen, formyl, alkyl of 1-3 carbon atoms, or alkoxycarbonyl where the alkyl moiety of the latter group is identical with R; and R" is hydrogen or lower-alkyl; or an alkali metal salt or N-methylglucamine salt of a compound where R" is hydrogen.
Claim 3
Dependent Claim
20 words
A compound according to claim 1 where R' and R" are hydrogen, and R is alkyl of 1-3 carbon atoms.
Claim 4
Dependent Claim
6 words
5,8-Dihydro-5-(methylamino)-8-oxo-1,3-dioxolo-[4,5-g]quinoline-7-carboxylic acid, according to claim 2.
Claim 5
Dependent Claim
6 words
5-(Ethylamino)-5,8-dihydro-8-oxo-1,3-dioxolo-[4,5-g]quinoline-7-carboxylic acid, according to claim 2.
Claim 6
Dependent Claim
6 words
5-Amino-5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]-quinoline-7-carboxylic acid, according to claim 1.
Claim 7
Dependent Claim
6 words
5,8-Dihydro-8-oxo-5-(propylamino)-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid, according to claim 2.
Claim 8
Dependent Claim
10 words
A compound according to claim 1 where R' is formyl.
Claim 9
Dependent Claim
6 words
Ethyl 5,8-dihydro-5-[(formyl)methylamino]-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylate, according to claim 7.
Claim 10
Dependent Claim
6 words
Ethyl 5-(formylamino)-5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylate, according to claim 7.
Claim 11
Dependent Claim
6 words
Ethyl 5-[ethyl(formyl)amino]-5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylate, according to claim 7.
Claim 12
Dependent Claim
6 words
5-[(Formyl)methylamino]-5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid, according to claim 7.
Claim 13
Dependent Claim
6 words
5-(Formylamino)-5,8-dihydro-8-oxo-1,3-dioxolo-[4,5-g]quinoline-7-carboxylic acid, according to claim 7.
Claim 14
Dependent Claim
6 words
Ethyl 5-[formyl(propyl)amino]-5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylate, according to claim 7.
Claim 15
Dependent Claim
6 words
Ethyl 5-amino-5,8-dihydro-8-oxo-1,3-dioxolo-[4,5-g]quinoline-7-carboxylate, according to claim 1.
Claim 16
Dependent Claim
6 words
Ethyl 5,8-dihydro-5-[(methoxycarbonyl)methylamino]-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylate, according to claim 1.
Claim 17
Dependent Claim
6 words
Ethyl 5,8-dihydro-5-(methylamino)-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylate, according to claim 1.
Claim 18
Dependent Claim
129 words
The process for preparing a compound of the formula ##STR10## wherein R is alkyl of 1-3 carbon atoms, and R" is hydrogen or lower-alkyl; or an alkali metal salt thereof where R" is hydrogen, which comprises: (a) alkylating a compound of the formula ##STR11## where R' is formyl or hydrogen, with an alkyl halide of 1-3 carbon atoms in the presence of a base when R' is formyl or an alkali metal carbonate when R' is hydrogen to give, respectively, a compound of the formula ##STR12## wherein R is alkyl of 1-3 carbon atoms, R' is formyl and R" is lower-alkyl; and (b) subjecting the resulting compound to alkaline hydrolysis; and, if desired, converting the resulting alkali metal salt of the product to the free acid (R" is hydrogen).
Claim 19
Dependent Claim
129 words
The process for preparing a compound of the formula ##STR10## wherein R is alkyl of 1-3 carbon atoms, and R" is hydrogen or lower-alkyl; or an alkali metal salt thereof where R" is hydrogen, which comprises: (a) alkylating a compound of the formula ##STR11## where R' is formyl or hydrogen, with an alkyl halide of 1-3 carbon atoms in the presence of a base when R' is formyl or an alkali metal carbonate when R' is hydrogen to give, respectively, a compound of the formula ##STR12## wherein R is alkyl of 1-3 carbon atoms, R' is formyl and R" is lower-alkyl; and (b) subjecting the resulting compound to alkaline hydrolysis; and, if desired, converting the resulting alkali metal salt of the product to the free acid (R" is hydrogen).
Claim 20
Dependent Claim
32 words
A composition for treatment of bacterial infections in animals, including humans, which comprises an antibacterially effective amount of a compound according to claim 2, together with one or more pharmaceutically acceptable excipients.
Claim 21
Dependent Claim
14 words
A composition according to claim 18 wherein the antibacterially effective compound is 5,8-dihydro-5-methylamino-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid.
Claim 22
Dependent Claim
35 words
A method for treatment of bacterial infections in animals, including humans, which comprises administering parenterally or orally to an animal or human so infected an antibacterially effective amount of a composition according to claim 18.
Claim 23
Dependent Claim
14 words
A method according to claim 20 wherein the antibacterially active compound is 5,8-dihydro-5-methylamino-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid.
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) | 1987-03-27 | 1987-09-26 | 1988-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-03-27 | 1991-09-26 | 1992-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-03-27 | 1995-09-26 | 1996-03-27 | $7700.00 | Window Closed / Lapsed |