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US4550103A
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Antibacterial 1-oxo-benzoquinolizine-2-carboxylic acids
Assignee: Warner Lambert Co LLC
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Filing: 1984-07-20
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Granted: 1985-10-29
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Expires: 2004-07-20
Abstract
Abstract Novel 10-amino-9-fluoro- and 9-fluoro-6,7-dihydro-5-methyl-1-oxo-8-(heterocyclyl)1H,5H-benzo (ij)-2-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.
Inventors
- 👤 Thomas F. Mich
- 👤 Townley P. Culbertson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 20:48
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/18; C07D207/22; C07D207/24; C07D207/26; C07D207/273; C07D207/277; A; A61; A61P; A61P31/00; A61P31/04; C07D207/04; C07D207/08; C07D207/09; C07D207/10; C07D207/14; C07D455/00; C07D455/03; C07D455/04; C07D487/00; C07D487/02; C07D487/10
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
160 words
A compound of the formula ##STR15## wherein Z is ##STR16## Y is hydrogen or amino; n is 1, 2, 3, or 4; n' is 1, 2, 3, or 4 wherein n+n' is a total of 2, 3, 4, or 5, and n" is 1or 2; R 1 is hydrogen, alkyl having from one to six carbon atoms or a cation; R 3 is hydrogen, alkyl having from one to four carbon atoms or cycloalkyl having three to six carbon atoms; R 4 is hydrogen, alkyl from one to four carbon atoms, hydroxyalkyl having two to four carbon atoms, trifluoroethyl, or R 7 CO-- wherein R 7 is alkyl having from one to four carbon atoms or alkoxy having from one to four carbon atoms; R 5 is hydrogen or alkyl having from one to three carbon atoms; R 6 is hydrogen or alkyl having from one to three carbon atoms; and the pharmaceutically acceptable acid addition or base salts thereof.
Claim 2
Dependent Claim
160 words
A compound of the formula ##STR15## wherein Z is ##STR16## Y is hydrogen or amino; n is 1, 2, 3, or 4; n' is 1, 2, 3, or 4 wherein n+n' is a total of 2, 3, 4, or 5, and n" is 1or 2; R 1 is hydrogen, alkyl having from one to six carbon atoms or a cation; R 3 is hydrogen, alkyl having from one to four carbon atoms or cycloalkyl having three to six carbon atoms; R 4 is hydrogen, alkyl from one to four carbon atoms, hydroxyalkyl having two to four carbon atoms, trifluoroethyl, or R 7 CO-- wherein R 7 is alkyl having from one to four carbon atoms or alkoxy having from one to four carbon atoms; R 5 is hydrogen or alkyl having from one to three carbon atoms; R 6 is hydrogen or alkyl having from one to three carbon atoms; and the pharmaceutically acceptable acid addition or base salts thereof.
Claim 3
Dependent Claim
11 words
A compound as claimed in claim 1, wherein Y is hydrogen.
Claim 4
Dependent Claim
19 words
A compound as claimed in claim 2, wherein R 1 is hydrogen or a pharmaceutically acceptable base salt thereof.
Claim 5
Dependent Claim
11 words
A compound as claimed in claim 3, wherein Z is ##STR17##
Claim 6
Dependent Claim
119 words
A compound of the formula ##STR18## wherein Z is ##STR19## Y is hydrogen or amino; n is 1, 2, 3, or 4; n' is 1, 2, 3, or 4 wherein n+n' is a total of 2, 3, 4, or 5; and n" is 0, 1, or 2; R 3 is hydrogen, alkyl having from one to four carbon atoms or cycloalkyl having from three to six carbon atoms; R 1 is hydrogen, alkyl having from one to six carbon atoms or a cation; R 5 is hydrogen or alkyl having from one to three carbon atoms; R 6 is hydrogen or alkyl having from one to three carbon atoms; and the pharmaceutically acceptable acid addition or base salts thereof.
Claim 7
Dependent Claim
119 words
A compound of the formula ##STR18## wherein Z is ##STR19## Y is hydrogen or amino; n is 1, 2, 3, or 4; n' is 1, 2, 3, or 4 wherein n+n' is a total of 2, 3, 4, or 5; and n" is 0, 1, or 2; R 3 is hydrogen, alkyl having from one to four carbon atoms or cycloalkyl having from three to six carbon atoms; R 1 is hydrogen, alkyl having from one to six carbon atoms or a cation; R 5 is hydrogen or alkyl having from one to three carbon atoms; R 6 is hydrogen or alkyl having from one to three carbon atoms; and the pharmaceutically acceptable acid addition or base salts thereof.
Claim 8
Dependent Claim
40 words
A compound as claimed in claim 1, wherein Y is hydrogen; Z is ##STR20## in which n" is 1 and R 3 is hydrogen, methyl, ethyl, 1- or 2-propyl; R 1 is hydrogen or a pharmaceutically acceptable base salt thereof.
Claim 9
Dependent Claim
36 words
A compound as claimed in claim 5, wherein Y is hydrogen; Z is ##STR21## R 3 is hydrogen, methyl, or ethyl, and R 1 is hydrogen or a pharmaceutically acceptable acid addition or base salt thereof.
Claim 10
Dependent Claim
21 words
A compound as claimed in claim 1 and being 8-[3-[ethylamino)methyl]-1-pyrrolidinyl]-9-fluoro-6,7-dihydro-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid or a pharmaceutically acceptable acid addition or base salt thereof.
Claim 11
Dependent Claim
22 words
A pharmaceutical composition comprising an antibacterially effective amount of a compound as claimed in claim 1 together with a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
22 words
The method of treating bacterial infections in mammals which comprises administering to said mammal a pharmaceutical composition as claimed in claim 9.
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) | 1988-10-28 | 1989-04-29 | 1989-10-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-10-28 | 1993-04-29 | 1993-10-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-10-28 | 1997-04-29 | 1997-10-29 | $7700.00 | Window Closed / Lapsed |