US4861779A
Expired / Lapsed
US
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Anti-bacterial substituted bridged-diazabicycloalkyl quinolone carboxylic acids
Assignee: Pfizer Inc
•
Filing: 1986-08-19
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Granted: 1989-08-29
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Expires: 2006-08-19
Abstract
Abstract Antibacterial compounds have the formula ##STR1## wherein R 1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R 2 is a bridged-diazabicycloalkyl group.
Inventors
- 👤 Martin R. Jefson
- 👤 Paul R. Mc Guirk
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 11:38
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/08; A; A61; A61P; A61P31/00; A61P31/04; C07D487/00; C07D487/02; C07D487/08; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
43 words
A compound of the formula ##STR22## or a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is hydrogen, a pharmaceutically acceptable cation, or (C 1 -C 6 )alkyl; Y 3 is cyclopropyl; and R 8 is 8-methyl-3,8-diazabicyclo[3.2.1]oct-3-yl, (1S, 4S)-2,5-diazabicyclo[2.2.1]hept-2-yl, or (1S, 4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl.
Claim 2
Dependent Claim
43 words
A compound of the formula ##STR22## or a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is hydrogen, a pharmaceutically acceptable cation, or (C 1 -C 6 )alkyl; Y 3 is cyclopropyl; and R 8 is 8-methyl-3,8-diazabicyclo[3.2.1]oct-3-yl, (1S, 4S)-2,5-diazabicyclo[2.2.1]hept-2-yl, or (1S, 4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl.
Claim 3
Dependent Claim
11 words
A compound according to claim 1, wherein R 7 is hydrogen.
Claim 4
Dependent Claim
13 words
A compound according to claim 1, wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-(8-methyl-3,8-diazabicyclo[3.2.1]oct-3-yl)-4-oxo-3-quinoline carboxylic acid.
Claim 5
Dependent Claim
13 words
A compound according to claim 1, wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-4-oxo-3-quinoline carboxylic acid.
Claim 6
Dependent Claim
13 words
A compound according to claim 1, wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo-[2.2.1]hept-2-yl]-4-oxo-3-quinoline carboxylic acid.
Claim 7
Dependent Claim
15 words
A compound according to claim 1 wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-(8-methyl-3,8-diaza-bicyclo[3.2.1]oct-3-yl)-4-oxo-3-quinoline carboxylic acid hydrochloride salt.
Claim 8
Dependent Claim
15 words
A compound according to claim 1, wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-(8-methyl-3,8-diazabicyclo[3.2.1]oct-3-yl)-4-oxo-3-quinoline carboxylic acid methanesulfonate salt.
Claim 9
Dependent Claim
25 words
An antibacterial composition comprising a compound according to claim 1 in an amount sufficient for treatment of a bacterial disease, and a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
11 words
A composition according to claim 8 wherein R 7 is hydrogen.
Claim 11
Dependent Claim
13 words
A composition according to claim 8 wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-4-oxo-3-quinoline carboxylic acid.
Claim 12
Dependent Claim
13 words
A composition according to claim 8 wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-4-oxo-3-quinoline carboxylic acid.
Claim 13
Dependent Claim
15 words
A composition according to claim 8 wherein said compound is 1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-4-oxo-3-quinoline carboxylic acid methanesulfonate salt.
Claim 14
Dependent Claim
15 words
A composition according to claim 8 wherein R 7 is (C 1 -C 6 )alkyl.
Claim 15
Dependent Claim
13 words
A composition according to claim 8 wherein R 7 is methyl or ethyl.
Claim 16
Dependent Claim
28 words
A method of treating a host affected by a bacterial infection which comprises administering to said host an antibacterially effective amount of a compound according to claim 1.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-28 | 1993-02-27 | 1993-08-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-28 | 1997-02-27 | 1997-08-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-28 | 2001-02-27 | 2001-08-29 | $7700.00 | Window Closed / Lapsed |