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US4861779A
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Anti-bacterial substituted bridged-diazabicycloalkyl quinolone carboxylic acids
Assignee: Pfizer Inc
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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 16:34
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.
References Cited (Backward Citations)
US4146719A
Cited
US4292317A
Cited
JPS54112876A
Cited
US4448962A
Cited
US4382892A
Cited
JPS5823381A
Cited
JPS5823382A
Cited
JPS58204193A
Cited
US4499091A
Cited
JPS58204194A
Cited
JPS58219293A
Cited
JPS59137481A
Cited
EP0131839A1
Cited
US4571396A
Cited
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 |