Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-10-12
2002-09-24
Weddington, Kevin E. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S300000, C514S311000
Reexamination Certificate
active
06455540
ABSTRACT:
This invention relates, in part, to newly identified methods of using quinolone antibiotics, particularly a gemifloxacin compound against anaerobic bacteria, especially unusual anaerobic bacteria.
BACKGROUND OF THE INVENTION
Quinolones have been shown to be effective to varying degrees against a range of certain anaerobic pathogens. However, as diseases caused by these pathogens are on the rise, there exists a need for antimicrobial compounds that are more potent than the present group of quinolones.
Gemifloxacin mesylate (SB-265805) is a novel fluoroquinolone useful as a potent antibacterial agent. Gemifloxacin compounds are described in detail in patent application PCT/KR98/00051 published as WO 98/42705. Patent application EP 688772 discloses novel quinoline(naphthyridine)carboxylic acid derivatives, including anhydrous (R,S)-7-(3-aminomethyl-4-methoxyiminopyrrolidin- 1 -yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid of formula I.
PCT/KR98/00051 discloses (R,S)-7-(3-aminomethyl4-syn-methoxyimino-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof including the sesquihydrate.
While in vitro testing of new antimicrobial compounds is often extensive, these studies tend to focus on a limited range of typical anaerobic bacterial pathogens (Cormicon, et al.,
Antimicrob. Agents Chemother.,
41:204-211, 1997; Hohl, et al.,
Clin. Microbiol. Infect.,
4:280-284, 1998; Marco, et al.,
J. Antimicrob. Chemother.,
40:605-607, 1997). Moreover, it has been reported that (Goldstein, et al.,
Antimicrob. Agents Chemother.,
Submitted) the activity of gemifloxacin against typical anaerobic bacteria; it showed activity against
Bacteroides fragilis
and certain Prevotella and Porphyromonas strains, but only limited activity against
B. thetaiotaomicron, B. distasonis
and
B. ovatus.
Data is lacking about the activities of new quinolone compounds against many of the less frequently encountered anaerobic pathogens, such as Actinomyces spp., Anaerobiospirrilum spp., Porphyromonas spp., and
Bilophila wadsworthia.
Provided herein is an invention based, in part, on a significant discovery made using a gemifloxacin compound against various unusual, though medically impotant, anaerobic bacteria, demonstrating the activity of the gemifloxacin compound used was superior to a number of quinolones as described in more detail herein. Gemifloxacin compounds are valuable compounds for the treatment of bacterial caused by a range of anaerobic pathogens, including those resistant to usual oral therapy, thereby filling an unmet medical need.
SUMMARY OF THE INVENTION
An object of the invention is a method for modulating metabolism of anaerobic pathogenic bacteria comprising the step of contacting anaerobic pathogenic bacteria with an antibacterially effective amount of a composition comprising a quinolone, particularly a gemifloxacin compound, or an antibacterially effective derivative thereof.
A further object of the invention is a method wherein said anaerobic pathogenic bacteria is selected from the group consisting of: a member of the genus Peptostreptococci, a
Peptostreptococci asaccharolyticus,
a
Peptostreptococci magnus,
a
Peptostreptococci micros,
a
Peptostreptococci prevotii,
a
Porphyromonas asaccharolytica,
a
Porphyromonas canoris,
a
Porphyromonas gingivalis,
a
Porphyromonas macaccae,
a member of the genus Actinomyces, an
Actinomyces israelii,
an
Actinomyces odontolyticus,
a member of the genus Clostridium, a
Clostridium innocuum,
a
Clostridium clostridioforme,
a
Clostridium difficile,
a member of the genus Anaerobiospirillum, a
Bacteroides tectum,
a
Bacteroides ureolyticus,
a
Bacteroides gracilis
(
Campylobacter gracilis
), a
Prevotella intermedia,
a
Prevotella heparinolytica,
a
Prevotella oris
-
buccae,
a
Prevotella bivia,
a
Prevotella melaninogenica,
a member of the genus Fusobacterium, a
Fusobacterium naviforme,
a
Fusobacterium necrophorum,
a
Fusobacterium varium,
a
Fusobacterium ulcerans,
a
Fusobacterium russii,
a member of the genus Bilophila, a
Bilophila wadsworthia.
Also provided by the invention is a method of treating or preventing a bacterial infection by anaerobic pathogenic bacteria comprising the step of administering an antibacterially effective amount of a composition comprising a quinolone, particularly a gemifloxacin compound to a mammal suspected of having or being at risk of having an infection with anaerobic pathogenic bacteria.
A preferred method is provided wherein said modulating metabolism is inhibiting growth of said bacteria or killing said bacteria.
A further preferred method is provided wherein said contacting said bacteria comprises the further step of introducing said composition into a mammal, particularly a human.
Further preferred methods are provided by the invention wherein said bacteria is selected from the group consisting of: a member of the genus Peptostreptococci, a
Peptostreptococci asaccharolyticus,
a
Peptostreptococci magnus,
a
Peptostreptococci micros,
a
Peptostreptococci prevotii,
a member of the genus Porphyromonas, a
Porphyromonas asaccharolytica,
a
Porphyromonas canoris,
a
Porphyromonas gingivalis,
a
Porphyromonas macaccae,
a member of the genus Actinomyces, an
Actinomyces israelii,
an
Actinomyces odontolyticus,
a member of the genus Clostridium, a
Clostridium innocuum,
a
Clostridium clostridioforme,
a
Clostridium difficile,
a member of the genus Anaerobiospirillum, a member of the genus Bacteroides, a
Bacteroides tectum,
a
Bacteroides ureolyticus,
a
Bacteroides gracilis
(
Campylobacter gracilis
), a member of the genus Prevotella, a
Prevotella intermedia,
a
Prevotella heparinolytica,
a
Prevotelia oris
-
buccae,
a
Prevotella bivia,
a
Prevotella melaninogenica,
a member of the genus Fusobacterium, a
Fusobacterium naviforme,
a
Fusobacterium necrophorum,
a
Fusobacterium varium,
a
Fusobacterium ulcerans,
a
Fusobacterium russii,
a member of the genus Bilophila, a
Bilophila wadsworthia.
Various changes and modifications within the spirit and scope of the disclosed invention will become readily apparent to those skilled in the art from reading the following descriptions and from reading the other parts of the present disclosure.
DESCRIPTION OF THE INVENTION
The present invention provides, among other things, methods for using a composition comprising a quinolone, particularly a gemifloxacin compound against anaerobic bacteria.
As used herein “gemifloxacin compound(s)” means a compound having antibacterial activity described in patent application PCT/KR98/00051 published as WO 98/42705, or patent application EP 688772.
This invention was based, in part, on analyses evaluating the comparative activity of gemifloxacin against various anaerobic pathogens. Since anaerobic susceptibility testing is not routinely performed in most clinical laboratories, if it is performed at all, the clinician must rely on published studies to help guide both empirical therapy as well as specific therapy in situations that involve less commonly isolated or identified anaerobes or mixed infections at other sites. Most in vitro studies of gemifloxacin against anaerobic bacteria focus their attention on common intra-abdominal pathogens such as
Bacteroides fragilis
and
Clostridium perfringens
or lump the anaerobes into large groups without speciation (Cormicon, et al., Antimicrob. Agents Chemother., 41:204-211, 1997; Marco, et al.,
J. Antimicrob. Chemother.,
40:605-607, 1997). Consequently there is unmet medical need for data regarding certain species often recovered from respiratory and gynecological infections as well as less frequently identified components of mixed abdominal infections, as well as methods used for ther treatment of such pathogens.
The present invention was based, in part, on analyses showing that gemifloxacin compared favorably with trovafloxacin against the Gram-positive anaerobes tested as well as the other unusual isolates studied &
Citron Diane M.
Goldstein Ellie J. C.
Gimmi Edward R.
Henderson Loretta J.
Kinzig Charles M.
SmithKline Beecham Corporation
Weddington Kevin E.
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