Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-09-09
2000-08-15
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142292, 544 66, A61K 31535, C07D27300, C07D27304
Patent
active
061037168
DESCRIPTION:
BRIEF SUMMARY
EP-A-0 259 804 describes the compound of formula (A): ##STR2## (9-fluoro-3-methyl-10(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido [3,2,1-ij]-1,3,4-benzadiazine-6-carboxylic acid, or marbofloxacin). The compound of formula (A) is reported to have antibacterial activity.
The present invention provides the compound of formula (I): ##STR3##
The compound of formula (I) has antibacterial activity and is therefore of use in the treatment and prophylaxis of bacterial infections in humans and animals.
The invention in a second aspect, further provides a process for the production of the compound of formula (I), which comprises treating the compound of formula (A) with an oxidizing agent, more especially an excess of hydrogen peroxide in the presence of an aqueous inorganic base. The process is typically carried out at ambient temperature and monitored by tlc. After filtration, the reaction is quenched by neutralization to pH6. The product is collected by slow filtration, washed, and stored in the dark.
The compound according to the invention is suitably provided in substantially pure form, for example at least 50% pure, suitable at least 60% pure, advantageously at least 75% pure, preferably at least 85% pure, more preferably at least 95% pure, especially at least 98% pure, all percentages being calculated as weight/weight. An impure or less pure form of the compound according to the invention may, for example, be used in the preparation of a more pure form of the same compound.
The compound of the invention has antibacterial activity and is useful for the prophylactic and therapeutic treatment of bacterial infections in animals especially mammals, including humans, in particular humans and domesticated animals (including farm animals). The compound may be used for the treatment of infections caused by, among, other organisms, species of Staphylococcus. Streptococcus, Aerococcus, Enterococcus, Micrococcus, Kactobacillus, Bifidobacterium, Clostndium, Eubacterium, Peptococcus, Peptostreptococcus, Propionibacterium, Citrobacter, Campylobacter, Enterobacter, Klebsiella, Proteus, Pseudomonas. Serratia, Salmonella, Shigella, Vibrio, Aeromonas, Haemophilus, Neisseria, Acinetobacter, Alcaligenes, Bordetella, Bacteroids, Fusobacterium, Myocoplasma and other microorganisms.
Accordingly a third aspect of the invention provides the compound of formula (I) for use in medical therapy, in particular for use as an antibacterial agent.
The invention further provides a method of treating a human or animal suffering from a bacterial infection by the administration of an effective amount of the compound of the invention.
A particular method of the invention comprises treating or preventing bacterial infections in non-human animals, more particularly domesticated mammals and birds, such as horses, cattle, swine, sheep, companion animals including dogs and cats, and poultry including chickens. The method comprises administering to the animal via the oral route an antibacterially effective amount of a compound of formula (I):
A further aspect of the invention provides use of a compound of formula (I) in the manufacture of a medicament for use in the treatment or prevention of bacterial infections in non-human animals by administration via the oral route.
The invention further provides a pharmaceutical composition comprising a compound of the formula (I) together with a pharmaceutically acceptable diluent or carrier.
The compound of the invention can be administered alone, but will generally be administered in admixture with a pharmaceutical carrier selected with regard to the intended route of administration and standard pharmaceutical practice. For example, it may be administered orally in the form of a tablet containing such excipients as starch or lactose, or in a capsule or ovule either alone or in admixture with excipients, or in the form of an elixir or suspension containing a flavouring or colouring agent It may be injected parenterally, for example, intravenously, intramuscularly or subcutaneously. For parenteral administr
REFERENCES:
patent: 4801584 (1989-01-01), Yokose et al.
Dorgan Roderick John
Gottschall David Walter
Donahue E. Victor
Ginsburg Paul H.
Pfizer Inc.
Richardson Peter C.
Schroeder Ben
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