Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-09-09
1997-09-16
Ivy, C. Warren
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
540603, 544129, 544364, 546 19, 546208, 546210, A61K 31445, C07D21146
Patent
active
056682867
DESCRIPTION:
BRIEF SUMMARY
This is the National Stage application of PCT/US95/02972 filed Mar. 14, 1995.
1. Field of Industrial Applicability
The present invention relates to novel oxazolidinone derivatives or pharmaceutically acceptable salts thereof, and pharmaceutical agents that contain them as active ingredients for preventing or treating infectious diseases.
More specifically, the present invention relates to useful antimicrobial agents effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
2. Information Disclosure
International Publication No. WO93/23384 discloses oxazolidinones containing a substituted diazine (piperazine) moiety and their uses as antimicrobials. International Publication No. WO93/09103 discloses substituted aryl and heteroaryl-phenyl-oxazolidinones useful as antimicrobials. International Publication No. WO90/02744 discloses 5'-indolinyl-5.beta.-amidomethyloxazolidinones, 3-(fused-ring substituted)phenyl-5.beta.-amidomethyloxazolidinones, and 3-(nitrogen substituted)-phenyl-5.beta.-amidomethyloxazolidinones which are useful as antibacterial agents.
Other references disclosing various oxazolidinones include U.S. Pat. No. 4,801,600, J. Med. Chem., 32, 1673-81 (1989); J. Med. Chem., 33, 2569-78 (1990); Tetrahedron 45, 1323-26 (1989); and J. Med. Chem., 35, 1156 (1992).
European Patent Publication 352,781 discloses phenyl and pyridyl substituted phenyl oxazolidinones. European Patent Publication 316,594 discloses 3-substituted styryl oxazolidinones. European Patent Publication 312,000 discloses phenylmethyl and pyridylmethyl substituted phenyl oxazolidinones.
SUMMARY OF THE INVENTION
The object of the present invention is to provide novel oxazolidinone derivatives or pharmaceutically acceptable salts thereof which have high antimicrobial activities, and antimicrobial compositions that contain them as active ingredients.
The present inventors conducted intensive studies in order to accomplish the above object. As a result, useful and novel oxazolidinone derivatives were found and the present invention has been accomplished on the basis of the finding.
The present invention provides an oxazolidinone derivative represented by the general formula (I): ##STR2## wherein R is hetero ring having 1-3 hetero atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom; group, a piperazino group, a morpholino group, or a thiomorpholino group, each of which may be substituted by C.sub.1 -C.sub.8 alkyl or --(CH.sub.2).sub.m --OH; and independently substituted by one or more substituents selected from the group consisting of a halogen atom, a hydroxy group, C.sub.1 -C.sub.8 alkoxy group, C.sub.1 -C.sub.8 acyloxy group, an amino group, C.sub.1 -C.sub.8 alkylamino group, C.sub.1 -C.sub.8 dialkylamino group, --CN group and a carboxyl group,
The present invention also provides an antimicrobial agent that contains the oxazolidinone derivative or a pharmaceutically acceptable salt thereof as an effective ingredient. The antimicrobial agent containing the effective ingredient of the present invention can be used for treatment or prevention of infectious diseases. The term "treatment" as used herein means partial or total lessening of symptoms of a disease which a patient suffers from; the term "prevention" as used herein means partial or total avoidance of symptoms of a disease in a patient who, according to a doctor's diagnosis, may suffer from the disease or a related state unless the preventive measure is taken.
This invention provides novel oxazolidinone derivatives useful as preventatives and therapeutics for infectious diseases. The compounds of this invention have excellent antimicrobial action against various human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia s
REFERENCES:
patent: 4476136 (1984-10-01), Dostert et al.
patent: 4891371 (1990-01-01), George et al.
patent: 4948801 (1990-08-01), Carlson et al.
patent: 5523403 (1996-06-01), Barbachyn
patent: 5547950 (1996-08-01), Hutchinson et al.
patent: 5565571 (1996-10-01), Barbachyn et al.
Park, C. et al, J. Med. Chem. 1992, 35, pp. 1156-65.
Munesada Kiyotaka
Taniguchi Mikio
Yamada Hiroyoshi
Dahlen Garth M.
Ivy C. Warren
Pharmacia & Upjohn Company
Welch Lawrence T.
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