Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-10-31
1996-08-20
Gibson, Sharon
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514255, 544369, C07D41300, A61K 31495
Patent
active
055479502
ABSTRACT:
A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is chosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are 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.
REFERENCES:
patent: Re29934 (1979-03-01), Fauran et al.
patent: 3941789 (1976-03-01), Renth et al.
patent: 4801600 (1989-01-01), Wang et al.
patent: 4921869 (1990-05-01), Wang et al.
Gregory, W. A. et al., "Antibacterials, Synthesis and Structure-Activity Studies of 3-Aryl-2-oxooxazolidines. 1. The B Group, " J. Med. Chem. 32:1673-81 (1989).
Gregory, W. A. et al., "Antibacterials. Synthesis and Structure-Activity Studies of 3-Aryl-2-oxooxazolidines. 2. The A Group," J. Med. Chem. 33:2569-78 (1990).
Wang, C-L. J. et al., "Chiral Synthesis of DUP 721, a New Antibacterial Agent," Tetrahedron 45(5):1323-26 (1989).
Park, Chung-Ho et al., "Antibacterials. Synthesis and Structure-Activity Studies of 3-Aryl-2-oxooxazolindines. 4. Multiply-Substituted Aryl Derivatives," J. Med. Chem. 35:1156-65 (1992).
Barbachyn Michael R.
Brickner Steven J.
Gammill Ronald B.
Hutchinson Douglas K.
Patel Mahesh V.
Corneglio Donald L.
Gibson Sharon
Kilby Scalzo Catherine
The Upjohn Company
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