Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-11-07
2000-07-18
Stockton, Laura L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514376, 546113, 548232, A61K 31422, A61K 31437, C07D48704
Patent
active
060908203
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The subject invention discloses new and useful oxazolidinones having a spirocyclic or bicyclic diazinyl or carbazinyl moiety. The compounds are useful antimicrobial agents effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species.
The present compounds are related by their phenyloxazolidinone ring structure to those disclosed in the publications below except that the subject compounds have a spirocyclic or bicyclic diazinyl or carbazinyl moiety. The instant compounds have useful antibacterial activity.
PCT/US94/08904 application discloses oxazolidinone antibacterial compounds having either a morpholine or thiomorpholine substituent.
PCT/US93/03570 application discloses oxazolidinones containing a substituted diazine moiety and their uses as antimicrobials.
PCT/US92/08267 application discloses substituted aryl and heteroaryl-phenyl-oxazolidinones useful as antibacterial agents.
PCT/US89/03548 application discloses 5'indolinyl-5.beta.-amidomethyloxazolidin-ones, 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, 4,921,869, Gregory W. A., et al., J. Med. Chem., 32, 1673-81 (1989); Gregory W. A., et al., J. Med. Chem., 33, 2569-78 (1990); Wang C., et al., Tetrahedron, 45, 1323-26 (1989); and Brittelli, et al., 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 pyridinylmethyl substituted phenyl oxazolidinones.
SUMMARY OF THE INVENTION
In one aspect the subject invention is a compound of structural Formula I: ##STR2##
In another aspect the subject invention is composed of structural Formula II: ##STR3## or pharmaceutically acceptable salts thereof wherein: R.sup.1 is (a) NR.sup.5, following: F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy), following: Cl, F, CN, OH, C.sub.1-4 alkoxy, amino, hydroxylamino, alkoxylamino, C.sub.1-4 acyloxy, C.sub.1-4 alkylsulfenyl, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, aminosulfonyl, C.sub.1-4 alkylaminosulfonyl, C.sub.1-4 dialkylaminosulfonyl, 4-morpholinylsulfonyl, phenyl (optionally substituted with one or more of F, Cl, CN, OH, C.sub.1 -C.sub.4 alkoxy), 5-isoxazolyl, ethenyloxy, ethynyl), following: Cl, F, OH, SH, C.sub.1-4 alkoxy, naphthalenoxy and phenoxy (optionally substituted with one or more of the following: Cl, F, OH, C.sub.1 -C.sub.4 alkoxy, amino, C.sub.1 -C.sub.4 acylamino, C.sub.1 -C.sub.4 alkyl), amino, C.sub.1 -C.sub.4 acylamino, hydroxylamino, alkoxylamino, C.sub.1-4 acyloxy, phenyl, C.sub.1 -C.sub.4 alkylcarbonyl, C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 dialkylamino, C.sub.1 -C.sub.4 hydroxyacyloxy, C.sub.1 -C.sub.4 alkylsulfenyl, phthalimido, maleimido, succinimido), following: Cl, F, OH, C.sub.1-4 alkoxy, amino, hydroxylamino, alkoxylamino, C.sub.1-4 acyloxy, phenyl), F, Cl, OCH.sub.3, OH or C.sub.1-4 alkyl), the following: Cl, F, OH, C.sub.1-4 alkoxy, C.sub.1-4 acyloxy, phenyi), dialkylaminocarbonyl (where the alkyl groups are optionally substituted with one or more of the following: Cl, F, OH, C.sub.1-4 alkoxy, phenyl), 2-thiazolyl, 3-isoxazolyl, 3-isothiazolyl and dihydro derivatives of these ring systems (all optionally substituted with one or more of the following: Cl, F, OH, amino, C.sub.1-4 acylamino, C.sub.1-4 alkylsulfonylamino, C.sub.1-4 alkoxycarbonylamino, C.sub.1-4 alkoxy, C.sub.1-4 acyloxy, C.sub.1-4 alkyl which can be substituted with F, OH or C.sub.1-4 alkoxy,
REFERENCES:
patent: 4801600 (1989-01-01), Wang et al.
patent: 4921869 (1990-05-01), Wang et al.
Gregory W. A., et al., J. Med. Chem., 32, 1673-81 (1989).
Gregory W. A., et al., J. Med. Chem., 33, 2569-78 (1990).
Wang C., et al., Tetrahedron, 45, 1323-26 (1989).
Brittelli, et al., J. Med. Chem., 35, 1156-1165 (1992).
Barbachyn Michael Robert
Brickner Steven Joseph
Hutchinson Douglas K.
Pharmacia & Upjohn Company
Solomon Andrew M.
Stockton Laura L.
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