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US 5,182,403 AGranted
Substituted 3(5'indazolyl) oxazolidin-2-ones
AssigneeThe Upjohn Company
InventorSteven J. Brickner
Life of this patent
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Abstract
The present invention relates to 3 indazol substituted 5 Beta amidomethyloxazolidin-2ones, useful as antibacterial agents and to intermediates for their production.
Claims5
A 3-(nitrogen substituted)phenyl-5.beta.-amidomethyl)oxazolidin-2-ones of formula (LV)
- where
- (I) R.sub.1 is --H, C.sub.1 -C.sub.4 alkyl, cyclopropyl, --CHCl.sub.2, --CCl.sub.3, --O--R.sub.1-3 where R.sub.1-3 is C.sub.1 -C.sub.4 alkyl, --CH.sub.2 OH, --CH.sub.2 OR.sub.1-5 where R.sub.1-5 is C.sub.1 -C.sub.4 alkyl or --CO--R.sub.1-6 where R.sub.1-6 is C.sub.1 -C.sub.4 alkyl or --.phi.;
- (II) two of R.sub.2, R.sub.3 and R.sub.4 are --H and the other of R.sub.2, R.sub.3 and R.sub.4 is --H, --F, --Cl, C.sub.1 -C.sub.6 alkyl, --C.tbd.N,
- (IIIA) where W.sub.1 and W.sub.2 taken together are
- --NR.sub.5 --N.dbd.CR.sub.6 -- (XXXII)
- where R.sub.5 is --H, C.sub.1 -C.sub.12 alkyl, --CH.sub.2 .phi., --CH.sub.2 CH.sub.2 --.phi., C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.12 alkynyl containing 1 triple bond, --CHO, --CO--R.sub.5-1 where R.sub.5-1 is
- (A) C.sub.1 -C.sub.6 alkyl optionally substituted with 1 13 O--CH.sub.3, --COOH, or 1-3 --Cl,
- (B) C.sub.3 -C.sub.7 cycloalkyl,
- (D) --.phi.optionally substituted with 1-3 --F, --Cl, C.sub.1 -C.sub.6 alkyl, --C.tbd.N,
- --CO--O--R.sub.5-8 where R.sub.5-8 is C.sub.1 -C.sub.4 alkyl or --.phi. optionally substituted with 1 or 2 --F, --Cl, C.sub.1 -C.sub.6 alkyl, --O--CH.sub.3, --C.tbd.N,
- --CO--N(R.sub.5-9).sub.2 where R.sub.5-9 is --H or R.sub.5-8 as defined above --CO--CH.sub.2 CN, --CO--CH.sub.2 --OH, --CO--CH.sub.2 O--.phi. where --.phi. is optionally substituted with 1-3 --O--CH.sub.3,
- --CO--CH.sub.2 --O--R.sub.5-10 where R.sub.5-10 is C.sub.1 -C.sub.6 alkyl, --.phi. optionally substituted with 1-3 --O--CH.sub.3, --CO--R.sub.5-11 where R.sub.5-11 is C.sub.1 -C.sub.6 alkyl, --.phi. optionally substituted with 1-4--F, 1-3 --Cl, 1 --OCH.sub.3, --SO.sub.2 CH.sub.3, --SO.sub.2 --.phi.,
- and R.sub.6 is --H and C.sub.1 -C.sub.3 alkyl;
- and pharmaceutically acceptable salts thereof.
11 more elements
Dependencies are inferred from the claim text.