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US 6,320,051 B1Granted
Quinolones used as MRS inhibitors and bactericides
AssigneeSmithKline Beecham Corporation
InventorsJohn Michael Berge, Pamela Brown, John Stephen Elder, Andrew Keith Forrest, Dieter Wolfgang Hamprecht, Richard Lewis Jarvest, David Jonathan McNair, Robert John Sheppard
Life of this patent
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Abstract
Compounds of formula (I) are inhibitors of the bacterial enzyme S aureus methionyl tRNA synthetase and are of use in treating bacterial infections.
Claims16
A compound of formula (I):
- in which:
- R1 is optionally substituted aryl or optionally substituted heteroaryl;
- R2 is hydrogen, C(1-6)alkyl, arylC(1-4)alkyl, arylC(2-4)alkenyl or C(1-6)alkylcarbonyl;
- R3 is selected from halo, cyano, hydroxy, (C1-6)alkyl (optionally substituted by halo, hydroxy, amino, mono to perfluoro(C1-3)alkyl, carboxy or (C1-6)alkoxycarbonyl), (C3-7)cycloalkyl, C(1-6)alkoxy, amino, mono- or di-(C1-6)alkylamino, acylamino, carboxy, (C1-6)alkoxycarbonyl, carboxy(C1-6)alkyloxy, (C1-6)alkylthio, (C1-6)alkylsulphinyl, (C1-6)alkylsulphonyl, sulphamoyl, mono- and di-(C1-6)alkylsulphamoyl, carbamoyl, mono- and di-(C1-6)alkylcarbamoyl, and heterocyclyl;
- m is 0 or an integer from 1 to 3;
- X is CHR4 (wherein R4 is hydrogen, C(1-6)alkyl or aryl), C(2-4)alkylene, C(3-4)alkenylene or CO;
- Y is a linker group having from 2 to 6 methylene groups in a straight chain and in which one or more methylene groups may have one or more C(1-6) alkyl, C(1-6)alkoxy or C(1-6)alkylidenyl substituents and in which chain 1,2- or 1,3-carbon atoms may be linked by a C(2-3) alkylene or a C3 alkenylene bridge;
- R1 and X or R1 and R2 may be linked by a polymethylene chain to form a 5 to 7 membered ring, optionally substituted by C(1-6) alkyl;
- X and R2, X and Y or Y and R2 may be linked by a polymethylene chain to form a 4 to 7 membered ring, optionally substituted by C(1-6) alkyl;
- Z is NH or O;
- and
- salts thereof, preferably pharmaceutically acceptable salts thereof.
9 more elements
Dependencies are inferred from the claim text.