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US 6,297,242 B1Granted
N-substituted amidine and guanidine oxazolidinone antibacterials and methods of use thereof
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorDennis Hlasta
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Abstract
N-substituted amidine and guanidine oxazolidinone compounds of the formula: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
Claims15
A compound of Formula I:
- wherein
- R is H, alkyl, cycloalkyl, OR1, SR1, amino, NHR1, NR1R2, C1-C8 alkylaryl, or mono-, di-, tri- or per-halo-C1-C8 alkyl;
- W is H, CN, COR1, COOR1, CONHR1, CO—NR1R2, SO2R2, SO2NHR1, SO2—NR1R2, or NO2;
- R1 and R2 are independently H, alkyl, or mono-, di-, tri- or per-halo-C1-C8 alkyl, or, in the case of —NR1R2, R1 and R2 taken together with the nitrogen may be a cyclic amino derivative;
- X is H, CN, COR1, COOR1, CONHR1, CO—NR1R2, SOR1, SO2R1, SO2NHR1, SO2—NR1R2, NO2, C1-C8 alkyl, OR1, SR1, amino, NHR1, NR1R2, C1-C8 alkylaryl, halogen, halo-alkyl, alkoxy, heteroaryl, or aryl;
- and
- Y is 0 to 4 members independently selected from the group consisting of H, halogen, OH, mercapto, nitro, halo-C1-8-alkyl, C1-8 alkoxyl, thio-C1-8-alkyl, C1-8 alkyl-amino, di(C1-8-alkyl-)amino, formyl, carboxy, alkoxycarbonyl, C1-8 alkyl-CO—O—, C1-8 alkyl-CO—NH—, carboxamide, aryl, substituted-aryl, heteroaryl, substituted-heteroaryl, CN, amine, alkoxy, NHCO—(C1-8 alkyl), C3-6 cycloalkyl, C1-8 alkyl optionally substituted with one or more members selected from the group consisting of F, Cl, OH, C1-8 alkoxyl and C1-8 acyloxy;
- and optical isomers, enantiomers, diastereomers, racemates and racemic mixtures thereof, or pharmaceutically acceptable salts thereof.
5 more elements
A method of treating a subject having a condition caused by or contributed to by bacterial infection, which comprises administering to said subject a therapeutically effective amount of the compound of Formula I.
Dependencies are inferred from the claim text.