Fluoro-pyridinone derivatives useful as antibacterial agents
AssigneePfizer Inc.
InventorsUsa REILLY, Michael MELNICK, Matthew F. BROWN, Mark S. PLUMMER, Justin MONTGOMERY, Ye CHE, Loren PRICE
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Abstract
The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
Claims14
A compound of the formula:
- or a pharmaceutically acceptable salt thereof,
- in which:
- R1 is represented by C1-C3 alkyl;
- R2 is represented by hydrogen or C1-C3 alkyl;
- R3 is represented by hydrogen, halogen, hydroxy, cyano, C1-C3alkyl, C1-C3alkoxy, trifluoromethyl or trifluoromethoxy;
- T is represented by ethynyl, optionally substituted (C6-C10)aryl or optionally substituted heteroaryl;
- D is absent, or is represented by —(CH2)r—, —(CH2)n—O—(CH2)p—, or a bond;
- r is represented by the integer 1, 2, or 3;
- n and p are each independently represented by the integer 0, 1, or 2;
- E is absent, or is represented by a substituent selected from the group consisting of:
- i) (C3-C10)cycloalkyl, optionally substituted;
- ii) (C6-C10)aryl optionally substituted;
- iii) heteroaryl, optionally substituted;
- and
- iv) heterocyclic, optionally substituted;
- with the proviso that:
- 1) if E is absent, then D is also absent;
- 2) T is not represented by unsubstituted phenyl;
- when E and D both are absent, R3 is hydrogen and R1 and R2 are each methyl.
A compound of the formula
- or a pharmaceutically acceptable salt thereof,
- in which;
- R3 is represented by hydrogen, halogen, hydroxy, cyano, C1-C3alkyl, C1-C3alkoxy, trifluoromethyl or trifluoromethoxy;
- Ra is represented by one or more substituents selected from the group consisting of C1-C3alkyl, C1-C3 alkoxy, fluorine, chlorine, hydroxy, trifluoromethyl and trifluoromethoxy.
(2R)-4-{5-Fluoro-2-oxo-4-[4-(2H-1,2,3-triazol-2-yl)phenyl]pyridin-1(2H)-yl}-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide, or a pharmaceutically acceptable salt thereof.
(2R)-4-[5-Fluoro-4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.