IP Library Granted Patent US 6,852,882
Granted Patent B2
US 6,852,882 · App. 10/478,620 · Granted Feb 8, 2005

Peptide deformylase inhibitors

Assignee: SmithKline Beecham Corporation
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Quick Facts
Patent No.
US 6,852,882
App. No.
10/478,620
Granted
Feb 8, 2005
Kind
B2
Abstract

Novel PDF inhibitors and novel methods for their use are provided.

Claims (32)

1. A compound according to formula (I):

wherein:

Ar is an aryl group selected from the group consisting of phenyl, azaindolyl, pyridyl, indolyl, quinolinyl, pyrazinyl, benzenethiophenyl, isoxazolyl, isoquinolinyl, napthyl, oxazolyl, isothiazolyl, benzothiaphenyl, furyl, pyridazinyl, thienyl, benzofuryl, triazolyl, imidazolyl, and thiazolyl; such that Ar may be optionally substituted with one, two, or three substituents selected from the group consisting of optionally substituted alkyl or cycloalkyl of one to nine carbons, halo, alkoxy of one to nine carbons, hydroxy, amino, hydroxyalkyl of one to nine carbons, alkoxyalkyl, wherein the alkyl and alkylene groups are independently of one to nine carbons, optionally substituted aryl or optionally substituted heteroaryl, carboxy, and alkoxycarbonyl.

2. A compound according to claim 1 selected from the group consisting of:

3,4-Dichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

3-Trifluoromethyl-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2-Methoxy-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

N-[2-(N-Formyl-N-hydroxy-amino)-ethyl]-thiophen-2-yl-carboxamide;

N-[2-(N-Formyl-N-hydroxy-amino)-ethyl]-thiophen-3-yl-carboxamide;

N-[2-(N-Formyl-N-hydroxy-amino)-ethyl]-benzamide;

3-Chloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-thiophen-2-yl-carboxamide;

5-Chloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-thiophen-2-yl-carboxamide;

3,5-Dichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

3-Chloro-2-fluoro-5-trifluoromethyl-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2-Chloro-5-trifluoromethyl-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

3-Phenoxy-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2,6-Dichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

6-Methoxy-2,3,5-trichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

5-Phenoxy-2-chloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2-Chloro-5-phenoxybenzoic acid;

2-Chloro-5-benzyloxy-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2-Chloro-5-methoxy-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2-Chloro-5-hydroxy-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

6-Hydroxy-2,3,5-trichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide; and

5-Chloro-4-[2-(N-formyl-N-hydroxy-amino)-ethyl]amido-benzimidazole.

3. A compound according to claim 2 selected from the group consisting of:

2,3-Dichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2,3,5-Trichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide;

2,5-Dichloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide; and

5-Bromo-2-chloro-N-[2-(N-formyl-N-hydroxy-amino)-ethyl]-benzamide.

4. A method of treating a bacterial infection by administering to a subject a compound according to claim 1 .

5. A method according to claim 4 wherein the bacterial infection is a respiratory tract infection or the Gram+ TPP.

Assignments (1)
CHANGE OF NAME Recorded Jan 8, 2010
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 023750/0387 →
Continuity (2)
Provisional Application 6029596300 · Jun 5, 2001
Related Publication 20040157916A1 · Aug 12, 2004