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US 6,472,406 B1Granted
Sulfonamidomethyl phosphonate inhibitors of beta-lactamase
AssigneeMethylGene Inc.
InventorsJeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Abstract
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic β-lactamase inhibitors presently available, and which do not require a β-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
Claims1
A compound of Formula (I):
- or a pro-drug or pharmaceutically acceptable salt thereof, wherein
- R1 is aryl or heteroaryl, wherein the aryl or heteroaryl group may be optionally substituted;
- n is 0, 1, or 2;
- R2 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aralkyl, and aryl, wherein the aryl portion of any such group may be optionally substituted;
- R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aralkyl, aryl, heteroaryl, and (heteroaryl) alkyl, any of which groups may be optionally substituted;
- R4 is OH;
- R5 is OR6;
- R6 is selected from the group consisting of aryl, pyridyl, quinolyl, or isoquinolyl, any of which may be optionally substituted;
- provided that R6 is not unsubstituted phenyl;
- and further provided that R1 is not 5-dimethylamino-1-naphthyl when R2 and R3 are both H, and R5 is 4-nitrophenoxy.
7 more elements
Dependencies are inferred from the claim text.