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US 6,184,363 B2Granted
Inhibitors of β-lactamases and uses therefor
AssigneeNorthwestern University
InventorsBrian K. Shoichet, Grady Scott Weston
Life of this patent
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Abstract
The invention provides novel non-β-lactam inhibitors of β-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with β-lactam antibiotics to treat β-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.
Claims3
A compound having the formula:
- (OH)2—B—R (1)
- wherein R has the following formula:
- wherein:
- the atom center * is (R) or (S) in the case of chiral compounds;
- X is O, NH, NCH3 or
- Y is OH, NH2, NCH3, N(CH3)2, NHCOCH3 or NHCOCH2COOH;
- and
- R9 is H, a halogen atom, CF3, CCl3, CBr3, CH2CF3, CH2CCl3, CH2CBr3, NO2, CO2H, CHCHCOOH, CH2CH2CH2COOH, SO3H, PO3H, OSO3H, OPO3H, OH, NH2, CONH2, COCH3, OCH3, phenyl boronic acid, lower alkyl, or a side chain of a standard amino acid.
5 more elements
Dependencies are inferred from the claim text.