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US 2011/0224186 A1Published application
Carbacephem beta-lactam antibiotics
AssigneeAchaogen, Inc.
InventorsAllan Scott Wagman, Heinz Ernst Moser
Life of this patent
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Abstract
Carbacephem β-lactam antibiotics having the following chemical structure (I) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, X, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
Claims29
A compound having the following structure (I):
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein:
- R1 is selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxyalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl and —C(═O)R1a,
- wherein:
- R1a is selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxyalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl and optionally substituted heteroarylalkyl;
- R2 is selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl and optionally substituted heteroarylalkyl;
- X is selected from —O—, —C(═O)—, —SCH2—, —CH2S—, —SCH═CH—, —CH═CHS—, —SCH2S—, —OCH2—, —CH2O—, optionally substituted alkylene, optionally substituted alkenylene and optionally substituted cycloalkyl;
- and
- Ar2 is optionally substituted aryl or optionally substituted heteroaryl.
6 more elements
5-8. (canceled)
10-11. (canceled)
15-16. (canceled)
18-21. (canceled)
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26-33. (canceled)
35-43. (canceled)
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A compound having the following structure:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof.
(canceled)
Dependencies are inferred from the claim text.