Compositions and methods for inhibition of phospholipase A2 mediated inflammation
AssigneeThe Regents of the University of California
InventorsEdward Dennis, Tony Yaksh, Karin Killermann Lucas, Camilla Svensson, David A. Six, George Kokotos, Violetta Constantinou-Kokotou
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Abstract
Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a method for treating hyperalgesia and other inflammatory conditions associated with PLA2 activity is provided.
Claims12
A compound of the formula (I):
- wherein:
- R1 is an acidic moiety, selected from the group consisting of carboxyl, phosphate, phosphinate, sulfate, and sulfonate;
- each of R2 and R3 is a moiety independently selected from the group consisting of phenyl, benzyl, and a carbyl having between 1 and 13 carbons, the carbyl being selected from the group consisting of a linear or branched, saturated or unsaturated alkyl, alkenyl, and alkynyl;
- n is an integer having a value of 3, m is an integer having a value of 0 to 3, and k is an integer having a value of 0 to 22;
- and isomers, enantiomers, and pharmacologically or immunologically acceptable salts thereof.
A pharmaceutical composition, comprising (4S)-4-[(2-oxododecanoyl)amino]octanoic acid, and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising 4-[(2-oxohexadecanoyl)amino]butanoic acid, and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising 4-[(2-oxooctanoyl)amino]butanoic acid, and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising (4R)-4-[(2-oxododecanoyl)amino]octanoic acid, and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (II),
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (III),
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (IV),
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (V),
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (VI),
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (VII),
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition, comprising the compound of formula (VIII),
- and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.