Inhibitors of human 12-lipoxygenase
AssigneesThe United States of America, as represented the Secretary Department of Health & Human Service, Thomas Jefferson University, Eastern Virginia Medical School, The Regents of the University of California
InventorsDavid J. Maloney, Theodore Holman, Ajit Jadhav, Anton Simeonov, Ganesha Rai Bantukallu, Jerry L. Nadler, Michael Holinstat
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Abstract
Disclosed are inhibitors of human 12-lipoxygenase of Formula (I) or (II), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating or preventing a 12-lipoxygenase mediated disease or disorder, e.g., diabetes. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.
Claims30
A compound of Formula (I) or Formula (II):
- wherein R1 and R2 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, nitro, fluoro, bromo, chloro, and iodo,
- R3 is selected from isoalkyl, cycloalkyl, aryl, heterocyclyl, and heteroaryl, each optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C3-C8 cycloalkenyl, C6-C10 aryl, heteroaryl, —NO2, —OH, —OR5, —SH, —SR5, —SOR5, —SO2R5, —COR5, —COOH, —COOR5, —CONHR5, and —CONR5R6,
- R4 is selected from hydrogen and alkyl, wherein alkyl is optionally substituted with halo, —NO2, —OH, —OR5, —SH, —SR5, —SOR5, —SO2R5, —COR5, —COOH, —COOR5, —CONHR5, and —CONR5R6,
- and
- R5 and R6 are independently selected from C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, and C3-C8 cycloalkenyl,
- or a pharmaceutically acceptable salt thereof, enantiomers thereof, a mixture of enantiomers thereof, or diastereomers thereof.
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Dependencies are inferred from the claim text.