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US 8,283,339 B2Granted
Vinyl phosphonate lysophosphatidic acid receptor antagonists
AssigneeUniversity of Virginia Patent Foundation
InventorsKaren M. Carter, Kevin R. Lynch, Timothy L. Macdonald
Life of this patent
Estimating the term…
Abstract
The present invention provides LPA analogs that are antagonists at the LPA receptors.
Claims17
A compound having the formula
- wherein Z is —CY═CH— in the trans (e) configuration;
- Y is hydrogen or halogen,
- each R1 is independently halo, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, —NH2, —NH(C1-C6)alkyl, —N((C1-C6)alkyl)2, or cyano;
- and
- R2 is hydrogen, halo, (C1-C12)alkyl, halo(C1-C12)alkyl, halo(C1-C12)alkoxyl, (C3-C10)cycloalkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —NH2, —NH(C1-C12)alkyl, —N((C1-C12)alkyl)2, aryl, (C1-C12)alkaryl, aryl(C1-C12)alkyl, or aryl-substituted aryl(C1-C12)alkyl;
- each R3 is independently halo, (C1-C12)alkyl, halo(C1-C12)alkyl, halo(C1-C12)alkoxyl, (C3-C10)cycloalkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —NH2, —NH(C1-C12) alkyl, —N((C1-C12)alkyl)2, aryl, (C1-C12)alkaryl, aryl(C1-C12)alkyl, or aryl-substituted aryl(C1-C12)alkyl;
- R4 is (C6-C24)alkyl, halo(C6-C24)alkyl, (C6-C24)alkoxy, —NH2, —NH(C1-C24)alkyl, —N((C1-C24)alkyl)2, cyano, (C3-C10)cycloalkyl, (C4-C15)bicycloalkyl, (C6-C24)alkenyl, (C6-C24)alkenyl, (C6-C24)-alkynyl, aryl, (C6-C24)alkaryl, aryl(C6-C24)alkyl, or aryl-substituted aryl(C6-C24)alkyl;
- wherein the alkyl, alkenyl aryl groups of R4 can be optionally substituted with halo, alkoxy or cyano;
- or
- R5 and R6 are independently hydroxy, (C1-C12)alkyl-O—, (C2-C12)alkenyl-O—, (C2-C12)alkynyl-O—, (C6-C10)aryl-O—,
- m is 0, 1, 2, 3, or 4;
- n is 0, 1, 2, or 3;
- or a pharmaceutically acceptable salt or ester thereof.
10 more elements
Dependencies are inferred from the claim text.