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US 2025/0032453 A1Published application
20-hete receptor (gpr75) antagonists and methods of use
AssigneesBoard of Regents, The University of Texas System, New York Medical College
InventorsJohn R. Falck, Michal L. Schwartzman, Victor Garcia
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Abstract
The present invention concerns compounds and their use to treat cardiovascular disease, renal disease, thrombic disease, stroke, metabolic syndrome, cell proliferation, and ischemic cardiovascular disorders. Compounds of the present invention display significant potency as antagonists of 20-hydroxyeicosatetraenoic acid (20-HETE), and function as anti-hypertensive, anti-inflammatory, or anti-growth agents.
Claims18
A compound of the formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R2 and R3 are each, independently, OH, C1-C3, F, or H, provided that at least one of R2 and R3 is OH;
- R4 is C1-C3, H, F, or —CH2N3 (azide);
- X is C;
- m is 1;
- n is 2;
- p is 1;
- q is 1;
- and
- R1 is NR8R9 or C(O)R6, wherein:
- R6 is OR7, NR8R9, a D-/L-/D,L-α-amino acid (MW<250) other than glycine, —NHS(O)2R10, glycerol, glyceride mono- or diester (MW<800), or a carboxylate isostere or mimetic selected from the group consisting of:
- —P(O)(OH)2, —S(O)2OH,
- wherein ii) lower alkyl is a C1-C6 alkyl or cycloalkyl;
- R7 is C1-C6 alkyl or cycloalkyl, or benzyl;
- R8 and R9 are each, independently, H, C1-C6 alkyl or cycloalkyl, or benzyl, or R8 and R9 together constitute a 3-7 membered ring with the nitrogen;
- and
- R10 is phenyl, C1-C5 alkyl or cycloalkyl, or CF3.
14 more elements
Dependencies are inferred from the claim text.