Agonists of peroxisome proliferator-activated receptor alpha (PPAR+60 ) and methods of use
AssigneeThe Board of Regents of the University of Oklahoma
InventorsAdam Duerfeldt, Xiaozheng Dou, Ziwei Hu
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Abstract
Benzyl derivative compounds having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, kits and compositions containing such compounds, and methods of their use in enhancing PPARα activity for treating diseases and/or conditions involving inflammation and/or angiogenesis, particularly ocular diseases and/or conditions such as but not limited to retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema.
Claims17
A compound, comprising the chemical structure:
- wherein:
- X=COOH,
- R1=4-F, 2,4-diF, 3,4-diF, 3,5-diF, or 4-OCH3,
- R2=H, 3-F, 3-Cl, 2-CH3 or 3-CH3,
- R3=H or F, and
- R4=H or CH3.
A compound, comprising the chemical structure:
- and salts and isomers thereof, the compound selected from the group consisting of (a)-(i),
- wherein:
- in (a) X=COOH, R1=4-F, R2=3-CH3, R3=H, and R4=H;
- in (b) X=COOH, R1=4-F, R2=3-CH3, R3=H, and R4=CH3;
- in (c) X=COOH, R1=4-F, R2=3-CH3, R3=F, and R4=H;
- in (d) X=COOH, R1=4-F, R2=3-Cl, R3=F, and R4=H;
- in (e) X=COOH, R1=2,4-diF, R2=3-CH3, R3=H, and R4=H;
- in (f) X=COOH, R1=3,4-diF, R2=3-CH3, R3=H, and R4=H;
- in (g) X=COOH, R1=3,5-diF, R2=3-CH3, R3=H, and R4=H;
- in (h) X=COOH, R1=4-F, R2=3-F, R3=H, and R4=H;
- and
- in (i) X=COOH, R1=4-OCH3, R2=H, R3=H, and R4=H.
A method of treating a disorder or condition in a subject by causing an increase in peroxisome proliferator-activated receptor α (PPARα) activity, comprising:
- administering to a subject in need of such therapy a compound comprising the chemical structure:
- and salts and isomers thereof, wherein:
- X=COOH,
- R1=4-F, 2,4-diF, 3,4-diF, 3,5-diF, or 4-OCH3,
- R2=H, 3-F, 3-Cl, 2-CH3, or 3-CH3,
- R3=H or F, and
- R4=H or CH3;
- and
- wherein the compound is optionally provided in a composition formulated to provide a delayed release, controlled release, extended release, and/or sustained release of the compound.
Dependencies are inferred from the claim text.