IP Library Granted Patent US 9,695,137
Granted Patent B2
US 9,695,137 · App. 14/773,022 · Granted Jul 4, 2017

Analogs of peroxisome proliferator activated receptor (PPAR) agonists, and methods of using the same

Inventors: Bruce E. Heck (Toledo, OH); Dong Hyun Kim (Toledo, OH); Paul Erhardt (Toledo, OH); Brian Kress (Toledo, OH)
Assignee: The University of Toledo
C07D277/22A61K31/426A61K31/5575A61K45/06
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Quick Facts
Patent No.
US 9,695,137
App. No.
14/773,022
Granted
Jul 4, 2017
Kind
B2
Abstract

Analogs of PPAR5 and analogs of 20-OH-PGE2, which are PPAR5 agonists and 20-OH-PGE2 antagonists, respectively, and methods of using the same for inducing osteogenesis or chondrogenesis, are disclosed.

Claims (11)

1. A method of treating or ameliorating osteoarthritis, the method comprising administering an effective amount of a pharmaceutical composition to a patient in need thereof;

the pharmaceutical composition comprising a peroxisome proliferator activated receptor (PPAR) compound in an amount sufficient to allow stem cells in the patient to differentiate into an osteocyte cell of osteoblast lineage, or into a chondrocyte cell of chondroblast lineage; and a pharmaceutically acceptable carrier, excipient, diluent, or adjuvant;

wherein the PPAR compound has a structural formula of Formula I:

X is O;

R is CH═CHR 3 , and R 3 is carboxylic acid; and,

R 1 is para CF 3 and R 2 is meta H; or R 1 is meta CF 3 and R 2 is para H; and

salts, isomers, stereoisomers, enantiomers, racemates, solvates, hydrates, polymorphs, and prodrugs thereof.

2. The method of claim 1 , wherein the administration of the pharmaceutical composition is by surgical implantation into the patient.

3. The method of claim 1 , wherein the administration comprises treating isolated mammalian stem cells with an effective amount of the pharmaceutical composition, and administering the treated mammalian stem cells to the patient.

4. The method of claim 1 , wherein the administration comprises intravenous administration of the pharmaceutical compound to the patient.

5. The method of claim 1 , wherein the administration comprises subcutaneous administration of the pharmaceutical compound to the patient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2015
From: HECK, BRUCE E.; KIM, DONG HYUN; ERHARDT, PAUL; KRESS, BRIAN
To: THE UNIVERSITY OF TOLEDO
Reel/Frame 036783/0852 →
Continuity (2)
Provisional Application 61786030 · Mar 14, 2013
Related Publication 20160016920A1 · Jan 21, 2016