# US 11,897,852 B2 · Proxisome proliferator activated receptor (PPAR) compounds and methods of using the same

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- Number: US 11,897,852 B2
- Document ID: US11897852B2
- Status: Granted
- Kind: B2
- Application number: 17/172,543
- Filed: 2021-02-10
- Published: 2021-06-03
- Granted: 2024-02-13
- Earliest claimed: 2013-03-14
- Assignees: The University of Toledo
- Applicants: The University of Toledo
- Inventors: Bruce E. Heck; Dong Hyun Kim; Paul W. Erhardt; Brian Kress
- Web page: https://patentgrep.com/patent/US11897852B2

## CPC

- C07D 277/24: Radicals substituted by oxygen atoms
- A61K 31/426: 1,3-Thiazoles
- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07D 277/22: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 277/28: Radicals substituted by nitrogen atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

## Claims

### Claim 1

A method of treating osteoarthritis by inducing chondrogenesis in a subject having osteoarthritis, the method comprising:
administering an effective amount of a pharmaceutical composition to the subject in need thereof sufficient to induce chondrogenesis;
the pharmaceutical composition comprising a peroxisome proliferator activated receptor (PPAR) compound in an amount sufficient to prompt stem cells in the subject to contribute toward improving cartilage health, and a pharmaceutically acceptable carrier, excipient, diluent or adjuvant;
wherein the PPAR compound has a chemical structure of Formula (12d):
wherein:
X is S;
R1 is CF3;
R2 is F; and
R3 is H; and,
salts, isomers, solvates, hydrates, polymorphs and prodrugs thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the administration is by one or more of:
oral administration;
surgical implantation including allograft bone, bone substitutes or bone scaffold matrices;
and,
localized injection of liquid or gel formulations or delivery systems to or near bone and/or cartilage tissue; wherein the injection is one or more of: intravenous, intramuscular and subcutaneous.

### Claim 3 (depends on 1)

The method of claim 1, wherein the subject is a human.

### Claim 4

A method of treating a mammalian patient in need thereof, the method comprising:
administering induced stem cells to a mammalian patient in need thereof;
wherein the induced stem cells are derived from incubating stem cells with a pharmaceutical composition comprising a peroxisome proliferator activated receptor (PPAR) compound in an amount sufficient to prompt stem cells in the patient to contribute toward improving cartilage health and inducing chondrogenesis, and a pharmaceutically acceptable carrier, excipient, diluent or adjuvant;
wherein the PPAR compound has a chemical structure of Formula (12d):
wherein:
X is S;
R1 is CF3;
R2 is F; and
R3 is H; and,
salts, isomers, solvates, hydrates, polymorphs and prodrugs thereof.

### Claim 5 (depends on 4)

The method of claim 4, wherein the mammalian patient is a human, and the stem cells are either harvested from the same patient or supplied from another mammalian donor.

### Claim 6 (depends on 5)

The method of claim 5, wherein the administration is by one or more of:
surgical implantation including allograft bone, bone substitutes or bone scaffold matrices; and,
localized injection of liquid or gel formulations or delivery systems to or near bone and cartilage tissue; wherein the injection is one or more of: intravenous, intramuscular and subcutaneous.