Compositions and methods for regulating glucose homeostasis and insulin action

Patent metadata

Field	Value
Publication number	US-11945825-B2
Application number	US-202117365528-A
Country	US
Kind code	B2
Filing date	Jul 1, 2021
Priority date	Jun 20, 2012
Publication date	Apr 2, 2024
Grant date	Apr 2, 2024

Abstract

The present invention encompasses the use of compounds for a novel approach to treat and prevent diseases, conditions, and disorders such as diabetes and ischemic reperfusion injury. Compounds of the invention, including but not limited to BAM15 ((2-fluorophenyl){6-[(2-fluorophenyl)amino](1,2,5-oxadiazolo[3,4-e]pyrazin-5-yl)}amine), a mitochondrial uncoupler, can improve glucose tolerance, increases cellular oxygen consumption, treat or prevent kidney ischemia reperfusion injury reverse insulin resistance, reverse or treat hyperinsulinemia, and reverse or treat hyperlipidemia. The present invention further provides novel compounds as well as methods for identifying compounds with the same or similar properties as BAM15.

First claim

What is claimed is:

1. A method for treating obesity, improving glycemia, improving insulin sensitivity, improving glucose tolerance, or treating ischemic reperfusion injury in a subject, said method comprising administering to a subject in need thereof an effective amount of a compound or pharmaceutically acceptable thereof, wherein the compound is a compound of the formula:

2. The method of claim 1 , wherein said compound is administered at a dosage ranging from about 0.1 mg/kg to about 50 mg/kg body weight.

3. The method of claim 2 , wherein said compound is administered at a dosage ranging from about 0.5 mg/kg to about 25 mg/kg body weight.

4. The method of claim 3 , wherein said compound is administered at a dosage ranging from about 1.0 mg/kg to about 5.0 mg/kg body weight.

5. The method of claim 2 , wherein said compound is administered as a unit dose ranging from about 10 mg to about 500 mg.

6. The method of claim 1 , wherein said compound is administered more than once.

7. The method of claim 1 , wherein said compound increases oxygen consumption.

8. The method of claim 1 , wherein the method is a method for treating obesity.

9. The method of claim 1 , wherein the method is a method for improving glucose tolerance.

10. The method of claim 1 , wherein the method is a method for treating ischemic reperfusion injury.

11. A method for improving glucose tolerance in a subject, said method comprising administering to a subject in need thereof an effective amount of a compound of the formula:

Assignees

• Univ Virginia Patent Foundation

Inventors

• Hoehn Kyle
• Kenwood Brandon

Classifications

• C07D498/04 Primary

  Ortho-condensed systems · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K31/4985

  Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems · CPC title

• G01N33/5014

  for testing toxicity · CPC title

• G01N33/5079

  Mitochondria · CPC title