Use of a PPAR-δ agonist for reducing loss of muscle strength, muscle mass, or type I muscle fibers in an immobilized limb

Patent metadata

Field	Value
Publication number	US-11096946-B2
Application number	US-201916660090-A
Country	US
Kind code	B2
Filing date	Oct 22, 2019
Priority date	Sep 9, 2013
Publication date	Aug 24, 2021
Grant date	Aug 24, 2021

Abstract

The present invention provides methods for reducing loss of muscle strength, muscle mass, or Type I muscle fibers in an immobilized limb by administering (E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.

First claim

We claim:

1. A method of treating disease-associated muscle atrophy in a human comprising administering to the human in need thereof (E)-[4-[3-(4-fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the disease-associated muscle atrophy results from a muscle disease.

3. The method of claim 2 , wherein the muscle disease is muscular dystrophy, polymyositis, or myotonia.

4. The method of claim 2 , wherein the muscle disease occurs as a response to systemic illness.

5. The method of claim 4 , wherein the systemic illness is hypothyroidism, hyperthyroidism, adrenal gland depletion, diabetes mellitus, or an autoimmune disease.

6. The method of claim 4 , wherein the systemic illness is cancer, Acquired Immune Deficiency Syndrome (AIDS), chronic obstructive lung disease, congestive heart failure, cardiomyopathy, chronic liver disease, renal disease, emphysema, tuberculosis, osteomalacia, hormonal deficiency, anorexia nervosa, or generalized malnutrition.

7. The method of claim 1 , wherein treating comprises muscle modulation in the human.

8. The method of claim 7 , wherein muscle modulation is selected from: increasing muscle mass in the human; modulating muscle growth, enhancing muscle formation, increasing muscle strength, maintaining muscle strength or reducing loss of muscle strength in the human; reducing the rate of decrease in mitochondrial biogenesis in a muscle tissue; and combinations thereof.

9. The method of claim 1 , wherein treating comprises activating PPARδ in muscle in the human.

10. The method of claim 1 , wherein (E)-[4-[3-(4-fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof is administered at a dose of 50-200 mg per day.

Assignees

• Vtv Therapeutics Llc

Inventors

• Valcarce Lopez Maria Carmen
• Ohlstein Eliot

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61K31/5375 Primary

  1,4-Oxazines, e.g. morpholine · CPC title

• A61P21/00

  Drugs for disorders of the muscular or neuromuscular system · CPC title

• A61K9/0053

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

• C07D295/096

  with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings · CPC title