IP Library › Granted Patent US 9,511,042
Granted Patent B2
US 9,511,042 · App. 13/703,292 · Granted Dec 6, 2016

N-acyl amino acid derivatives for treating skin conditions such as cellulite

Inventors: Timothy J. Falla (Woodinville, WA); Lijuan Zhang (Kenmore, WA)
Assignee: HELIX BIOMEDIX INC.
A61K31/198A61K8/42A61K8/44A61K31/20A61K45/06A61Q19/06C07C237/12
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Quick Facts
Patent No.
US 9,511,042
App. No.
13/703,292
Granted
Dec 6, 2016
Kind
B2
Abstract

The invention relates to small molecules having biological and therapeutic activity. Particularly, the invention relates to small molecules having lipolytic and anti-adipogenic activity. Two examples of such molecules are 4-methyl-2-(octanoylamino) pentanoic acid and N-isopentyloctanamide. The invention further relates to methods of preventing or treating skin conditions such as cellulite using small molecules having lipolytic and anti-adipogenic activity.

Claims (26)

1. A method of stimulating lipolysis in one or more adipocytes of a mammal, said method comprising administering to the skin tissue of said mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound, or salt thereof, wherein the compound is:

2. The method of claim 1 , wherein said composition further comprises carnitine, resveratrol, isoproterenol, aminophylline, theophylline, or caffeine.

3. The method of claim 1 , wherein said composition is administered to skin tissue superficial to the subcutaneous layer.

4. The method of claim 1 , wherein said composition is directly injected into the subcutaneous layer of the skin tissue.

5. A method of stimulating lipolysis in one or more adipocytes of a mammal, said method comprising administering to the skin tissue of said mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound or pharmaceutically acceptable salts thereof, wherein the compound is of the formula:

R 1 —CO—NH—R 2 ; wherein

R 1 is a saturated or unsaturated aliphatic chain of 5 to 9 carbon atoms,

R 2 is an alkyl of 5 to 9 carbon atoms, and wherein the R 1 —C(O) portion of the formula is a fatty acyl group.

6. The method of claim 5 , wherein the fatty acyl group is an octanoyl group.

7. The method of claim , wherein the fatty acyl group is saturated.

8. The method of claim 5 , wherein said composition is in the form of an aerosol, emulsion, liquid, lotion, cream, paste, ointment, powder, or foam.

9. The method of claim 5 , wherein said composition further comprises carnitine, resveratrol, isoproterenol, aminophylline, theophylline, or caffeine.

10. The method of claim 5 , wherein said composition is administered to skin tissue superficial to the subcutaneous layer or directly injected into the subcutaneous layer.

11. A method of reducing adipogenesis in subcutaneous tissue of a mammal, said method comprising administering to the skin tissue of said mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound, or salt thereof, wherein the compound is:

12. The method of claim 11 , wherein said composition further comprises carnitine, resveratrol, isoproterenol, aminophylline, theophylline, or caffeine.

13. The method of claim 11 , wherein said composition is administered to skin tissue superficial to the subcutaneous layer.

14. The method of claim 11 , wherein said composition is directly injected into the subcutaneous layer of the skin tissue.

15. A method of reducing adipogenesis in subcutaneous tissue of a mammal, said method comprising administering to the skin tissue of said mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound or pharmaceutically acceptable salts thereof, wherein the compound is of the formula:

R 1 —CO—NH—R 2 ; wherein

R 1 is a saturated or unsaturated aliphatic chain of 5 to 9 carbon atoms,

R 2 is an alkyl of 5 to 9 carbon atoms, and wherein the R 1 —C(O) portion of the formula is a fatty acyl group.

16. The method of claim 15 , wherein the fatty acyl group is an octanoyl group.

17. The method of claim 15 , wherein the fatty acyl group is saturated.

18. The method of claim 15 , wherein said composition is in the form of an aerosol, emulsion, liquid, lotion, cream, paste, ointment, powder, or foam.

19. The method of claim 15 , wherein said composition further comprises carnitine, resveratrol, isoproterenol, aminophylline, theophylline, or caffeine.

20. The method of claim 15 , wherein said composition is administered to skin tissue superficial to the subcutaneous layer or directly injected into the subcutaneous layer.

Continuity (2)
Provisional Application 61361179 · Jul 2, 2010
Related Publication 20130096143A1 · Apr 18, 2013