Combination of a MC1R receptor agonist and UVB for the treatment and/or prevention of pigmentation disorders

Patent metadata

Field	Value
Publication number	US-9610461-B2
Application number	US-201314385416-A
Country	US
Kind code	B2
Filing date	Mar 15, 2013
Priority date	Mar 15, 2012
Publication date	Apr 4, 2017
Grant date	Apr 4, 2017

Abstract

A system comprising a combination of at least one MCI R receptor agonist and a source of NB-UVB, wherein said system is adapted for simultaneous or sequential use of said MC1R receptor agonist and said NB-UVB in amounts effective for the treatment and/or prevention of dermatological conditions linked to a hypopigmentation.

First claim

The invention claimed is:

1. A system comprising a combination of at least one MC1R receptor agonist and a source of NB-UVB, wherein said system is adapted for simultaneous or sequential use of said MC1R receptor agonist and said NB-UVB in amounts effective for the treatment of dermatological conditions linked to a hypopigmentation,
wherein said MC1R agonist is N-[((R)-2-[3-(4-hydroxybutoxy)-3-o-tolyl-azetidin-1-yl]-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(1H-imidazol-4-yl)-propionamide or N—[(R)-2-(3-cyclopropylmethoxy-3-o-tolyl-azetidin-1-yl)-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(5-methyl-1H-imidazol-4-yl)-propionamide,
and
wherein said source of NB-UVB has a wavelength between 280 nm and 315 nm.

2. The system according to claim 1 , wherein said MC1R agonist is present in a composition applied topically or administered orally.

3. The system according to claim 2 , wherein said composition comprises, in a cosmetically acceptable medium, at least one MC1R agonist.

4. The system according to claim 2 , wherein said MC1R agonist is present in the composition at a concentration between about 0.001% and 10% by weight based on the total weight of the composition comprising it.

5. The system according to claim 1 , wherein the skin disease associated with hypopigmentation is selected from the group consisting of vitiligo, albinism, hypomelanoses, depigmentation by physical or chemical agents, post-inflammatory hypopigmentation, phenomenon of Sutton and other hypopigmentation lesions.

6. A method of treating a dermatological condition linked to a hypopigmentation, the method comprising administering to an individual subject in need thereof a composition comprising at least one MC1R receptor agonist in combination with NB-UVB,
wherein said MC1R agonist is N-[(R)-2-[3-(4-hydroxybutoxy)-3-o-tolyl-azetidin-1-yl]-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(1H-imidazol-4-yl)-propionamide or N—[(R)-2-(3-cyclopropylmethoxy-3-o-tolyl-azetidin-1-yl)-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(5-methyl-1H-imidazol-4-yl)-propionamide,
and
wherein said source of NB-UVB has a wavelength between 280 nm and 315 nm.

7. A method of treating a dermatological condition linked to hypopigmentation, the method comprising applying to an affected or susceptible area, a combination of at least one MC1R receptor agonist and NB-UVB for simultaneous or sequential in time treatment of the dermatological condition,
wherein said MC1R agonist is N-[((R)-2-[3-(4-hydroxybutoxy)-3-o-tolyl-azetidin-1-yl]-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(1H-imidazol-4-yl)-propionamide or N—[(R)-2-(3-cyclopropylmethoxy-3-o-tolyl-azetidin-1-yl)-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(5-methyl-1H-imidazol-4-yl)-propionamide,
and
wherein said source of NB-UVB has a wavelength between 280 nm and 315 nm.

8. The method according to claim 7 , wherein the skin disease associated with hypopigmentation is selected from the group consisting of vitiligo, albinism, hypomelanoses, depigmentation by physical or chemical agents, post-inflammatory hypopigmentation, phenomenon of Sutton and other hypopigmentation lesions.

9. A product containing a composition comprising at least one MC1R receptor agonist for use in combination with NB-UVB, as a medicament for simultaneous or sequential in time treatment of dermatological conditions linked to a hypopigmentation,
wherein said MC1R agonist is N-[((R)-2-[3-(4-hydroxybutoxy)-3-o-tolyl-azetidin-1-yl]-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(1H-imidazol-4-yl)-propionamide or N—[(R)-2-(3-cyclopropylmethoxy-3-o-tolyl-azetidin-1-yl)-1-(4-methoxybenzyl)-2-oxo-ethyl]-3-(5-methyl-1H-imidazol-4-yl)-propionamide,
and
wherein said source of NB-UVB has a wavelength between 280 nm and 315 nm.

10. The system according to claim 1 , wherein the NB-UVB length wave is between 305 nm and 310 nm.

11. The system according to claim 1 , wherein the NB-UVB length wave is between 307 nm and 309 nm.

12. The method according to claim 6 , wherein the NB-UVB length wave is between 305 nm and 310 nm.

13. The method according to claim 6 , wherein the NB-UVB length wave is between 307 nm and 309 nm.

14. The method according to claim 7 , wherein the NB-UVB length wave is between 305 nm and 310 nm.

15. The method according to claim 7 , wherein the NB-UVB length wave is between 307 nm and 309 nm.

Assignees

• Galderma Res & Dev

Inventors

• Chomat Carole
• Martel Philippe
• Voegel Johannes

Classifications

• A61N2005/0661

  ultraviolet · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K31/4178

  not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin · CPC title

• A61K31/435

  having six-membered rings with one nitrogen as the only ring hetero atom · CPC title

• A61K38/34

  Melanocyte stimulating hormone [MSH], e.g. alpha- or beta-melanotropin · CPC title