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

• US 9,610,461 B2
• Filed: 03/15/2013
• Issued: 04/04/2017
• Est. Priority Date: 03/15/2012
• Status: Expired due to Fees

• Current Assignee: Galderma Research And Development Snc (Nestle SA)
• Original Assignee: Galderma Research And Development Snc (Nestle SA)
• Inventors: Chomat, Carole, Martel, Philippe, Voegel, Johannes
• Primary Examiner(s): Cordero Garcia, Marcela M
• Application Number:
  US14/385,416
• Publication Number:
  US 20150045719A1
• Time in Patent Office: 1,481 Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/397 having four-membered rings, e.g. azetidine
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 31/4178 not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• CPC Class Codes: A61K 31/4196 1,2,4-Triazoles
• CPC Class Codes: A61K 31/435 having six-membered rings with one nitrogen as the only ring hetero atom
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/454 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• CPC Class Codes: A61K 38/33 derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
• CPC Class Codes: A61K 38/34 Melanocyte stimulating hormone [MSH], e.g. alpha- or beta-melanotropin
• CPC Class Codes: A61K 38/35 Corticotropin [ACTH]
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61N 2005/0661 ultraviolet
• CPC Class Codes: A61N 5/0614 Tanning
• CPC Class Codes: A61N 5/062 Photodynamic therapy, i.e. excitation of an agent
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: F04C 2270/041 Controlled or regulated

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.

Claims

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.

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.

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.

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.

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.

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.

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.