Cosmetic/dermatological applications of PPAR receptor activators

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Patent No.: US None
App. No.: 11/444,371

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Abstract

Cosmetic/pharmaceutical compositions useful for regulating the size of sebaceous glands and, in particular, for inhibiting sebum production, or for treating pathologies entailing an overproduction of sebum, or for treating greasy skin and/or a scalp prone to dandruff, contain thus effective amounts of at least one activator of PPAR type receptors.

Claims (50)

1 . A regime or regimen for regulating the size of sebaceous glands, comprising administering to a subject in need of such treatment, a thus effective amount of at least one activator of PPAR type receptors.

2 . The regime or regimen as defined by claim 1 , said effective amount of at least one activator of PPAR type receptors inhibiting the production of sebum by the sebaceous glands.

3 . The regime or regimen as defined by claim 1 , said at least one activator of PPAR type receptors having, for at least one of the subtypes PPAR α, γ or δ, a dissociation constant Kdapp of less than or equal to 500 nM.

4 . The regime or regimen as defined by claim 3 , said dissociation constant Kdapp being less than or equal to 100 nM.

5 . The regime or regimen as defined by claim 1 , said at least one activator of PPAR type receptors having, for at least the subtype PPAR-γ, a dissociation constant Kdapp of less than or equal to 500 nM.

6 . The regime or regimen as defined by claim 5 , said dissociation constant Kdapp being less than or equal to 100 nM.

7 . The regime or regimen as defined by claim 5 , said at least one activator of PPAR-γ type receptors being specific.

8 . The regime or regimen as defined by claim 1 , comprising topically applying a composition containing said effective amount of at least one activator of PPAR type receptors onto the skin, mucous membranes or keratin fibers of said subject in need of such treatment.

9 . A regime or regimen for treating perioral dermatitis, a pathology associated with hyperplasia of the sebaceous glands, hereditary hyperplasia of the sebaceous glands, the overproduction of sebum associated with a hormonal disorder, or hyperandrogeny of endocrine origin, comprising administering to a subject in need of such treatment, a thus effective amount of at least one activator of PPAR type receptors.

10 . A regime or regimen for treating greasy skin or a skin prone to dandruff, comprising administering to a subject in need of such treatment, a thus effective amount of at least one activator of PPAR type receptors.

11 . The regime or regimen as defined by claim 10 , comprising topically applying said at least one activator of PPAR type receptors onto the skin, mucous membranes or keratin fibers of said subject in need of such treatment.

12 . The regime or regimen as defined by claim 1 , said at least one activator of PPAR type receptors comprising:

1. 5-{4-2-methylpyrid-2-ylamino)ethoxy]benzyl}-thiazolidine-2,4-dione,

2. N-methyl-N-[4′-(2,4-dioxothiazolidin-5-ylmethyl)-biphenyl-3-ylmethyl)-6-(2-methoxyethoxymethoxy)-naphthalene-2-carboxamide,

3. (S)-3-[3′-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-[2-(1-phenylmethanoyl)phenylamino]propionic acid,

4. N-methyl-N-[4′-(2,4-dioxothiazolidin-5-ylmethyl)-biphenyl-3-ylmethyl]-6-propoxynaphthalene-2-carboxamide,

5. (S)-2-ethoxy-3-{3′-[(methyloctanoylamino)methyl]biphenyl-4-yl}propionic acid,

6. 2-{3′-[({1-[6-(2-methoxyethoxymethoxy)naphthalene-2-yl]methanoyl}methylamino)methyl]biphenyl-4-ylamino}-benzoic acid,

7. (S)-3-{3′-[3-(4-dimethylaminophenyl)-1-methyl-ureido]biphenyl -4-yl}-2-[2-(1-phenylmethanoyl)phenyl-amino]propionic acid,

8. 2-(4-{2-[3-(2,4-difluorophenyl)-1-heptylureido]ethyl}phenylsulfanyl)-2-methylpropionic acid,

9. 1-[4′-(2,4-dioxothiazolidin-5-ylmethyl)biphenyl-3-yl]-3-heptyl-1-methylurea,

10. {3-[4-(3-cyclohexyl-1-phenethylureido)phenyl sulfanyl]phenyl}acetic acid,

11. {3-[4-(3-hexyl-1-phenethylureido)phenylsulfanyl]-phenyl}acetic acid,

12. {3-[4-(1-butyl-3-cyclohexylureido)phenylsulfanyl]-phenyl)acetic acid,

13. {3-[4-(3-benzyl-1-butylureido)phenylsulfanyl]-phenyl}acetic acid,

14. (S)-3-[3′-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-[2-(1-phenylmethanoyl)phenylamino]propionic acid, and/or

15. ethyl (S)-3-[3′-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-[2-(1-phenylmethanoyl)phenylamino]propionate.

13 . A cosmetic/dermatological composition suited for regulating the size of sebaceous glands, comprising a thus effective amount of at least one activator of PPAR type receptors, formulated into a physiologically acceptable medium therefor.

14 . The cosmetic/dermatological composition as defined by claim 13 , comprising from 0.001% to 10% by weight of said at least one activator of PPAR type receptors.

15 . The cosmetic/dermatological composition as defined by claim 13 , comprising from 0.01% to 1% by weight of said at least one activator of PPAR type receptors.

16 . The cosmetic/dermatological composition as defined by claim 13 , comprising a matting agent.

17 . The cosmetic/dermatological composition as defined by claim 13 , comprising an anti-dandruff agent.

18 . The cosmetic/dermatological composition as defined by claim 13 , formulated for topical application onto the skin, mucous membranes or keratin fibers.

19 . The cosmetic/dermatological composition as defined by claim 13 , said at least one activator of PPAR type receptors comprising: