USRE37770EExpiredUtility

Treatment of skin conditions by use of PPARα activators

75
Assignee: UNIV CALIFORNIAPriority: Jan 24, 1997Filed: Jan 8, 2001Granted: Jun 25, 2002
Est. expiryJan 24, 2017(expired)· nominal 20-yr term from priority
Inventors:Peter M. EliasNathan N. BassKaren HanleyKenneth R. Feingold
A61K 31/192A61K 31/20A61K 31/00A61K 31/045A61K 31/08A61K 31/11A61K 31/201A61K 31/202A61K 31/215A61K 31/216A61K 31/22A61K 31/336A61K 31/505A61K 31/56A61K 31/575
75
PatentIndex Score
6
Cited by
12
References
18
Claims

Abstract

Disorders of the skin and mucous membrane that have a disrupted or dysfunctional epidermal barrier are treated or prevented by topical application of compounds that are either activators of the farnesoid X receptor, activators of the peroxisome proliferator-activated receptor alpha, and oxysterol activators of the LXRalpha receptor. The same compounds are also effective in treating disorders of epidermal differentiation and proliferation.

Claims

exact text as granted — not AI-modified
We claim:  
     
       1. A method for treating the epidermis of a terrestrial mammalian subject suffering from a perturbed epidermal barrier function, said method comprising topically applying to said epidermis a topical composition comprising an activator of peroxisome proliferator-activated receptor α selected from the group consisting of  5 , 8 , 11 , 14 - eicosatetraynoic acid,  (   4   - chloro -   6   -(   2 , 3   - xylidino )-   2   - pyrimidinyl ) thioacetic acid, cloribrate, and gemfibrozil  in an amount effective in enhancing barrier development. 
     
     
       2. A method in accordance with  claim 1  in which said activator is a member selected from the group consisting of linoleic acid, oleic acid, 5, 8, 11, 14-eicosatetraynoic acid, 4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thioacetic acid, clofibrate, and gemfibrozil. 
     
     
       3. A method in accordance with  claim 1  in which said activator is linoleic acid. 
     
     
       4. A method in accordance with  claim 1  in which said activator is clofibrate. 
     
     
       5. A method in accordance with  claim 1  in which the concentration of said active ingredient is from about 10 μm to about 1000 μM. 
     
     
       6. A method in accordance with  claim 1  in which said active ingredient is clofibrate and the concentration of said active ingredient is from about 100 μM to about 1,000 μM. 
     
     
       7. A method in accordance with  claim 1  in which said active ingredient is oleic acid and the concentration of said active ingredient is from about 100 μm to about 1000 μM. 
     
     
       8. A method in accordance with  claim 1  in which said active ingredient is linoleic acid and the concentration of said active ingredient is from about 5 μM to about 50 μM. 
     
     
       9. A method in accordance with  claim 1  in which said activator is gemfibrozil. 
     
     
       10. A method for treating the epidermis or mucous membrane of a terrestrial mammalian subject suffering from disturbed differentiation or excess epidermis of mucous membrane proliferation, said method comprising topically applying to said epidermis or  of mucous membrane a topical composition comprising an activator of peroxisome proliferator-activated receptor α selected from the group consisting of  5 , 8 , 11 , 14 - eicosatetraynoic acid,  (   4   - chloro -   6   -(   2 , 3   - xylidino )-   2   - pyrimidinyl ) thioacetic acid, cloribrate, and gemfibrozil  in an amount effective in reducing said condition. 
     
     
       11. A method in accordance with  claim 10  in which said activator is a member selected from the group consisting of linoleic acid, oleic acid, 5, 8, 11, 14-eicosatetraynoic acid, 4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thioacetic acid, clofibrate, and gemfibrozil. 
     
     
       12. A method in accordance with  claim 10  in which said activator is linoleic acid. 
     
     
       13. A method in accordance with  claim 10  in which said activator is clofibrate. 
     
     
       14. A method in accordance with  claim 10  in which the concentration of said active ingredient is from about 10 μM to about 1000 μM. 
     
     
       15. A method in accordance with  claim 10  in which said active ingredient is clofibrate and the concentration of said active ingredient is from about 100 μM, to about 1,000 μM. 
     
     
       16. A method in accordance with  claim 10  in which said active ingredient is oleic acid and the concentration of said active ingredient is from about 100 μM to about 1000 μM. 
     
     
       17. A method in accordance with  claim 10  in which said active ingredient is linoleic acid and the concentration of said active ingredient is from about 5 μM to about 50 μM. 
     
     
       18. A method in accordance with  claim 10  in which said activator is gemfibrozil.

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