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Use of 2,5-Dihydroxybenzene Derivatives for Treating Actinic Keratosis

a technology of hydroxybenzene and derivatives, which is applied in the direction of drug compositions, metabolism disorders, therapy, etc., can solve the problems of no effective treatment for skin photoaging and no effective treatment for obesity

Inactive Publication Date: 2008-05-29
ACTION MEDICINES SL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007]Surprisingly, the inventors have found that 2,5-dihydroxybenzene derivatives, the pharmaceutically acceptable salts and solvates thereof, as well as isomers and prodrugs thereof are useful to prevent and / or therapeutically treat skin aging due to exposure to ultraviolet rays B (UVB), or to exposure to sun rays in general, to treat pathologies associated with said skin photoaging such as skin wrinkles, actinic keratosis, skin pigmentation and hyperpigmentation, as well to treat hirsutism and hypertricosis, obesity due to excessive adipogenesis, and to treat viral warts.

Problems solved by technology

Currently, there is no effective treatment for skin photoaging (Dermatol Surg.
Currently, there is no effective treatment for obesity.

Method used

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  • Use of 2,5-Dihydroxybenzene Derivatives for Treating Actinic Keratosis
  • Use of 2,5-Dihydroxybenzene Derivatives for Treating Actinic Keratosis
  • Use of 2,5-Dihydroxybenzene Derivatives for Treating Actinic Keratosis

Examples

Experimental program
Comparison scheme
Effect test

example 1

Assay of 2,5-dihydroxybenzenesulfonic Acid on Photoaged Skin

[0277]In this study, 2,5-dihydroxybenzenesulfonic acid, potassium salt, formulated as 5% by weight in the form of cream has been used, since this type of formulation is a habitual procedure for topical treatments of the skin. Distilled water has been used as the aqueous phase of the cream. The oil phase thereof may comprise cetyl alcohol, stearyl alcohol or vaseline. Span (sorbitan monooleate) is an effective emulsifier to make the cream.

[0278]The following example illustrates the formulation of an effective cream for the topical treatment of skin photoaging and must not be construed as a limitation of the scope of the invention.

[0279]Active principle: 2,5-dihydroxybenzenesulfonic acid, potassium salt, 5% by weight. Excipients: cetyl alcohol (2.5%), stearyl alcohol (2.5%), liquid vaseline (30%), white soft vaseline (20%), sorbitan monooleate (5%) and distilled water (q.s. to 100 g).

[0280]Continuous topical treatment of huma...

example 2

Effect of 2,5-dihydroxybenzenesulfonate on Seborrheic Keratosis, Actinic Keratosis and Viral Warts

[0281]Topical treatment with the above described cream (twice a day for 11 days) of human skin (basal conditions shown in FIG. 2A) results in a reduction of seborrheic keratosis (big circle) as well as of viral warts (small circle), as shown in FIG. 2B.

[0282]Another example of the effect of 2,5-dihydroxybenzenesulfonate on seborrheic keratosis is shown in FIG. 3, wherein the seborrheic keratosis is reduced due to the topical treatment on the affected area for 4 weeks, twice a day, with an emulsion containing the 2,5-dihydroxybenzenesulfonic acid, 2.5% by weight.

[0283]The emulsion containing 2.5% by weight of 2,5-dihydroxybenzenesulfonic acid was also used to treat two lesions of actinic keratosis in the same patient, as shown in FIGS. 4 and 5. After 15 days of treatment with said emulsion (twice a day), the actinic keratosis was clearly reduced, and the effect was even more evident afte...

example 3

Effect of an Emulsion of 2.5% 2,5-dihydroxybenzenesulfonate on Actinic Keratosis

[0284]An emulsion containing 2.5% by weight of 2,5-dihydroxybenzenesulfonic acid was used to treat two lesions of actinic keratosis in the same patient, as shown in FIGS. 4 and 5. After 15 days of treatment with said emulsion (twice a day), the actinic keratosis was clearly reduced, and the effect was even more evident after 4 weeks of treatment. Calcium salt of 2,5-dihydroxybenzenesulfonic acid was used.

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Abstract

The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and / or phrophylactic treatment of, inter alia, actinic keratosis.

Description

RELATED APPLICATIONS[0001]This application is a continuation-in-part of U.S. Ser. No. 11 / 506,469, which is a national stage filing under 35 U.S.C. § 371 of International Application Number PCT / ES05 / 70017, filed Feb. 16, 2005, which claims the benefit of priority under 35 U.S.C. § 119 of ES Application Number P200400371, filed Feb. 17, 2004. In addition, this application claims the benefit of priority under 35 U.S.C. § 119 of ES Application No. P200602219, filed Aug. 16, 2006 and of ES Application No. P200701857, filed Jul. 2, 2007. The foregoing applications, and all documents cited therein, are hereby incorporated herein by reference in their entirety.FIELD OF THE INVENTION[0002]The present invention relates to the use of 2,5-dihydroxybenzene derivatives to manufacture medicaments useful to prevent and / or treat skin aging due to exposure to ultraviolet B rays (UVB), or to exposure to sun rays in general, to treat pathologies associated to said skin photoaging such as skin wrinkles ...

Claims

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Application Information

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IPC IPC(8): A61K31/22A61K31/192A61K31/185
CPCA61K31/185A61K31/192A61K31/22A61K31/56A61K31/59A61K31/60C07C309/60A61N5/062A61M37/00A61K45/06A61K31/216A61B17/320708C07C309/42A61P3/04A61P17/00A61P17/12A61P31/12
Inventor CUEVAS SANCHEZ, PEDROGIMENEZ GALLEGO, GUILLERMOSAENZ DE TEJADA MORGAN, INIGOANGULO FRUTOS, JAVIERVALVERDE LOPEZ, SERAFINROMERO GARRIDO, ANTONIOLOZANO PUERTO, ROSA MARIA
Owner ACTION MEDICINES SL
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