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Compounds, formulations, and methods for treating or preventing rosacea

a technology for rosacea and rosacea gel, applied in the field of compound and method for treating or preventing rosacea, can solve the problem that the skin cannot penetrate in sufficient amounts to induce serious systemic side effects, and achieve the effect of ameliorating reducing the symptoms of rosacea

Inactive Publication Date: 2006-08-03
GALDERMA LAB LP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides methods, compounds, and topical skin formulations for treatment of rosacea and its symptoms. The compounds are α2 adrenoceptor agonists that act on the peripheral vasculature to cause vasoconstriction and thereby ameliorate the symptoms of rosacea. The compounds are delivered in a topical skin composition that insures that the compounds are effective in the skin of a patient but do not penetrate the skin in sufficient amounts to induce serious systemic side effects. The compounds are represented by Formula I below: \n\nFormula I: \n\nCompounds of this embodiment of the invention are topical formulations that can be applied to the skin to treat or prevent rosacea. These formulations can be aqueous or non-aqueous solutions, creams, lotions, gels, or ointments. The compounds of this embodiment are effective in reducing the symptoms of rosacea by causing vasoconstriction in the peripheral vasculature."

Problems solved by technology

The compounds are delivered in a topical skin composition that insures that the compounds are effective in the skin of a patient but do not penetrate the skin in sufficient amounts to induce serious systemic side effects.

Method used

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  • Compounds, formulations, and methods for treating or preventing rosacea
  • Compounds, formulations, and methods for treating or preventing rosacea
  • Compounds, formulations, and methods for treating or preventing rosacea

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Embodiment Construction

1.1 COMPOUNDS OF THE INVENTION

[0019] In one embodiment, the invention is directed to compounds of the Formula I:

[0020] wherein each of R1, R2, and R3 is independently hydrogen, halogen, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy; each of R4 and R5 is independently hydrogen, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy. In a preferred embodiment of the compounds of Formula I, R6 and R7 are both hydrogen. In another preferred embodiment, R4 and R5 are both hydrogen.

[0021] In another embodiment, the invention is directed to compounds of the Formula Ia;

[0022] wherein each of R1, R2, and R3 is independently hydrogen, halogen, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy; each of R4 and R5 is independently hydrogen, alkyl, pref...

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Abstract

In methods, compounds, and topical formulations for treatment of rosacea incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat rosacea and its symptoms.

Description

CROSS REFERENCE TO RELATED APPLICATION [0001] This application is a continuation of U.S. patent application Ser. No. 10 / 853,585, filed May 25, 2004, which in turn claims priority from U.S. Patent Application Ser. No. 60 / 473,611, filed on May 27, 2003, both of which are incorporated herein by reference.FIELD OF THE INVENTION [0002] The present invention is directed to compounds and methods for treatment or prevention of rosacea. The compounds and methods taught by the present invention are particularly useful for treating or preventing rosacea and the symptoms of rosacea. BACKGROUND OF THE INVENTION [0003] Many people are affected by inflammatory skin disorders that result in unsightly and painful rashes, acne, persistent red veins, and acne-like skin eruptions, such as macules, nodules, and pustules that may ooze or crust. Inflammatory skin disorders often result in intense psychosocial distress. Rosacea is a common inflammatory skin disorder affecting over 10 million people in the ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/498A61K31/4164A61K31/137A61K31/00A61K45/06
CPCA61K31/00A61K31/137A61K31/4164A61K31/498A61K31/4174A61K45/06A61K2300/00A61P17/00A61P17/10A61P29/00A61P7/10A61P9/00Y02A50/30A61K9/0014A61K9/06
Inventor DEJOVIN, JACKROSSI, THOMAS M.
Owner GALDERMA LAB LP
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