Rosacea: An Introduction

Summary

The present invention provides methods, compounds, and topical skin formulations for treatment of rosacea and its symptoms. Compounds of the invention are .alpha..sub.2 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.

Compounds of one embodiment of the invention are represented by Formula I below: 2

wherein each of R.sub.1, R.sub.2, and R.sub.3 is independently hydrogen, halogen, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy; each of R.sub.4 and R.sub.5 is independently hydrogen, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy; and each of R.sub.6 and R.sub.7 is independently hydrogen, nitro, alkyl, preferably, unsubstituted alkyl, or alkoxy, preferably, unsubstituted alkoxy. In a preferred embodiment of the compounds of Formula I, R.sub.6 and R.sub.7 are both hydrogen. In another preferred embodiment, R.sub.4 and R.sub.5 are both hydrogen.

To treat or prevent rosacea, according to the methods of the invention, the compounds of this embodiment of the invention are topically applied. Preferably the compounds of the invention are delivered in a topical formulation. Formulations for topical delivery of compounds of the invention are well-known in the art, such as aqueous or non-aqueous solutions or suspensions, creams, lotions, gels, or ointments.

Compounds of another embodiment of the invention are represented by Formula II below: 3

Compounds of another embodiment of the invention are represented by Formula III below:

Compounds of other embodiments of the invention are shown below:

These and other features, aspects, and advantages of the present invention will become better understood with reference to the following detailed description, examples, and claims.

These and other features, aspects, and advantages of the invention will become better understood with reference to the following detailed description, examples, and appended claims.


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