IP Library Granted Patent US 8,557,817
Granted Patent B2
US 8,557,817 · App. 13/545,566 · Granted Oct 15, 2013

Compounds, formulations, and methods for treating or preventing inflammatory skin disorders

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Quick Facts
Patent No.
US 8,557,817
App. No.
13/545,566
Granted
Oct 15, 2013
Kind
B2
Abstract

In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R 1 , R 2 , and R 3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R 4 and R 5 is independently hydrogen, alkyl, or alkoxy; and each of R 6 and R 7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A 1 , A 3 , and A 4 is independently hydrogen or alkyl; and A 2 is independently hydrogen or hydroxy; and wherein each of B 1 , B 2 , and B 3 is independently hydrogen, hydroxy, or alkoxy; and each of B 4 and B 5 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 inflammatory skin disorders and the symptoms associated therewith.

Claims (13)

1. A method of treating rhinophyma, comprising topically administering to the skin of a patient in need of such treatment a composition comprising:

a therapeutically effective amount of at least one of an α 2 adrenergic receptor agonist or a pharmaceutically acceptable salt thereof; and

a pharmaceutically acceptable carrier.

2. The method according to claim 1 , wherein the at least one of an α 2 adrenergic receptor agonist or a pharmaceutically acceptable salt thereof is selected from the group consisting of the compounds shown below:

wherein each of R 1 , R 2 , and R 3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R 4 and R 5 is independently hydrogen, alkyl, or alkoxy; and each of R 6 and R 7 is independently hydrogen, nitro, alkyl, or alkoxy;

wherein each of A 1 , A 3 , and A 4 is independently hydrogen or alkyl; and A 2 is independently hydrogen or hydroxy; and

wherein each of B 1 , B 2 , and B 3 is independently hydrogen, hydroxy, or alkoxy; and each of B 4 and B 5 is independently hydrogen or alkyl.

3. The method according to claim 2 , wherein the compounds are selected from the group consisting of brimonidine, naphazoline, tetrahydrozaline, oxymetazoline, xylometazoline, epinephrine, nerepinephrine, phenylephrine, and methoxamine.

4. The method according to claim 2 , wherein the compound is brimonidine, or its analogs, or pharmaceutically acceptable salts thereof.

5. The method according to claim 4 , wherein the compound is brimonidine tartrate.

6. The method according to claim 1 , wherein the at least one of an α 2 adrenergic receptor agonist or a pharmaceutically acceptable salt thereof is a reversible α 2 adrenergic receptor agonist or a pharmaceutically acceptable salt thereof.

7. The method according to claim 1 , wherein the pharmaceutically acceptable carrier is selected from the group consisting of sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions.

8. The method according to claim 1 , wherein the composition acts locally in the skin of the patient.

Assignments (4)
CHANGE OF NAME Recorded Dec 31, 2020
From: NESTLÉ SKIN HEALTH S.A.
To: GALDERMA HOLDING SA
Reel/Frame 054899/0803 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 8, 2016
From: GALDERMA LABORATORIES, L.P.
To: NESTLE SKIN HEALTH S.A.
Reel/Frame 039363/0320 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 5, 2014
From: GALDERMA LABORATORIES INC.
To: GALDERMA LABORATORIES, L.P.
Reel/Frame 034105/0937 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2012
From: DEJOVIN, JACK; DEJOVIN, ISABELLE JEAN
To: GALDERMA LABORATORIES INC.
Reel/Frame 028526/0427 →