CA2530938A1 - Compounds, formulations, and methods for treating or preventing rosacea - Google Patents
Compounds, formulations, and methods for treating or preventing rosacea Download PDFInfo
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- CA2530938A1 CA2530938A1 CA002530938A CA2530938A CA2530938A1 CA 2530938 A1 CA2530938 A1 CA 2530938A1 CA 002530938 A CA002530938 A CA 002530938A CA 2530938 A CA2530938 A CA 2530938A CA 2530938 A1 CA2530938 A1 CA 2530938A1
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- pharmaceutically acceptable
- topical composition
- independently hydrogen
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
In methods, compounds, and topical formulations for treatment of rosacea incorporating compounds represented by the formulas below: (I) 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.
Claims (28)
1. A method of treating or preventing rosacea and the symptoms associated therewith, comprising topically administering to the skin of a patient in need of such treatment or prevention a composition comprising:
a therapeutically effective amount of at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.
a therapeutically effective amount of at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.
2. The method according to claim 1 wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is selected from the group consisting of the compounds shown 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.
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.
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 1, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is a reversible .alpha.2 adrenergic receptor agonist or a pharmaceutically acceptable salt thereof.
5. The method according to claim 1, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is administered in an amount sufficient to decrease blood flow through the small arteries or arterioles of the skin of the patient.
6. 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.
7. The method according to claim 1, wherein the composition acts locally in the skin of the patient.
8. A topical composition suitable for treating or preventing the symptoms of rosacea comprising:
at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof;
and a pharmaceutically acceptable carrier.
at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof;
and a pharmaceutically acceptable carrier.
9. The topical composition according to claim 8, 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.
10. The topical composition according to claim 8, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is selected from the group consisting of the compounds shown 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.
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.
11. The topical composition according to claim 8, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is selected from the group consisting of brimonidine, naphazoline, tetrahydrozoline, oxymetazoline, xylometazoline, epinephrine, norepinephrine, phenylephrine, and methoxamine.
12. The topical composition according to claim 8, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is present in an amount in the range of about 0.01 to 5 weight percent.
13. The topical composition according to claim 8, wherein the pH value of the composition is in the range of about 5 to 8.
14. The topical composition according to claim 9, wherein the pharmaceutically acceptable carrier is an aqueous gel comprising water, and a water-gelling amount of a pharmaceutically acceptable gelling agent selected from the group consisting of carbomers, glycerine polyacrylate, and mixtures thereof, the topical composition having a physiologically acceptable pH.
15. The topical composition according to claim 14, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is present in an amount in the range of about 0.01 to 5 weight percent.
16. The topical composition according to claim 14, wherein the pH value of the composition is in the range of about 5 to 8.
17. The topical composition according to claim 14, further comprising a preservative.
18. The topical composition according to claim 14, further comprising a local anesthetic.
19. The topical composition according to claim 14, further comprising a skin humectant.
20. A package for a topical composition suitable for treating or preventing the symptoms of rosacea comprising at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, comprising a container and instructions for use of the topical composition.
21. The topical composition according to claim 9, wherein the pharmaceutically acceptable carrier is at least one of a cream and an ointment comprising stearic acid, stearyl alcohol, cetyl alcohol, glycerin, and water, the topical composition having a physiologically acceptable pH.
22. The topical composition according to claim 21, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is present in an amount in the range of about 0.01 to 5 weight percent.
23. The topical composition according to claim 21, wherein the pH value of the composition in the range of about 5 to 8.
24. The topical composition according to claim 21, further comprising a preservative.
25. The topical composition according to claim 21, further comprising a local anesthetic.
26. The topical composition according to claim 21, further comprising a skin humectant.
27. The topical composition according to claim 8, wherein the at least one of an .alpha.2 adrenergic receptor agonist and a pharmaceutically acceptable salt thereof is provided in a concentration sufficient to decrease blood flow through the small arteries or arterioles of the skin of the patient to which it is applied.
28. The topical composition according to claim 8, wherein the composition acts locally in the skin of the patient.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US47361103P | 2003-05-27 | 2003-05-27 | |
US60/473,611 | 2003-05-27 | ||
US10/853,585 | 2004-05-25 | ||
US10/853,585 US7439241B2 (en) | 2003-05-27 | 2004-05-25 | Compounds, formulations, and methods for treating or preventing rosacea |
PCT/US2004/016799 WO2004105703A2 (en) | 2003-05-27 | 2004-05-26 | Compounds, formulations, and methods for treating or preventing rosacea |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2530938A1 true CA2530938A1 (en) | 2004-12-09 |
CA2530938C CA2530938C (en) | 2011-12-13 |
Family
ID=33457481
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2530938A Expired - Fee Related CA2530938C (en) | 2003-05-27 | 2004-05-26 | Compounds, formulations, and methods for treating or preventing rosacea |
Country Status (22)
Country | Link |
---|---|
US (13) | US7439241B2 (en) |
EP (3) | EP2815748B1 (en) |
CN (4) | CN101380321B (en) |
AT (1) | ATE530185T1 (en) |
AU (1) | AU2004242967C1 (en) |
CA (1) | CA2530938C (en) |
CY (3) | CY1112242T1 (en) |
DK (3) | DK2815748T3 (en) |
ES (3) | ES2376172T5 (en) |
HK (3) | HK1084591A1 (en) |
HR (1) | HRP20150957T1 (en) |
HU (3) | HUE027616T2 (en) |
IL (1) | IL172612A (en) |
LT (1) | LT2815748T (en) |
LU (1) | LU92462I2 (en) |
MX (1) | MXPA05014107A (en) |
NO (1) | NO333468B1 (en) |
NZ (1) | NZ544300A (en) |
PL (3) | PL1631293T5 (en) |
PT (3) | PT1631293E (en) |
SI (3) | SI2815748T1 (en) |
WO (1) | WO2004105703A2 (en) |
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