IP Library › Granted Patent US 9,095,609
Granted Patent B2
US 9,095,609 · App. 13/821,840 · Granted Aug 4, 2015

Ophthalmic composition comprising ws-12 and methods to treat xerophthalmia

Inventors: Carlos Belmonte Martnez (San Joan d'Alacant, ES); Juana Gallar Martinez (San Joan d'Alacant, ES); Antonio Ferrer Montiel (San Joan d'Alacant, ES); Asia Fernández Carvajal (San Joan d'Alacant, ES); Félix Viana De La Iglesia (San Joan d'Alacant, ES)
Assignees: UNIVERSIDAD MIGUEL HERNÁNDEZ DE ELCHE; CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS (C.S.I.C.)
A61K45/00A61K31/00A61K31/045A61K31/047A61K31/075A61K31/16A61K31/164A61K31/167A61K31/17A61K31/196A61K31/215A61K31/22A61K31/221A61K31/245A61K31/27A61K31/352A61K31/357A61K31/381A61K31/4025A61K31/4164A61K31/4745A61K31/496A61K31/505A61K31/55A61K31/662A61K31/713A61K31/7105
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Quick Facts
Patent No.
US 9,095,609
App. No.
13/821,840
Granted
Aug 4, 2015
Kind
B2
Abstract

The invention relates to therapeutic compositions for the treatment of dry eye, more specifically to compositions comprising a TRPM8 receptor agonist ligand. Furthermore, the invention relates to therapeutic compositions for the treatment of epiphora, more specifically to compositions comprising a TRPM8 receptor antagonist.

Claims (24)

1. An ophthalmic composition comprising a therapeutically effective amount of WS-12 (2-isopropyl-5-methyl-cyclohexanecarboxylic acid (4-methoxy phenyl)-amide), wherein the amount of WS-12 can effectively treat or reduce the likelihood of xerophthalmia in a subject in need thereof, and wherein the amount of WS-12 is not cytotoxic.

2. The ophthalmic composition of claim 1 , wherein WS-12 acts as a Transient receptor potential cation channel subfamily M member 8 (TRPM8) agonist that has an efficacy of at least 50, 100, 1000 or 2000 times more than the other channel of other members of the Transient receptor potential cation channel subfamily M.

3. The ophthalmic composition of claim 1 , wherein the amount of WS-12 per dose ranges from 0.0005 milligrams to 0.1 milligrams.

4. The ophthalmic composition of claim 1 , wherein the amount of WS-12 per dose is about 0.0005 milligrams.

5. The ophthalmic composition of claim 1 , wherein the amount of WS-12 per dose ranges from 0.007 micrograms/kilogram to 0.01 milligrams/kilogram of body weight.

6. The ophthalmic composition of claim 1 , wherein the amount of WS-12 per dose is about 0.007 micrograms/kilogram of body weight.

7. The ophthalmic composition of claim 1 , wherein the composition can be administered a variable number of times a day.

8. The ophthalmic composition of claim 1 , wherein the composition can be administered from 1 to 4 times a day.

9. The ophthalmic composition according to claim 1 , wherein the composition comprises an additional TRPM8 agonist.

10. The ophthalmic composition according to claim 9 , wherein the additional TRPM8 agonist is selected from the group consisting of WS-3, WS-5, WS-11, WS-14, WS-23, WS-30, WS-148, menthol, and a combination thereof.

11. The ophthalmic composition according to claim 1 , wherein the composition further comprises a drug useful for the treatment of xerophthalmia.

12. The ophthalmic composition according to claim 11 , wherein the drug useful for the treatment of xerophthalmia is selected from the group consisting of a corticoid, vitamin A, pylocarpine, hypromellone, carbomer, cyclosporine, and a combination thereof.

13. The ophthalmic composition according to claim 1 , wherein the composition comprises a lubricant.

14. The ophthalmic composition according to claim 13 , wherein the lubricant is selected from the group consisting of glycerol, hydroxypropyl methylcellulose, hydroxymethyl cellulose, carboxymethyl cellulose, polyethylene glycol, polyvinyl alcohol, hyaluronic acid, castor oil, mineral oil, and combinations thereof.

15. The ophthalmic composition according to claim 1 , wherein the composition comprises a pharmaceutically acceptable vehicle.

16. The ophthalmic composition according to claim 1 , wherein the subject is an animal subject.

17. A method to treat or reduce the likelihood of xerophthalmia, comprising the administration of a therapeutically effective amount of a composition comprising WS-12 (2-isopropyl-5-methyl-cyclohexanecarboxylic acid (4-methoxyphenyl)-amide) to an individual suffering from xerophthalmia.

18. The method of claim 17 , wherein WS-12 acts as a TRPM8 agonist that has an efficacy of 50, 100, 1000 or 2000 times more than the other channel of other members of the Transient receptor potential cation channel subfamily M.

19. The method of claim 17 , wherein the dose of WS-12 ranges from 0.0005 milligrams to 0.1 milligrams.

20. The method of claim 17 , wherein the dose of menthol and/or WS-12 is about 0.0005 milligrams.

21. The method of claim 17 , wherein the dose of WS 12 ranges from 0.007 micrograms/kilogram to 0.01 milligrams/kilogram of body weight.

22. The method of claim 17 , wherein the dose of WS-12 is about 0.007 micrograms/kilogram of body weight.

23. The method of claim 17 , wherein the composition is administered a variable number of times a day.

24. The method of claim 17 , wherein the composition is administered from 1 to 4 times a day.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2013
From: BELMONTE MARTINEZ, CARLOS; GALLAR MARTINEZ, JUANA; FERRER MONTIEL, ANTONIO; FERNANDEZ CARVAJAL, ASIA; VIANA DE LA IGLESIA, FELIX
To: UNIVERSIDAD MIGUEL HERNANDEZ DE ELCHE; CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS (C.S.I.C)
Reel/Frame 030434/0699 →
Priority Claims (1)
ES 201031341 · Sep 8, 2010 · national
Continuity (1)
Related Publication 20130245231A1 · Sep 19, 2013