US2014094451A1PendingUtilityA1

Preventive or remedy for glaucoma

Assignee: KOWA COPriority: Jun 21, 2005Filed: Dec 6, 2013Published: Apr 3, 2014
Est. expiryJun 21, 2025(expired)· nominal 20-yr term from priority
A61P 43/00A61K 31/4725A61K 31/551A61P 27/02A61P 27/06A61K 45/06A61K 45/00A61K 31/517
51
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Claims

Abstract

There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an α 1 blocker in combination.

Claims

exact text as granted — not AI-modified
1 . (canceled) 
     
     
         2 . A method for treating glaucoma in a subject in need thereof, comprising:
 administrating to said subject an effective amount of a Rho kinase inhibitor and an effective amount of an α 1  blocker, wherein the Rho kinase inhibitor is (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine or a salt thereof.   
     
     
         3 . The method of  claim 2 , wherein the effective amount of the Rho kinase inhibitor is from 0.1 to 1000 μg per day. 
     
     
         4 . The method of  claim 3 , wherein the effective amount of the α 1  blocker is from 50 to 250 μg per day. 
     
     
         5 . The method of  claim 4 , wherein the α 1  blocker comprises at least one of bunazosin and bunazosin hydrochloride. 
     
     
         6 . The method of  claim 2 , wherein a solution comprising the Rho kinase inhibitor at 0.5% is administered. 
     
     
         7 . The method of  claim 6 , wherein a solution comprising the α 1  blocker at 0.01% is administered. 
     
     
         8 . The method of  claim 7 , wherein the solution comprising the α 1  blocker is administered prior to administration of the solution comprising the Rho kinase inhibitor. 
     
     
         9 . The method of  claim 2 , wherein a composition comprising the Rho kinase inhibitor and the α 1  blocker is administered. 
     
     
         10 . The method of  claim 9 , wherein the composition is at least one of an aqueous eye drop, a nonaqueous eye drop, a suspension eye drop, an emulsion eye drop, and an eye ointment. 
     
     
         11 . The method of  claim 9 , wherein the composition further comprises at least one selected from the group consisting of a tonicity agent, a chelating agent, a stabilizer, a pH modifier, a preservative, an antioxidant, a solubilizing agent, and a thickening agent. 
     
     
         12 . A method for treating ocular hypertension in a subject in need thereof, comprising:
 administrating to said subject an effective amount of a Rho kinase inhibitor and an effective amount of an α 1  blocker,   wherein the Rho kinase inhibitor is (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine or a salt thereof.   
     
     
         13 . The method of  claim 12 , wherein the effective amount of the Rho kinase inhibitor is from 0.1 to 1000 μg per day. 
     
     
         14 . The method of  claim 13 , wherein the effective amount of the α 1  blocker is from 50 to 250 μg per day. 
     
     
         15 . The method of  claim 14 , wherein the α 1  blocker comprises at least one of bunazosin and bunazosin hydrochloride. 
     
     
         16 . The method of  claim 12 , wherein a solution comprising the Rho kinase inhibitor at 0.5% is administered. 
     
     
         17 . The method of  claim 16 , wherein a solution comprising the α 1  blocker at 0.01% is administered. 
     
     
         18 . The method of  claim 17 , wherein the solution comprising the α 1  blocker is administered prior to administration of the solution comprising the Rho kinase inhibitor. 
     
     
         19 . The method of  claim 12 , wherein a composition comprising the Rho kinase inhibitor and the α 1  blocker is administered. 
     
     
         20 . The method of  claim 19 , wherein the composition is at least one of an aqueous eye drop, a nonaqueous eye drop, a suspension eye drop, an emulsion eye drop, and an eye ointment. 
     
     
         21 . The method of  claim 19 , wherein the composition further comprises at least one selected from the group consisting of a tonicity agent, a chelating agent, a stabilizer, a pH modifier, a preservative, an antioxidant, a solubilizing agent, and a thickening agent.

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