Topical ocular analgesic agents

Abstract

The topical ophthalmic use of certain 2,4-diamino-substituted 1,3-triazines for preventing or alleviating ocular pain in patients is disclosed. Topical ocular pharmaceutical composition are also disclosed.

What is claimed is: 
     
         1 . A method for the treatment of ocular pain which comprises administering to a patient in need thereof a topical ophthalmic formulation containing a therapeutically effect amount of at least one compound of Formula I 
       
         
           
           
               
               
           
         
         wherein: 
       
       
         
           
           
               
               
           
         
         to Y=CH or N; 
         n=0 or 1, with the proviso that n=0 if Y=N; 
         X=a direct bond or CH 2 ; 
         Z=a phenyl or heteroatomic group, optionally substituted with phenyl, methyl; halo, trihalomethyl, or trihalomethoxy; and 
         R 2 =H, Me, or F, with the Me or F groups in the 2 or 6 positions on the acetamide-bearing phenyl ring, 
         wherein the patient has trauma due to accidental injury or surgical injury, uveitis, dry eye, or diabetic neuropathy. 
       
     
     
         2 . The method of  claim 1 , wherein said treatment comprises treatment with any of the following compounds: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         3 . The method of  claim 1 , wherein the compound of Formula I has the following structure: 
       
         
           
           
               
               
           
         
       
     
     
         4 . The method of  claim 1 , wherein the topical ophthalmic formulation comprises one or more ingredients selected from the group consisting of surfactants; tonicity agents; buffers; preservatives; co-solvents; and viscosity building agents. 
     
     
         5 . The method of  claim 1 , wherein the therapeutically effect amount of a compound of Formula I is between 0.01-3%. 
     
     
         6 . The method of  claim 5 , wherein the therapeutically effect amount of a compound of Formula I is between 0.1-1%. 
     
     
         7 . The method of  claim 1 , wherein the surgical injury is postoperative photorefractive keratectomy (PRK) surgery. 
     
     
         8 . A method of inhibiting sodium channel 1.7 (Nav 1.7) activity in the eye of a patient, comprising administering to a patient a topical ophthalmic formulation containing a therapeutically effect amount of at least one compound of Formula I 
       
         
           
           
               
               
           
         
         wherein: 
       
       
         
           
           
               
               
           
         
         Y=CH or N; 
         n=0 or 1, with the proviso that n=0 if Y=N; 
         X=a direct bond or CH 2 ; 
         Z=a phenyl or heteroatomic group, optionally substituted with phenyl, methyl; halo, trihalomethyl, or trihalomethoxy; and 
         R 2 =H, Me, or F, with the Me or F groups in the 2 or 6 positions on the acetamide-bearing phenyl ring. 
       
     
     
         9 . The method of  claim 8 , comprising administering any of the following compounds: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         10 . The method of  claim 8 , wherein the compound of Formula I has the following structure: 
       
         
           
           
               
               
           
         
       
     
     
         11 . The method of  claim 8 , wherein the topical ophthalmic formulation comprises one or more ingredients selected from the group consisting of surfactants; tonicity agents; buffers; preservatives; co-solvents; and viscosity building agents. 
     
     
         12 . The method of  claim 8 , wherein the therapeutically effect amount of a compound of Formula I is between 0.01-3%. 
     
     
         13 . The method of  claim 12 , wherein the therapeutically effect amount of a compound of Formula I is between 0.1-1%. 
     
     
         14 . The method of  claim 8 , wherein the patient has trauma due to accidental injury or surgical injury, uveitis, dry eye, or diabetic neuropathy.