Substituted-aryl-(imidazole)-methyl)-phenyl compounds as subtype selective modulators of alpha 2b and/or alpha 2c adrenergic receptors

Abstract

A compound having selective modulating activity at the alpha 2B and or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein R 1 -R 6 is independently selected from the group consisting of H, C 1-6 alkyl, halogen, CH 2 OH, CH 2 N(R 7 ) 2 , CH 2 CN, C(O)R 8 , CF 3 , and aryl; wherein R 7 is H or C 1-6 alkyl; and R 8 is H, C 1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.

1 . A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound of formula 
       
         
           
           
               
               
           
         
         wherein 
         R 1 -R 6  is independently selected from the group consisting of H, C 1-6  alkyl, halogen, CH 2 OH, CH 2 N(R 7 ) 2 , CH 2 CN, C(O)R 8 , CF 3 , and aryl; wherein 
         R 7  is H or C 1-6  alkyl; 
         R 8  is H, C 1-6  alkyl or aryl; and 
         at least one additional component selected from the group consisting of one or more emulsifying agent, wetting agent, sweetening agent, flavoring agent, tonicity adjuster, preservative, buffer, anti-oxidant and combinations thereof. 
       
     
     
         2 . The pharmaceutical composition according to  claim 1  wherein the compound is selected from: 
       
         
           
           
               
               
           
         
       
     
     
         3 . A method comprising administering to a mammal a pharmaceutical composition according to  claim 1 , for treating autoimmune diseases, Crohn's disease, Alzheimer's, Parkinson's ALS, dry eye disorders, Tourette's syndrome. 
     
     
         4 . The method according to  claim 3  wherein the disease is an autoimmune disease. 
     
     
         5 . The method according to  claim 4  wherein the autoimmune disease is lupus erythematosis. 
     
     
         6 . The method according to  claim 3  wherein the disease is dry eye. 
     
     
         7 . The method according to  claim 3  wherein the disease is Crohn's disease. 
     
     
         8 . The method according to  claim 3  wherein the disease is Parkinson's ALS. 
     
     
         9 . The method according to  claim 3  wherein the disease is Alzheimer's. 
     
     
         10 . The method according to  claim 3  wherein the disease is Tourette's syndrome.