Method of using (2-imidazolin-2-ylamino) quinoxalines in treating ocular neural injury

Abstract

The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from ischemia, e.g. spinal ischemia.

1 . A method comprising: 
 a) identifying a mammal suffering from or at risk of suffering from glaucoma; and    b) administering to said mammal for the purpose of providing protection of the optic nerve or retina an effective amount of an aryl-imino-2-imidazolidine of formula I                          wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2-or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof.    
     
     
         2 . The method of  claim 1  wherein said mammal is a human.  
     
     
         3 . The method of  claim 2  further comprising administering to said mammal a separate intraocular pressure lowering medicament.  
     
     
         4 . The method of  claim 2  wherein the mammal has normal intraocular pressure.  
     
     
         5 . The method of any of claims  2 ,  3  or  4  wherein the protection is prophylactic.  
     
     
         6 . The method of any of claims  2 ,  3 ,  4  or  5  wherein the effective amount is administered in a series of treatments over a period to time.  
     
     
         7 . The method of any of claims  2 ,  3 ,  4 ,  5  or  6  wherein the aryl-imino-2-imidazolidine is  
       
         
           
           
               
               
           
         
       
     
     
         8 . The method of any of claims  2 ,  3 ,  4 ,  5 ,  6  or  7  further comprising topically administering said aryl-imino-2-imidazolidine of formula I to said mammal.  
     
     
         9 . A method comprising: 
 b) identifying a mammal suffering from or at risk of suffering from glaucoma; and    b) topically administering to said mammal for the purpose of providing protection of the optic nerve or retina an effective amount of an aryl-imino-2-imidazolidine of formula II                          or a pharmaceutically acceptable salt thereof.    
     
     
         10 . The method of  claim 9  wherein said mammal is a human.  
     
     
         11 . The method of  claim 10  further comprising administering to said mammal a separate intraocular pressure lowering medicament.  
     
     
         12 . The method of  claim 10  wherein the mammal has normal intraocular pressure.  
     
     
         13 . The method of any of claims  10 ,  11  or  12  wherein the protection is prophylactic.  
     
     
         14 . The method of any of claims  10 ,  11 ,  12  or  13  wherein the effective amount is administered in a series of treatments over a period to time.  
     
     
         15 . A method comprising: 
 c) identifying a human suffering from or at risk of suffering from glaucoma; and    b) topically administering to said human for the purpose of providing protection of the optic nerve or retina an effective amount of an aryl-imino-2-imidazolidine of formula II                          or a pharmaceutically acceptable salt thereof and mixtures thereof.