Male anti-fertility agents

Abstract

Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.

1 - 42 . (canceled)  
   
   
       43 . A method for inhibiting the ability of a male mammal to conceive progeny, comprising administering to said male mammal, for a period time effective to sufficiently reduce or eliminate spermatozoa in the semen of said male mammal, an effective amount of a compound represented by the following structure:  
     
       
         
         
             
             
         
       
       or a pharmaceutically acceptable salt thereof, wherein:  
       X 2  is CH or N;  
       R 2  is H, F, or OCH 3 ;  
       R 2 * is H or F;  
       R 8  is H, or lower alkyl of 1 to 6 carbons; and  
       R 14  is 4-(lower-alkyl)phenyl.  
     
   
   
       44 . The method of  claim 43 , wherein the effective amount of the compound is in a range of between about 0.5 mg/kg of body weight and about 0.001 mg/kg of body weight.  
   
   
       45 . The method of  claim 44 , wherein the effective amount of the compound is in a range of between about 0.3 mg/kg of body weight and about 0.005 mg/kg of body weight.  
   
   
       46 . The method of  claim 45 , wherein the effective amount of the compound is in a range of between about 0.075 mg/kg of body weight and about 0.01 mg/kg of body weight.  
   
   
       47 . A method for inhibiting the ability of a male mammal to conceive progeny, comprising administering to said male mammal, for a period time effective to sufficiently reduce or eliminate spermatozoa in the semen of said male mammal, an effective amount of a compound represented by the following structure:  
     
       
         
         
             
             
         
       
       or a pharmaceutically acceptable salt thereof.  
     
   
   
       48 . The method of  claim 47 , wherein the effective amount of the compound is in a range of between about 0.5 mg/kg of body weight and about 0.001 mg/kg of body weight.  
   
   
       49 . The method of  claim 48 , wherein the effective amount of the compound is in a range of between about 0.3 mg/kg of body weight and about 0.005 mg/kg of body weight.  
   
   
       50 . The method of  claim 49 , wherein the effective amount of the compound is in a range of between about 0.075 mg/kg of body weight and about 0.01 mg/kg of body weight.  
   
   
       51 . A method for inhibiting spermatogenesis in a male mammal, comprising administering to said male mammal, over a period of time effective to prevent conception, an effective amount of a compound represented by the following structure:  
     
       
         
         
             
             
         
       
       or a pharmaceutically acceptable salt thereof, wherein:  
       X 2  is CH or N;  
       R 2  is H, F, or OCH 3 ;  
       R 2 * is H or F;  
       R 8  is H, or lower alkyl of 1 to 6 carbons; and  
       R 14  is 4-(lower-alkyl)phenyl.  
     
   
   
       52 . The method of  claim 51 , wherein the effective amount of the compound is in a range of between about 0.5 mg/kg of body weight and about 0.001 mg/kg of body weight.  
   
   
       53 . The method of  claim 52 , wherein the effective amount of the compound is in a range of between about 0.3 mg/kg of body weight and about 0.005 mg/kg of body weight.  
   
   
       54 . The method of  claim 53 , wherein the effective amount of the compound is in a range of between about 0.075 mg/kg of body weight and about 0.01 mg/kg of body weight.  
   
   
       55 . A method for inhibiting spermatogenesis in a male mammal, comprising administering to said male mammal, over a period of time effective to prevent conception, an effective amount of a compound represented by the following structure:  
     
       
         
         
             
             
         
       
       or a pharmaceutically acceptable salt thereof.  
     
   
   
       56 . The method of  claim 55 , wherein the effective amount of the compound is in a range of between about 0.5 mg/kg of body weight and about 0.001 mg/kg of body weight.  
   
   
       57 . The method of  claim 56 , wherein the effective amount of the compound is in a range of between about 0.3 mg/kg of body weight and about 0.005 mg/kg of body weight.  
   
   
       58 . The method of  claim 57 , wherein the effective amount of the compound is in a range of between about 0.075 mg/kg of body weight and about 0.01 mg/kg of body weight.