Novel Antigiardial Agents and Methods of Use Thereof

Abstract

The present invention provides a method of preventing or treating one or more of the following medical conditions, or treating symptoms of one or more of the following medical conditions: amebic infections, giardiasis, estrogen deficient states, osteoporosis, cardiovascular heart disease, high cholesterol levels, hyperlipidemia, cancer by administering to a subject having, or predisposed to, one or more of the conditions, a therapeutically effective amount of a compound of the present invention and a pharmaceutically acceptable carrier.

1 - 11 . (canceled) 
   
   
       12 . A hormone replacement therapy regimen comprising:
 co-administering a therapeutically effective amount of a combination of mammalian estrogen and a compound of the following formula:   
     
       
         
         
             
             
         
       
       wherein R 2  and R 4  are each independently H, alkyl halogen; 
       R 15  and R 16  are each independently H, alkyl, acyl, alkoxy, aryl, amino, HET, halogen; 
       and pharmaceutically acceptable salts thereof; and 
       a pharmaceutically acceptable carrier to a woman having reduced levels of endogenous estrogen. 
     
   
   
       13 . A method for inhibiting or treating coronary heart disease, cardiovascular disease, comprising:
 administering a therapeutically effective amount of a compound of the following formula:   
     
       
         
         
             
             
         
       
       wherein R 2  and R 4  are each independently H, alkyl, halogen; 
       R 15  and R 16  are each independently H, alkyl, acyl, alkoxy, aryl, amino, HET, halogen; 
       and pharmaceutically acceptable salts thereof; and a pharmaceutically acceptable carrier to a patient in need thereof. 
     
   
   
       14 . A method of inhibiting or treating osteoporosis, comprising:
 administering a therapeutically effective amount of a compound of the following formula:   
     
       
         
         
             
             
         
       
       wherein R 2  and R 4  are each independently H, alkyl, halogen; 
       R 15  and R 16  are each independently H, alkyl, acyl, alkoxy, aryl, amino, HET, halogen; 
       and pharmaceutically acceptable salts thereof; and a pharmaceutically acceptable carrier to a patient in need thereof. 
     
   
   
       15 . A method of inhibiting or treating gastrointestinal disease, comprising:
 administering a therapeutically effective amount of a compound of the following formula:   
     
       
         
         
             
             
         
       
       wherein R 2  and R 4  are each independently H, alkyl, halogen; 
       R 15  and R 16  are each independently H, alkyl, acyl, alkoxy, aryl, amino, HET, halogen; 
       and pharmaceutically acceptable salts thereof; and a pharmaceutically acceptable carrier to a patient in need thereof. 
     
   
   
       16 . A method of inhibiting or treating amebic infections comprising:
 administering a therapeutically effective amount of a compound of the following formula:   
     
       
         
         
             
             
         
       
       wherein R 2  and R 4  are each independently H, alkyl, halogen; 
       R 15  and R 16  are each independently H, alkyl, acyl, alkoxy, aryl, amino, HET, halogen; 
       and pharmaceutically acceptable salts thereof; and a pharmaceutically acceptable carrier to a patient in need thereof. 
     
   
   
       17 . The method of  claim 12 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
   
   
       18 . The method of  claim 13 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
   
   
       19 . The method of  claim 14 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
   
   
       20 . The method of  claim 15 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
   
   
       21 . The method of  claim 16 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
   
   
       22 . The method of  claim 12 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
     
   
   
       23 . The method of  claim 13 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
     
   
   
       24 . The method of  claim 14 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
     
   
   
       25 . The method of  claim 15 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
     
   
   
       26 . The method of  claim 16 , wherein the compound is chosen from: 
     
       
         
         
             
             
         
       
     
   
   
       27 . The method of  claim 12 , wherein the R 16  is chosen from pyrrolidine, morpholine. 
   
   
       28 . The method of  claim 13 , wherein the R 16  is chosen from pyrrolidine, morpholine. 
   
   
       29 . The method of  claim 14 , wherein the R 16  is chosen from pyrrolidine, morpholine. 
   
   
       30 . The method of  claim 15 , wherein the R 16  is chosen from pyrrolidine, morpholine. 
   
   
       31 . The method of  claim 16 , wherein the R 16  is chosen from pyrrolidine, morpholine.