Method for the preparation of 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP)

Abstract

A 21-Hydroxy-6,19-oxidoprogesterone derivative of Formula (1): where R is —C(O)—CH 2 CH 3 , —C(O)—(CH 2 ) 2 —COOH, —C(O)—(CH 2 ) 7 —CH═CH—(CH 2 ) 7 —COOH, or —C(O)—PO 3 Na 2 .

1 - 13 . (canceled)  
     
     
         14 . A 21-Hydroxy-6,19-oxidoprogesterone derivative of Formula (1):  
       
         
           
           
               
               
           
         
       
       wherein R is selected for the group consisting of —C(O)—CH 2 CH 3 , —C(O)—(CH 2 ) 2 —COOH, —C(O)—(CH 2 ) 7 —CH═CH—(CH 2 ) 7 —COOH, and —C(O)—PO 3 Na 2 .  
     
     
         15 . The 21-hydroxy-6,19-oxidoprogesterone derivative of  claim 14 , wherein R is C(O)—(CH 2 ) 2 —COOH.  
     
     
         16 . A composition comprising the 21-hydroxy-6,19-oxidoprogesterone derivative of  claim 14  and a pharmaceutically acceptable carrier.  
     
     
         17 . A method of preparing the composition of  claim 16  for the treatment of at least one disorder associated with a glucocorticoid imbalance comprising incorporating and mixing the 21-hydroxy-6,19-oxidoprogesterone derivative into the carrier to form the composition.  
     
     
         18 . A method for treating a disease comprising a glucocorticoid imbalance comprising administering the 21-hydroxy-6,19-oxidoprogesterone derivative of  claim 14 , in an amount sufficient to treat the disease, to a patient in need thereof.  
     
     
         19 . The method of  claim 18 , wherein the glucocorticoid imbalance is an excess of glucocorticoids.  
     
     
         20 . The method of  claim 18 , wherein the disease is selected from the group consisting of Cushing's syndrome, iatrogenic hypercoticolism, and depression.