US2007249826A1PendingUtilityA1

Method for the preparation of 21-hydroxy-6,19-oxidoprogesterone (21oh-6op)

Assignee: APPLIED RESEARCH SYSTEMSPriority: Sep 18, 2000Filed: Apr 12, 2007Published: Oct 25, 2007
Est. expirySep 18, 2020(expired)· nominal 20-yr term from priority
C07J 71/00C07J 71/0005
56
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Claims

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 .

Claims

exact text as granted — not AI-modified
1 - 13 . (canceled)  
     
     
         14 . A 21-hydroxy-6,19-oxidoprogesterone ester of Formula (1):  
       
         
           
           
               
               
           
         
         wherein R is selected from 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 ester of  claim 14 , wherein R is —C(O)—CH 2 CH 3 .  
     
     
         16 . The 21-hydroxy-6,19-oxidoprogesterone ester of  claim 14 , wherein R is —C(O)—(CH 2 ) 2 —COOH.  
     
     
         17 . The 21-hydroxy-6,19-oxidoprogesterone ester of  claim 14 , wherein R is —C(O)—(CH 2 ) 7 —CH═CH—(CH 2 ) 7 —COOH.  
     
     
         18 . The 21-hydroxy-6,19-oxidoprogesterone ester of  claim 14 , wherein R is —C(O)—PO 3 Na 2 .  
     
     
         19 . A composition comprising the 21-hydroxy-6,19-oxidoprogesterone ester of  claim 14  and a pharmaceutically acceptable carrier.  
     
     
         20 . A method of preparing the composition of  claim 19 , comprising mixing the 21-hydroxy-6,19-oxidoprogesterone ester and the carrier to form the composition.  
     
     
         21 . At method of treating a disease resulting from an excess of glucocorticoid in a patient in need thereof, comprising 
 administering the 21-hydroxy-6,19-oxidoprogesterone ester of  claim 14  to the patient in an amount sufficient to treat the disease.    
     
     
         22 . The method of  claim 21 , wherein the disease is selected from the group consisting of Cushing's syndrome, iatrogenic hypercoticolism, depression, and a combination thereof.  
     
     
         23 . The method of  claim 22 , wherein the disease is Cushing's syndrome.  
     
     
         24 . The method of  claim 22 , wherein the disease is depression.  
     
     
         25 . The method of  claim 22 , wherein the disease is iatrogenic hypercoticolism.  
     
     
         26 . A method of treating a clinical manifestation of Cushing's syndrome selected from the group consisting of hypertension, renal calculi, osteoporosis, glucose intolerance, muscle wasting, reduced resistance to infection, psychiatric disturbances, and combinations thereof, in a patient in need thereof, comprising administering the 21-hydroxy-6,19-oxidoprogesterone ester of  claim 14  to the patient in an amount sufficient to treat the clinical disease manifestation.  
     
     
         27 . The method of  claim 26 , wherein the clinical disease manifestation is hypertension.  
     
     
         28 . The method of  claim 26 , wherein the clinical disease manifestation is renal calculi.  
     
     
         29 . The method of  claim 26 , wherein the clinical disease manifestation is osteoporosis.  
     
     
         30 . The method of  claim 26 , wherein the clinical disease manifestation is glucose intolerance.  
     
     
         31 . The method of  claim 26 , wherein the clinical disease manifestation is muscle wasting.  
     
     
         32 . The method of  claim 26 , wherein the clinical disease manifestation is reduced resistance to infection.

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