US2003144346A1PendingUtilityA1

Methods and compositions for regulation of 5-alpha reductase activity

Priority: Oct 31, 1997Filed: Nov 14, 2002Published: Jul 31, 2003
Est. expiryOct 31, 2017(expired)· nominal 20-yr term from priority
A61P 43/00A61P 35/00A61P 3/04A61P 17/00A61P 17/14A61P 13/08C07C 49/255C07D 311/62C07C 49/248A61K 31/35A61K 31/075A61K 31/12A61K 31/00A61K 31/44A61K 31/55
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Claims

Abstract

Compounds that inhibit 5α-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A process of inhibiting 5α-reductase activity comprising the step of exposing 5α-reductase to an effective inhibiting amount of a compound of any of Tables 1-7.  
     
     
         2 . A process of treating prostate cancer in a subject in need of such treatment comprising the step of administering to the subject an effective therapeutic amount of a compound of any of Tables 1-7.  
     
     
         3 . A process of treating breast cancer in a subject in need of such treatment comprising the step of administering to the subject an effective therapeutic amount of a compound of any of Tables 1-7.  
     
     
         4 . A process of treating baldness in a subject in need of such treatment comprising the step of administering to the subject an effective therapeutic amount of a compound of any of Tables 1-7.  
     
     
         5 . A process of treating a skin disorder in a subject in need of such treatment comprising the step of administering to the subject an effective therapeutic amount of a compound of any of Tables 1-7.  
     
     
         6 . A process of treating obesity in a subject in need of such treatment comprising the step of administering to the subject an effective therapeutic amount of a compound of any of Tables 1-7.  
     
     
         7 . A process of treating benign prostatic hyperplasia or prostatitis in a subject in need of such treatment comprising the step of administering to the subject an effective therapeutic amount of a compound of any of Tables 1-7.  
     
     
         8 . A compound of the formula:  
       
         
           
           
               
               
           
         
         where x is —NHCH 2 CH 2 — or —CH═CH—;  
         R 1 , R 2  and R 3  each may be —H, —OH or —OCH 3 , provided that only one of R 1 , R 2 , and R 3  may be —H;  
         R 4 , R 5  and R 6  each may be —H, —OH, —OCH 3  or —N(CH 3 ) 2 , provided that only one of R 4 , R 5  and R 6  may be —H; and  
         n is 0 or 1.  
       
     
     
         9 . A compound of the formula:  
       
         
           
           
               
               
           
         
         where R is a chain with 2 to 20 atoms from the group consisting of carbon, oxygen, sulfur, and nitrogen, without or with one to four double bonds and additional hydrogen.  
       
     
     
         10 . A compound of the formula:  
       
         
           
           
               
               
           
         
         where R is  
         
           
             
             
                 
                 
             
           
         
       
     
     
         11 . A method for the stabilization of compounds shown in Tables 1-7 comprising adding an effective ambient of an inorganic acid, an organic acid, or a natural product that contains these acids to maintain the acidity of the therapeutic preparations of these compounds at pH 3.0 to pH 6.8.

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