US2013150337A1PendingUtilityA1

Substituted 16,17-annellated steroid compounds for use in womens health

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Individually held — no corporate assignee on recordPriority: Jun 10, 2009Filed: Feb 5, 2013Published: Jun 13, 2013
Est. expiryJun 10, 2029(~2.9 yrs left)· nominal 20-yr term from priority
Inventors:Fredericus Antonius DijcksHubert Jan Jozef LoozenSamira AddoAntonius Gerardus Hendrikus Ederveen
A61P 15/00C07J 53/00A61P 15/18C07J 53/002
37
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Claims

Abstract

The present invention relates to substituted steroid compounds having the formula Wherein R 1 is H or halogen; R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R 3 is H or halogen; R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R 5 is methyl or ethyl; R 6 is H or methyl; R 7 is H or methyl; R 8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A compound having the formula 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is H or halogen; 
         R 2  is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; 
         R 3  is H or halogen; 
         R 4  is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; 
         R 5  is methyl or ethyl; 
         R 6  is H or methyl; 
         R 7  is H or methyl; 
         R 8  is H or acyl. 
       
     
     
         2 . The compound according to  claim 1 , wherein R 8  is H. 
     
     
         3 . The compound according to  claim 1 , wherein R 1  is H or F and R 3  is H or F. 
     
     
         4 . The compound according to  claim 1 , wherein R 6  is H or α-methyl. 
     
     
         5 . The compound according to  claim 1 , wherein R 5  is methyl. 
     
     
         6 . The compound according to  claim 1 , wherein R 4  is (1C-4C)alkyl. 
     
     
         7 . The compound according to  claim 6 , wherein R 4  is propyl. 
     
     
         8 . The compound according to  claim 5 , wherein R 6  is H and R 7  is H. 
     
     
         9 . The compound according to  claim 3 , wherein R 5  is methyl; R 6  is H and R 7  is H. 
     
     
         10 . The compound according to  claim 9 , wherein R 4  is propyl. 
     
     
         11 . The compound according to  claim 1 , wherein R 2  is H or (1C-4C) acyl. 
     
     
         12 . The compound according to  claim 11 , wherein R 1  is H; R 3  is H; R 4  is propyl; R 5  is methyl; R 6  is H and R 7  is H. 
     
     
         13 . A compound having the formula 
       
         
           
           
               
               
           
         
       
     
     
         14 . A pharmaceutical composition comprising a compound according to any one of  claims 1 - 12  and one or more pharmaceutical excipients. 
     
     
         15 . A pharmaceutical composition comprising the compound according to  claim 13  and one or more pharmaceutical excipients. 
     
     
         16 . A method of treatment of a human or an animal in need of treatment with the compound according to any one of  claims 1 - 12  by administration of the compound in a pharmaceutical formulation and in a therapeutically effective dose. 
     
     
         17 . The method according to  claim 16 , whereby the human is a woman and the need for treatment is for therapy of endometriosis. 
     
     
         18 . A method of treatment for endometriosis comprising administering a compound having the formula 
       
         
           
           
               
               
           
         
       
       in a pharmaceutical formulation at a therapeutically effective dose. 
     
     
         19 . A method of contraception comprising administration to a woman of a compound according to  claim 1 .

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