Use of ERbeta-selective ligands for regulating fertility and compounds useful therefor

Abstract

The present invention discloses the use of ERβ-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ERβ-agonists are used for treatment of infertility and ERβ-antagonists for contraception.

1 . A method for regulating fertility with or without an additional follicular sex steroid comprising administering a therapeutically effective amount of a ERβ-selective ligand to a patient in need thereof, wherein said ligand is not a 17-Chloro-D homosteroid of formula I  
       
         
           
           
               
               
           
         
       
       in which 
 R 1  is a hydrogen atom or a C 1-6  alkanoyl radical or a benzoyl radical,  
 R 2  is a C 1-6  alkyl group,  
 R 3  is a hydrogen atom, a C 1-6  alkyl radical, a C 1-6  alkanoyl radical or a benzoylyl radical, and  
 R4 is a hydrogen atom, a C 1-6  alkyl radical, a C n F 2n+1  group, in which n=1, 2 or 3, or a C≡CR 5  group, in which R 5  is a hydrogen atom, a C 1-6  alkyl radical or an unsubstituted or substituted phenyl radical.  
 
     
     
         2 . The method according to claim 1 , wherein a therapeutically effective amount of a ERβ-selective agonist is administered for the treatment of female infertility.  
     
     
         3 . The method according to  claim 2  to in connection with in vitro fertilization.  
     
     
         4 . The method according to  claim 2 , wherein said female infertility is ovarian infertility.  
     
     
         5 . A method for treating ovarian failure associated with aging comprising administering a therapeutically effective amount of a ERβ-selective ligand to a patient in need thereof, wherein said ligand is not a 17-Chloro-D homosteroid of formula I  
       
         
           
           
               
               
           
         
       
       in which 
 R 1  is a hydrogen atom or a C 1-6  alkanoyl radical or a benzoyl radical,  
 R 2  is a C 1-6  alkyl group,  
 R3 is a hydrogen atom, a C 1-6  alkyl radical, a C 1-6  alkanoyl radical or a benzoylyl radical, and  
 R4 is a hydrogen atom, a C 1-6  alkyl radical, a C n F 2n+1  group, in which n=1, 2 or 3, or a C≡CR 5  group, in which R 2  is a hydrogen atom, a C 1-6  alkyl radical or an unsubstituted or substituted phenyl radical.  
 
     
     
         6 . The method according to  claim 1 , wherein a therapeutically effective amount of a ERβ-selective antagonist is administered for ovarian contraception.  
     
     
         7 . The method according to  claim 6 , wherein said method inhibits folliculogenesis.  
     
     
         8 . The method according to  claim 6 , wherein said method inhibits ovulation.  
     
     
         9 . The method according to  claim 6 , wherein said method inhibits preimplantational development of ovulated oocytes.  
     
     
         10 . A method for regulating fertility without additional use of a follicular sex steroid comprising administering a pharmaceutical composition comprising, a ERβ-selective ligand according to  claim 1 .  
     
     
         11 . The method according to  claim 1 , wherein an additional sex steroid is administered which is progestin.  
     
     
         12 - 24 . (Cancelled)  
     
     
         25 . The method according to  claim 2 , in connection with an in vivo treatment.