Agent for lowering prolactin

Abstract

The present invention relates to a prolactin lowering drug containing at least one bicyclic diterpene of the labdane type. wherein R1=H, C 1 to C 3 alkyl or C 1 to C 3 acyl.

1 . A prolactin lowering drug comprising at least one bicyclic diterpene compound of the labdane type in accordance with at least one of general formulae (I) or (II):  
       
         
           
           
               
               
           
         
         wherein R 1 =H, C 1  to C 3  alkyl or C 1  to C 3  acyl;  
         wherein the rings a and/or b in the case of general formulae (I) or (II) are optionally substituted in position 1, 2, 3, 6, 7, 8 or 9 with at least one OX radical, with X=H, C 1  to C 3  alkyl or C 1  to C 3  acyl;  
         wherein optionally at least one carbon atom in position 17, 18, 19 and 20 is substituted with an ox radical, with X=H, C 1  to C 3  alkyl or C 1  to C 3  acyl;  
         wherein optionally at least one CH 3  group in position 17, 18, 19 and 20 is replaced by one COOH group;  
         wherein optionally at least one of ring positions 1, 2, 3, 6, or 7 is a keto group; and  
         wherein optionally at least one double bond is present in ring positions 1, 2, 3, 6, 7, 8, 8(17) of formula (I); and  
         wherein optionally at least one double bond is present in ring positions 1, 2, 3, 6, 7, 8, 8(17) of formula (II);  
         with the exception of the following compounds:  
         rotundifuran, sclareol, larixol acetate, vitexilactone,7α-hydroxy-manool, ent-15,16-epoxy-9αH-labda-13(16)14-diene-3β, 8α-diol, solidagenon, and 15, 16-epoxy-8(17),14,16-labdatrien-19-oic acid methyl ester, and 6β,7β-diacetoxy-13-hydroxy-labda-8,14-dien-diacetoxy-13-hydroxy-labda-8,14-dien.  
       
     
     
         2 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         3 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         4 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         5 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         6 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         7 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         8 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         9 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         10 . A prolactin lowering drug according to  claim 1 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         11 . A prolactin lowering drug according to  claim 10 , comprising a compound having the following formula:  
       
         
           
           
               
               
           
         
       
     
     
         12 . A method of treating premenstrual syndrome, mastodynia, or a disorder of the menstrual cycle to a woman in need of treatment, comprising: 
 administering a pharmaceutically acceptable formulation comprising the prolactin lowering drug of any of claims  1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 , or  11  to the woman in need of treatment.    
     
     
         13 . The method of  claim 12 , wherein the disorder of the menstrual cycle is oligomenorrhea or amenorrhea.  
     
     
         14 . A method of lowering prolactin release by a mammalian pituitary cell, comprising: 
 adding the prolactin lowering drug of any of claims  1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 , or  11  to the cell in an amount sufficient to lower the release of prolactin by the cell, compared to a control not receiving the prolactin lowering drug or the compound    
     
     
         15 . A method of treating premenstrual syndrome, mastodynia, or a disorder of the menstrual cycle to a woman in need of treatment, comprising: 
 administering to the woman in need of treatment a pharmaceutically acceptable formulation of a prolactin lowering drug comprising a bicyclic diterpene compound of the labdane type selected from the group consisting of rotundifuran, sclareol, and solidagenon.    
     
     
         16 . The method of  claim 15 , wherein the disorder of the menstrual cycle is oligomenorrhea or amenorrhea.  
     
     
         17 . A method of lowering prolactin release by a mammalian pituitary cell, comprising: 
 adding to the cell a prolactin lowering drug comprising a bicyclic diterpene compound of the labdane type selected from the group consisting of rotundifuran, sclareol, and solidagenon, in an amount sufficient to lower the release of prolactin by the cell, compared to a control not receiving the prolactin lowering drug.