Treatment of central nervous system disorders with selective estrogen receptor modulators

Abstract

The present invention provides a method of treating depression, mood swings, or Alzheimer's disease in a patient in need of such treatment by administering a selective estrogen receptor modulating compound of the formula in which R 1 and R 2 are independently hydroxy and alkoxy of one to four carbon atoms; and R 3 and R 4 are independently methyl or ethyl, or R 3 and R 4 , taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methyl-pyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring.

We claim:  
     
         1 . The use of a compound having the structure  
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or pro-drug thereof,  
         wherein R 1  and R 2  are independently selected from the group consisting of hydroxy and alkoxy of one to four carbon atoms; and  
         R 3  and R 4  are independently selected from methyl or ethyl, or R 3  and R 4 , taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methylpyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring;  
         in the preparation of a medicament useful for treating a central nervous system disorder selected from depression, mood swings, and Alzheimer's disease in a patient.  
       
     
     
         2 . The use of  claim 1  wherein said medicament is useful for treating depression or mood swings.  
     
     
         3 . The use of  claim 1  wherein said medicament is useful for treating Alzheimer's disease.  
     
     
         4 . The use of  claim 1  wherein R 1  and R 2  are both hydroxy.  
     
     
         5 . The use of  claim 2  wherein R 1  and R 2  are both hydroxy.  
     
     
         6 . The use of  claim 3  wherein R 1  and R 2  are both hydroxy.  
     
     
         7 . The use of  claim 1  wherein R 1  is hydroxy and R 2  is alkoxy of one to four carbon atoms.  
     
     
         8 . The use of  claim 2  wherein R 1  is hydroxy and R 2  is alkoxy of one to four carbon atoms.  
     
     
         9 . The use of  claim 3  wherein R 1  is hydroxy and R 2  is alkoxy of one to four carbon atoms.  
     
     
         10 . The use of  claim 1  wherein R 3  and R 4  combine with the nitrogen atom to which they are attached to form a piperidino ring.  
     
     
         11 . The use of  claim 2  wherein R 3  and R 4  combine with the nitrogen atom to which they are attached to form a piperidino ring.  
     
     
         12 . The use of  claim 3  wherein R 3  and R 4  combine with the nitrogen atom to which they are attached to form a piperidino ring.  
     
     
         13 . The use of a compound having the structure  
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or pro-drug thereof,  
         wherein R 2  is hydroxy or methoxy; in the preparation of a medicament useful for treating depression or mood swings in a patient.  
       
     
     
         14 . The use of  claim 13  wherein said compound is 6-hydroxy-2-(4-methoxyphenyl)-3-[4-(2-piperidinoethoxy)phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof.  
     
     
         15 . The use of  claim 13  wherein said compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof.  
     
     
         16 . The use of a compound having the structure  
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or pro-drug thereof,  
         wherein R 2  is hydroxy or methoxy; in the preparation of a medicament useful for treating Alzheimer's disease in a patient.  
       
     
     
         17 . The use of  claim 16  wherein said compound is 6-hydroxy-2-(4-methoxyphenyl)-3-[4-(2-piperidinoethoxy)phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof.  
     
     
         18 . The method of  claim 16  wherein said compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof.  
     
     
         19 . The use of  claim 13  wherein said salt is the hydrochloride salt.  
     
     
         20 . The use of  claim 16  wherein said salt is the hydrochloride salt.