Sulfonyl-3-heterocyclylindazole derivatives as 5-hydroxytryptamine-6 ligands

Abstract

The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.

1 - 9 . (canceled) 
     
     
         10 . A method for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor in a patient in need thereof which comprises providing to said patient a therapeutically effective amount of a compound of formula I 
       
         
           
           
               
               
           
         
       
       wherein
 R is H, halogen or an optionally substituted alkyl or haloalkyl group; 
 R 1  is an aryl or heteroaryl group each group optionally substituted or an optionally substituted 8- to 13-membered bicyclic or tricyclic ring system having a N atom at the bridgehead and optionally containing 1, 2 or 3 additional heteroatoms selected from N, O or S; 
 R 2  is H or an alkyl, cycloalkyl, aryl or heteroaryl group each group optionally substituted; 
 R 3  and R 4  are each independently H, or an optionally substituted alkyl group; 
 n is 0 or an integer of 1 or 2; and 
 R 5  is H or an alkyl, alkenyl, alkynyl or cycloalkyl, group each group optionally substituted; or 
 a stereoisomer thereof or a pharmaceutically acceptable salt thereof. 
 
     
     
         11 . The method according to  claim 10  wherein said disorder is a cognitive disorder, a developmental disorder or a neurodegenerative disorder. 
     
     
         12 . The method according to  claim 11  wherein said disorder is a cognitive disorder. 
     
     
         13 . The method according to  claim 11  wherein said disorder is selected from the group consisting of: a learning disorder; attention deficit disorder; Down's syndrome, Fragile X syndrome or autism. 
     
     
         14 . The method according to  claim 11  wherein said disorder is stroke or head trauma. 
     
     
         15 - 20 . (canceled) 
     
     
         21 . The method according to  claim 10  wherein said disorder is cognitive impairment in Alzheimer's patients. 
     
     
         22 . The method according to  claim 10  wherein n is 1. 
     
     
         23 . The method according to  claim 10  wherein R 1  is an optionally substituted phenyl or naphthyl group. 
     
     
         24 . The method according to  claim 10  wherein R, R 3  and R 4  are H. 
     
     
         25 . The method according to  claim 10  wherein R 2  is H or methyl and R 3  and R 4  are H. 
     
     
         26 . The method according to  claim 21  wherein n is 1. 
     
     
         27 . The method according to  claim 21  wherein R 1  is an optionally substituted phenyl or naphthyl group. 
     
     
         28 . The method according to  claim 21  wherein R, R 3  and R 4  are H. 
     
     
         29 . The method according to  claim 21  wherein R 2  is H or methyl and R 3  and R 4  are H.