Novel Compounds Having Selective Inhibiting Effect at GSK3

Abstract

The present invention relates to new compounds of formula I wherein Z is N; Y is CONR 5 , NR 5 CO, SO 2 NR 5 , NR 5 SO 2 , CH 2 NR 5 , NR 5 , NR 5 CONR 5 , CH 2 CO, CO, O or CH 2 O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.

1 - 34 . (canceled) 
   
   
       35 . A compound having the formula I 
     
       
         
         
             
             
         
       
       wherein: 
       Z is N; 
       Y is CONR 5 ; 
       X is N; 
       P is phenyl; 
       Q is C 1-6 alkyl; 
       R is C 0-6 alkyl(SO 2 )NR 1 R 2 ; 
       R 1  and R 2  may together form a substituted 5 or 6 membered heterocyclic ring containing one or more heteroatoms independently selected from N, O or S, which heterocyclic ring may be optionally substituted by A; 
       R 4  is C 3-6 cycloalkyl; which may be optionally be substituted by one or more A; 
       R 5  is hydrogen; 
       R 6  and R 7  are independently selected from hydrogen, C 1-6 alkyl; 
       A is halo, nitro, OR 6 , C 1-6 alkyl, C 0-6 alkylNR 6 R 7 ; 
       m is 0; 
       n is 1; 
       as a free base or a pharmaceutically acceptable salt, solvate or solvate of a salt thereof. 
     
   
   
       36 . A compound according to  claim 35 , wherein R 1  and R 2  in C 0-6 alkyl(SO 2 )NR 1 R 2  is a piperazinyl moiety, as a free base or a pharmaceutically acceptable salt, solvate or solvate of a salt thereof. 
   
   
       37 . A compound according to any one of  claim 35  or  36 , wherein A is C 1-6 alkyl, as a free base or a pharmaceutically acceptable salt, solvate or solvate of a salt thereof. 
   
   
       38 . A pharmaceutical formulation comprising as active ingredient a therapeutically effective amount of the compound according to  claim 35  in association with a pharmaceutically acceptable carrier or diluent. 
   
   
       39 . A pharmaceutical formulation comprising as active ingredient a therapeutically effective amount of the compound according to  claim 36  in association with a pharmaceutically acceptable carrier or diluent. 
   
   
       40 . A pharmaceutical formulation comprising as active ingredient a therapeutically effective amount of the compound according to  claim 37  in association with a pharmaceutically acceptable carrier or diluent.