Pyridylacetylenes for use as radiotracers and imaging agents

Abstract

The present invention relates to novel pyridylacetylene derivatives, their preparation, their use as radiotracers/markers and compositions containing them.

1 . A compound having a structure that is embraced within the genus of formula I 
       
         
           
           
               
               
           
         
         wherein R is 11CH3, (3H)3C, (CH2)n123I, (CH2)n76Br or (CH2)n18F, n being 1,2, 3 or 4; 
       
       in free base or acid addition salt form, and which exhibits activity as an mGluR5 receptor antagonist. 
     
     
         2 . The compound of  claim 1 , wherein R is 11CH3. 
     
     
         3 . The compound of  claim 1 , wherein R is (3H)3C. 
     
     
         4 . The compound of  claim 1 , wherein R is (CH2)123I. 
     
     
         5 . The compound of  claim 1 , wherein R is (CH2)2123I. 
     
     
         6 . The compound of  claim 1 , wherein R is (CH2)3123I. 
     
     
         7 . The compound of  claim 1 , wherein R is (CH2)4123I. 
     
     
         8 . The compound of  claim 1 , wherein R is (CH2)76Br. 
     
     
         9 . The compound of  claim 1 , wherein R is (CH2)276Br. 
     
     
         10 . The compound of  claim 1 , wherein R is (CH2)376Br. 
     
     
         11 . The compound of  claim 1 , wherein R is (CH2)476Br. 
     
     
         12 . The compound of  claim 1 , wherein R is (CH2)18F. 
     
     
         13 . The compound of  claim 1 , wherein R is (CH2)218F. 
     
     
         14 . The compound of  claim 1 , wherein R is (CH2)318F. 
     
     
         15 . The compound of  claim 1 , wherein R is (CH2)418F.