Imaging agents

Abstract

Provided herein is technology relating to imaging agents and particularly, but not exclusively, to methods of manufacturing fluorine-18-labeled phenethylguanidines and uses thereof.

1 .- 205 . (canceled) 
     
     
         206 . A composition comprising an  18 F-labeled arylalkylguanidine having a structure according to 
       
         
           
           
               
               
           
         
       
       or a salt, a free base, or a combination thereof, wherein:
 a) R 1 , R 2 , R 3 , R 4 , and R 5  are independently selected from the group consisting of  18 F-labeled,  19 F, hydrogen, halogen, hydroxyl, guanyl, alkoxy, haloalkoxy,  18 F-labeled alkoxy, alkyl, haloalkyl,  18 F-labeled alkyl, amine, and an amine comprising a protecting group; 
 b) n is equal to 0 or 2; 
 c) Z is independently selected from the group comprising hydrogen, hydroxyl, alkoxy, haloalkoxy,  18 F-labeled alkoxy, halogen, amino, alkyl, haloalkyl, and  18 F-labeled alkyl; and 
 d) R 6 , R 7 , R 8 , and R 9  are independently selected from the group consisting of hydrogen, carbamate, cyclic carbamate, amide, cyclic amide, and a nitrogen-protecting group. 
 
     
     
         207 . The composition of  claim 206  wherein R 6  is a hydrogen, R 7  is a hydrogen, R 8  is a hydrogen, and/or R 9  is a hydrogen. 
     
     
         208 . The composition of  claim 206  further comprising a biologically compatible carrier. 
     
     
         209 . The composition of  claim 206  further comprising a physiological buffered saline solution or a physiological buffered sodium acetate carrier. 
     
     
         210 . The composition of  claim 206  comprising 0.1 to 100 mCi of labeled radiotracing agent. 
     
     
         211 . The composition of  claim 206  comprising 50 to 500 mCi of labeled radiotracing agent. 
     
     
         212 . A composition comprising an  18 F-labeled aryl-Y-alkylguanidine having a structure according to 
       
         
           
           
               
               
           
         
       
       or a salt, a free base, or a combination thereof, wherein:
 a) R 1 , R 2 , R 3 , R 4 , and R 5  are independently selected from the group consisting of  18 F-labeled,  19 F, hydrogen, halogen, hydroxyl, guanyl, alkoxy, haloalkoxy,  18 F-labeled alkoxy, alkyl, haloalkyl,  18 F-labeled alkyl, amine, and an amine comprising a protecting group; 
 b) Y is independently selected from the group comprising O, S or NH. 
 c) R 6 , R 7 , R 8 , and R 9  are independently selected from the group consisting of hydrogen, carbamate, cyclic carbamate, amide, cyclic amide, and a nitrogen-protecting group; and 
 d) n is equal to 1, 2 or 3. 
 
     
     
         213 . The composition of  claim 212  wherein R 6  is a hydrogen, R 7  is a hydrogen, R 8  is a hydrogen, and/or R 9  is a hydrogen. 
     
     
         214 . The composition of  claim 212  further comprising a biologically compatible carrier. 
     
     
         215 . The composition of  claim 212  further comprising a physiological buffered saline solution or a physiological buffered sodium acetate carrier. 
     
     
         216 . The composition of  claim 212  comprising 0.1 to 100 mCi of labeled radiotracing agent. 
     
     
         217 . The composition of  claim 212  comprising 50 to 500 mCi of labeled radiotracing agent. 
     
     
         218 . A composition comprising an  18 F-labeled heteroarylalkylguanidine having a structure according to: 
       
         
           
           
               
               
           
         
       
       or a salt, a free base, or a combination thereof, wherein:
 e) R 1 , R 2 , R 3 , and R 4  are independently selected from the group consisting of  18 F-labeled,  19 F, hydrogen, halogen, hydroxyl, guanyl, alkoxy, haloalkoxy,  18 F-labeled alkoxy, alkyl, haloalkyl,  18 F-labeled alkyl, amine, and an amine comprising a protecting group; 
 f) L, M, N and Q are independently selected from the group comprising CH 2 , CH, O, N, NH, S, CO, alkyl, haloalkyl, alkoxy, haloalkoxy,  18 F-labeled alkyl, and  18 F-alkoxy; 
 g) R 5 , R 6 , R 7 , and R 8  are independently selected from the group consisting of hydrogen, carbamate, cyclic carbamate, amide, cyclic amide, and a nitrogen-protecting group; and 
 h) n is equal to 0, 1, 2 or 3. 
 
     
     
         219 . The composition of  claim 218  wherein R 5  is a hydrogen, R 6  is a hydrogen, R 7  is a hydrogen, and/or R 8  is a hydrogen. 
     
     
         220 . The composition of  claim 218  further comprising a biologically compatible carrier. 
     
     
         221 . The composition of  claim 218  further comprising a physiological buffered saline solution or a physiological buffered sodium acetate carrier. 
     
     
         222 . The composition of  claim 218  comprising 0.1 to 100 mCi of labeled radiotracing agent. 
     
     
         223 . The composition of  claim 218  comprising 50 to 500 mCi of labeled radiotracing agent.