Radiolabeled darapladib and analogs thereof and their use as imaging compounds

Abstract

The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of choice concerning inflammation and atherosclerosis progression. Thus, the present invention relates to radiolabeled Darapladib and analogs thereof and their use as imaging compounds.

1 . A method for detecting atherosclerotic plaques in a patient, said method comprising the steps of:
 administering to said patient a detectable amount of a compound of formula
                     
 wherein X is 
 18 F,  124 I  131 I,  123 I,  125 I or  211 At,   subjecting said patient to Positron Emission Tomography (PET) or Single-Photon Emission Computed Tomography (SPECT), and   collecting the PET or SPECT signal.   
     
     
         2 . The method according to  claim 1 , wherein the compound is administered to said patient by intra-venous, subcutaneous or oral route. 
     
     
         3 . The method according to  claim 1 , wherein blood vessels of the patient are subjected to PET or SPECT. 
     
     
         4 . The method according to  claim 3 , wherein blood vessels of the heart, brain, liver, pancreas, spleen, kidney, bladder, intestine or lung of the patient are subjected to PET or SPECT. 
     
     
         5 . The method according to  claim 3 , wherein carotid, coronary, femoral or cerebral arteries of the patient are subjected to PET or SPECT. 
     
     
         6 . The method according to  claim 1 , wherein bones, muscles, brain, aorta, stomach and thyroid of the patient are subjected to PET or SPECT. 
     
     
         7 . The method according to  claim 1 , wherein the atherosclerotic plaques are vulnerable atherosclerotic plaques. 
     
     
         8 . The method according to  claim 1 , wherein X is  18 F.