[EN] IMPROVED IMAGING AGENTS COMPRISING BARBITURIC ACID DERIVATIVES<br/>[FR] AGENTS D'IMAGERIE AMELIORES CONTENANT DES DERIVES DE L'ACIDE BARBITURIQUE
申请人:AMERSHAM PLC
公开号:WO2004032936A1
公开(公告)日:2004-04-22
The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic barbituric acid derivative labelled at the 5-position with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides pharmaceutical and radiopharmaceutical compositions comprising the imaging agents, together with kits of the preparation of the radiopharmaceuticals. Also described are chelator conjugates of the barbituric acid derivative, which are suitable for the preparation of imaging agents comprising a radioactive or paramagnetic metal ion. The imaging agents are useful for the diagnostic imaging in vivo of various disease states, including atherosclerosis.
The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic barbituric acid derivative labelled at the 5-position with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides pharmaceutical and radiopharmaceutical compositions comprising the imaging agents, together with kits of the preparation of the radiopharmaceuticals. Also described are chelator conjugates of the barbituric acid derivative, which are suitable for the preparation of imaging agents comprising a radioactive or paramagnetic metal ion. The imaging agents are useful for the diagnostic imaging in vivo of various disease states, including atherosclerosis.
The present invention relates to methods and reagents for [
18
F]-fluorination, particularly of peptides. The resultant
18
F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET). Thus, a compound of formula
18
F-(Linker)-SH, such as a compound of formula (IV), (V), or (VI):
18
F—(CH
2
CH
2
O)
n
—(CH
2
)
m
—SH (IV)
18
F—(CH
2
)
p
—SH (V)
may be reacted with an activated peptide as a means for
18
F-labelling.
The invention relates to compounds of formula (I): and their use as targeting vectors that bind to receptors associated with angiogenesis. Such compounds may thus be used for diagnosis or therapy of, for example, malignant diseases, heart diseases, endometriosis, inflammation-related diseases, rheumatoid arthritis and Kaposi's sarcoma.
The present invention discloses that imaging agents which comprise a specific type of matrix metalloproteinase inhibitors (MMPi's) of the sulphonamide hydroxamate class labelled with an imaging moiety, are useful diagnostic imaging agents for in vivo imaging and diagnosis of the mammalian body.