The present invention relates to the field of diagnostic imaging. Specifically, the invention relates to the diagnostic imaging of diseases where specific matrix metalloproteinases are known to be involved. One embodiment of the invention is a compound having matrix metalloproteinase inhibitory acti
The present invention relates to the field of diagnostic imaging. Specifically, the invention relates to the diagnostic imaging of diseases where specific matrix metalloproteinases are known to be involved. One embodiment of the invention is a compound having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the diagnostic imaging agent of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention. The pharmaceutical composition of the invention may be used in the diagnosis of diseases where specific matrix metalloproteinases are known to be involved.
대표청구항▼
1. A diagnostic imaging agent: wherein: R1 is selected from hydrogen, hydroxy, C1-6 alkyl, C6-14 aryl, C7-20 arylalkyl, or together with R5 and the carbon to which it is attached forms either a C6-8 cycloalkyl ring or a C4-6 heterocyclic ring, or together with R4 forms a C4-6 heterocyclic ring cont
1. A diagnostic imaging agent: wherein: R1 is selected from hydrogen, hydroxy, C1-6 alkyl, C6-14 aryl, C7-20 arylalkyl, or together with R5 and the carbon to which it is attached forms either a C6-8 cycloalkyl ring or a C4-6 heterocyclic ring, or together with R4 forms a C4-6 heterocyclic ring containing 5-7 atoms and 1 or 2 heteroatoms chosen from N or O;R2 is a γ-emitting isotope of iodine attached via a direct covalent bond to the 3- or 4-position of the aromatic ring;R3 is hydrogen;R4 is C6-14 aryl, C4-6 heteroaryl, C7-20 arylalkyl, C7-20 carbamoylaryl or arylcarbamoylaryl; and,R5 is selected from hydrogen or C1-6 alkyl. 2. The diagnostic imaging agent of claim 1 wherein: R1 is selected from C1-6 alkyl, C6-14 aryl, or C7-20 arylalkyl, or together with R5 forms a C4-6 heterocyclic ring together with the carbon to which it is attached;R4 is pyridyl or (Ar1)y-(R′″)z(NH)-phenyl wherein Ar1 is phenylene, R′″ is CH2 or C═O, y=0 or 1 and z=0 or 1; and,R5 is hydrogen. 3. The diagnostic imaging agent of claim 1 wherein: R1 is methyl, isobutyl, isopropyl, benzyl or hydroxybenzyl;R4 is pyridyl or (Ar1)y-(R′″)z(NH)-phenyl wherein Ar1 is 1,4-phenylene, R′″ is CH2 or C═O, y=0 or 1 and z=0 or 1; andR5 is hydrogen. 4. The diagnostic imaging agent of claim 1 wherein R5 is hydrogen and the diagnostic imaging agent is of Formula Ia: 5. The diagnostic imaging agent of claim 1 wherein R2 is positioned para to the sulfonamide. 6. The diagnostic imaging agent of claim 1, wherein said γ-emitting isotope of iodine is 123I. 7. A pharmaceutical composition comprising the diagnostic imaging agent of claim 1 together with a biocompatible carrier, in a form suitable for mammalian administration. 8. A kit for the preparation of a pharmaceutical composition comprising a precursor useful in the preparation of the diagnostic imaging agent of claim 1, wherein said precursor is a compound of Formula I wherein: R1 is selected from hydrogen, hydroxy, C1-6 alkyl, C6-14 aryl, C7-20 arylalkyl, or together with R5 and the carbon to which it is attached forms either a C6-8 cycloalkyl ring or a C4-6 heterocyclic ring, or together with R4 forms a C4-6 heterocyclic ring containing 5-7 atoms and 1 or 2 heteroatoms chosen from N or O;R2 is hydroxy, tributyltin, or 127I;R3 is hydrogen;R4 is C6-14 aryl, C4-6 heteroaryl, C7-20 arylalkyl, C7-20 carbamoylaryl or arylcarbamoylaryl; and,R5 is selected from hydrogen or C1-6 alkyl.
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Olexa Stephanie A. (Hellertown PA) Knight Linda C. (Plainsboro NJ) Budzynski Andrei Z. (Glenside PA), Use of radiolabeled peptide derived from crosslinked fibrin to locate thrombi in vivo.
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