Ge Healthcare Limited

Amersham Plc

Amersham International Plc

Nycomed Amersham Plc

Marivi Mendizabal

Anthony Eamon Storey

Ian Andrew Wilson

Peter Knox

Alan Michael Forster

Susan Champion

Benedicte Guilbert

Alex Gibson

Alan Cuthbertson

Timothy Charles Richardson

Henry Raphael Wolfe

Duncan George Wynn

Alexander Mark Gibson

Joseph Maduabuchi Arukwe

Gary Robert Bower

Philip Duncanson

Richard Pither

Edward R Bacon

Vinay Chandrakant Desai

Sudhakar Kasina

Stefan Wagner

Michael Schafers

Mark Dixon

Hans-Jörg Breyholz

Kirsty Heywood

Shirley Elizabeth Pullan

Vaughan Griffiths

Sally-Ann Ricketts

Karen Jane Barnes

Julie Davis

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.

Diagnostic imaging agents with MMP inhibitory activity

A peptide-chelate conjugate with affinity for the ST receptor is disclosed, wherein the chelate is tetradentate. The peptide-chelate conjugate of the invention may be labelled with a radiometal to provide a metal complex. A radiopharmaceutical composition comprising the metal complex is provided. which is suitable for the diagnostic imaging of colorectal cancer. Also provided for in the invention is a kit for the preparation of the radiopharmaceutical preparation.

Peptide-chelate conjugates

Synthetic analogues of lysine and glutamine are provided which function as substrates for the fibrin-stabilising enzyme Factor XIIIa even when labelled with a detectable moiety. The use of suitable protecting groups provides compounds which possess reduced susceptibility to in vivo metabolism especially by peptidases, and are hence useful agents for the diagnosis of thrombosis, embolism, atherosclerosis, inflammation or cancer.

Labelled glutamine and lysine analogues

A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula (Y)-A-NHR)can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.

Labelled factor XIIIa substrates

A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula &mdash;(Y) &mdash;A&mdash;NHR, can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.

The present invention relates to P or P-labelled bisphosphonates as radiotherapeutic radiopharmaceuticals. The P- or P-labelled bisphosphonates, which are chemically identical to the unlabelled agent, are expected to target the lesion site in an identical manner, but also deliver a significant radiocytotoxic effect to the surrounding cells. This should result, given the favorable energetics of the &bgr; particle emission from the P nuclide, in a loss of proliferative capacity of cells associated with the tumor lesion. The relative stability and in vivo localisation of bisphosphonates makes them good candidates as P/ P delivery vehicles.

Radiolabelled bisphosphonates and method

A human leucocyte elastase (HLE) inhibitor labelled with a detector moiety where the inhibitor is synthetic and has a molecular weight of less than 2000, is useful for the diagnostic imaging of sites of inflammation of infection in vivo, for labelling leucocytes in vitro, or for radiotherapy of rthritis. The HLE inhibitor is preferably a &bgr;-lactam or an azetidinone.

Labelled elastase inhibitors

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Amersham, United Kingdom

Marivi Mendizabal