Ge Healthcare Limited

Ge Healthcare As

Amersham Plc

Philip Duncanson

Harry John Wadsworth

Anthony Eamon Storey

Nigel Anthony Powell

Alan Cuthbertson

Magne Solbakken

Alexander Mark Gibson

Marivi Mendizabal

Dagfinn Lovhaug

Richard Pither

Shirley Elizabeth Pullan

Vaughan Griffiths

The present invention provides tetra-amine chelator conjugates with biological targeting moieties, linked via a linker group and technetium complexes thereof as radiopharmaceuticals. The linker group is such that the chelator is mono-functionalized at the bridgehead position and provides both flexibility and a lack or aryl groups, to minimize lipophilicity and steric hulk. Protected versions of the chelators are provided which permit conjugation with a wide range of targeting molecules without interfering reactions with the amine nitrogens of the tetra-amine chelator. Syntheses of the functionalised chelators are described, together with bifunctional chelate precursors. Radiopharmaceutical compositions comprising the technetium metal complexes of the invention are described, together with non-radioactive kits for the preparation of such radiopharmaceuticals.

N4 chelator conjugates

A contrast agent of formula I: V-L-R (I) where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linear or branched amino acid-comprising biomodifier or linker moiety, and R is a reporter moiety detectable in in vivo imaging of a human or animal body.

Contrast agent

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

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London, United Kingdom

Philip Duncanson