Ge Healthcare Limited

Ge Healthcare as

G.d. Searle & Company

Hammersmith Imanet Limited

Alexander Mark Gibson

Matthias Eberhard Glaser

Sajinder Kaur Luthra

Frank Brady

Harry John Wadsworth

Colin Mill Archer

Torgrim Engell

Bard Indrevoll

Magne Solbakken

Alan Cuthbertson

Dennis O'Shea

Ian M Newington

William John Trigg

Bo Shan

Joanna Marie Passmore

Anthony Eamon Storey

Duncan George Wynn

Nigel Anthony Powell

Keith G McCullagh

Robert James Domett Nairne

Michelle E Avory

David K Donald

Amanda Ewan

Philip Duncanson

John Saunders

Oskar Axelsson

Dimitrios Mantzilas

Radha Achanath

Steven Michael Fairway

Clare Louise Jones

Denis Raymond Christophe Bouvet

Alexander Jackson

Dagfinn Lovhaug

Umamaheshwar P Mokkapati

Afsal Mohammed Kadavilpparampu Mohamed

Srinath Balaji

Michael Andrew Carroll

Bård Indrevoll

Lynda Jane Brown

Richard Charles Downie Brown

Amanda Eewan

Peter Anthony Devenish

David Arthur Widdowson

Emmanuelle Wilson

The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.

Imaging neuroinflammation

An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

Indole derivatives

The present invention provides a novel radiolabelled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.

Aryloxyanilide imaging agents

The present invention provides novel radioiodinated fatty acids. Also provided are methods of preparation of said radioiodinated fatty acids from non-radioactive precursors, as well as radiopharmaceutical compositions comprising such radioiodinated fatty acids. The invention also provides in vivo imaging methods using the radioiodinated fatty acids.

Radioiodinated fatty acids

The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are functionalised BTMs useful in the method, as well as methods of preparing such functionalised BTMs under mild conditions.

Radioiodination method

The present invention relates to improved chelator conjugates with biological targeting molecules, suitable for forming metal complexes with radiometals. The radiometal complexes, especially with the radiometalTc, are useful as radiopharmaceuticals.

Chelator conjugates

The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.

The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds of the formula R&#x2014;Y&#x2014;X&#x2014;Z&#x2014;R where each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties, Y and Z are urea and urethane groups and X is a alkylene group which may be further substituted. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Contrast agents

The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.

Active enantiomer

The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).

Paramagnetic chelates thereof and their use as contrast agents in magnetic resonance imaging (MRI)

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.

Peptide-based compounds

The present invention relates to chelating agents, in particular to chelating agents which are capable of forming complexes with paramagnetic metal ions such as iron (III) and gadolinium (III). The invention also relates to the complexes formed and their use as MRI contrast agents.

Chelating agents

The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing urea or urethane functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

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Amersham, United Kingdom

Harry John Wadsworth