Hammersmith Imanet Limited

Ge Healthcare Limited

General Electric Company

Imperial Innovations Limited

Ge Healthcare As

Imperial College

Matthias Eberhard Glaser

Erik Arstad

Alan Cuthbertson

Bard Indrevoll

Eric Ofori Aboagye

Ian M Newington

Magne Solbakken

Faisal Ahmed Syud

Julian Grigg

Sajinder Kaur Luthra

Duncan George Wynn

Rajiv Bhalla

Steven Michael Fairway

Ernest William Kovacs

Imtiaz Ahmed Khan

Peter Brian Iveson

Robert James Nairne

Robert James Domett Nairne

Anthony Wilson

Joseph Maduabuchi Arukwe

Hege Karlsen

Jane Brown

Omayra Liz Padilla De Jesus

Lisa Iddon

Duncan Hiscock

Quang-De Nguyen

Julius Leyton

James Nairne

Graham Smith

Sajinker Kaur Luthra

Gareth Edwin Smith

Sajinder Luthra

Quang-Dé Nguyen

The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to automated methods for the preparation and purification ofF-labelled tau imaging radiotracers. Also provided are interchangeable cassettes useful in the methods, and the use of automated synthesizers and cassettes in the methods.

Radiolabelling method

Novel radiotracer(s) for Positron Emission Tomography (PET) imaging are described. Novel radiotracer(s) for Positron Emission Tomography (PET) imaging of neuorendocrine tumors are described. Specifically the present invention describes novel [18F]Fluoroethyltriazol-[Tyr3]Octreotate analogs; in particular those that target somatostatin receptors found on the cell surface of gastroenteropancreatic neuorendocrine tumors. The present invention also describes intermediate(s), precursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Radiolabelled octreotate analogues as PET tracers

[F]-fluoralkyl tosylates are useful building block for the radiosynthesis of a number of small molecules. A method of purifying [F]-fluoroalkyl tosylates using an automated radiosynthesis apparatus (e.g. FASTlab module) is described. A method of purifying [F]-fluoroalky tosylates using a FASTlab module that includes a solid phase extraction (SPE) purification system is described.

[object Object]

Imaging agents comprising an isolated polypeptide conjugated with a radionucleide and a chelator; wherein the isolated polypeptide binds specifically to HER2, or a variant thereof; and methods for preparing and using these imaging agents.

HER2 binding peptides labeled with aluminium-[18] fluoride complexed by NOTA

Isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising the derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing the derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity are disclosed.

Isatin derivatives for use as in vivo imaging agents

The present invention relates toF radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety ofF-labelled positron emission tomography (PET) tracers.

Radiofluorination

The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods of making such radiodiagnostic and radiotherapeutic agents and the compounds used in such methods. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Radiolabelling methods

The present invention provides a process for [F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particularF-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [F]-labelled prosthetic groups. [F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.

Radiofluorinated compounds and their preparation

The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-C&#x2261;N&#x2014;O&#x2003;&#x2003;(II) or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I): with a compound of formula (II) or, a compound of formula (III): with a compound of formula (IV): in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy. 

The invention relates to conjugates of formula (V) or (VI): wherein X is &#x2014;CO&#x2014;NH&#x2014;, &#x2014;NH&#x2014;, &#x2014;O&#x2014;, &#x2014;NHCONH&#x2014;, or &#x2014;NHCSNH&#x2014;; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes. 

Methods of radiofluorination of biologically active vectors

The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.

Provided herein are methods for introducing fluorine atom onto a biomolecule comprising: (i) providing a linker comprising a thiol-reactive terminus and an azido/alkyne-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a biomolecule comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the azido/alkyne-reactive terminus of the linker with a fluorine-substituted azide or alkyne respectively. Also provided are compositions and method of synthesis of bifunctional linkers and bioconjugates as well as radio-diagnostic agents comprising fluorine-labeled biomolecules.

Selective radiolabeling of biomolecules

The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N(II) or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy. 

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London, United Kingdom

Matthias Eberhard Glaser