Hammersmith Imanet Limited

Ge Healthcare Limited

General Electric Company

Ucl Business Plc

Imperial Innovations Limited

Ge Healthcare as

Erik Arstad

Matthias Eberhard Glaser

Sajinder Kaur Luthra

Frank Brady

Edward George Robins

Nicholas Toby Jeffery

Alan Cuthbertson

Bengt Langstrom

Magne Solbakken

Faisal Ahmed Syud

Farhad Karimi

Duncan George Wynn

Alexander Mark Gibson

Ernest William Kovacs

Eric Ofori Aboagye

Robert James Domett Nairne

Omayra Liz Padilla De Jesus

Gjermund Henriksen

Benedicte Guilbert

Alessandra Gaeta

Quang-De Nguyen

Ian Wilson

Bo Shan

Kerstin Sander

Julie Davis

Thibault Gendron

Graham Smith

Tony Storey

Quang-Dé Nguyen

Duncan Wynn

Bengt Langström

The present invention relates to sulfonium salts of formula (I): (I), their preparation, and utility as precursors for preparing functionalized organic compounds, wherein Rand Rare the same or different and each is independently selected from an optionally substituted aryl group, an optionally substituted alkynyl group, an optionally substituted alkenyl group, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted cycloalkenyl group, an optionally substituted aralkyl group, an optionally substituted arylalkenyl group, an optionally substituted heteroaryl group, an optionally substituted heterocyclyl group, an optionally substituted amine, an optionally substituted alkoxy group, an optionally substituted thioether group, an optionally substituted phosphine group, an optionally substituted boron species, an optionally substituted carbene, an organometallic moiety, and a halide, or Rand Rare joined together to form an optionally substituted sulfur-containing ring; W is a bond, an optionally substituted alkynylene group, an optionally substituted alkenylene group, and optionally substituted alkylene group, an optionally substituted heterocyclyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group; Ris a moiety comprising at least one basic group, provided that when Rdoes not contain any carbon atoms, W is not a bond; X is an anionic species; and n is an integer selected from 1 to 5. 

Compounds and their synthesis

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 new processes for preparation ofF-fluoroalkyl halides suitable for use in labelling of Positron Emission Tomography (PET) radiotracers. The process of preparation comprises the step of reacting aF-fluoroacylhalide with Wilkinson's catalyst.

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The present invention provides novel tetracyclic indole compounds of Formula (I) either as in vivo imaging agents or as therapeutic agents. A method for the preparation of the in vivo imaging agent compound is also provided by the invention, as well as a precursor for use in said method. Pharmaceutical compositions comprising the compounds of the invention are additionally provided. Where the pharmaceutical composition comprises a compound suitable for in vivo imaging, a kit is provided for the preparation of the pharmaceutical composition. In a further aspect, use of the compound for in vivo imaging or treatment of conditions associated with PBR is provided. 

Tetracyclic indole derivatives as in vivo imaging agents and having peripheralbenzodiazepine receptor affinity (PBR)

The invention relates to methods and apparatus for drying [F]fluoride which comprises (i) passing a [F]fluoride solution comprising water, a solvent, [F]fluoride, and a cationic counterion through a narrow bore vessel at elevated temperature such that the water and solvent are vaporised forming a vaporised component, and (ii) collecting the resulting vaporised component by condensing into a collection vessel.

Fluoride drying apparatus

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 methods and apparatus for purifying a radiolabelled compound. The method comprises (i) passing a crude reaction mixture comprising the desired radiolabelled compound and one or more contaminants in a solvent through a narrow bore vessel at elevated temperature such that the organic solvent and either the radiolabelled compound or one or more contaminants is vaporised forming a vaporised component, and (ii) collecting the resulting vaporised component by condensing into a collection vessel.

Method for the purification of radiolabelled compounds

The invention relates to novelF-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. TheF-labelled compounds of the invention comprise a [F]fluoroalkenyl group.

PET radiotracers

The invention relates to novel processes for the purification of radiolabelled tracers, using a solid-support bound scavenger group. The general concept being illustrated by the scheme:

Purification methods

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 methods and apparatus for drying [F]fluoride which comprises (i) passing a [F]fluoride solution comprising water, a solvent, [F]fluoride, and a cationic counterion through a narrow bore vessel at elevated temperature such that the water and solvent are vaporized forming a vaporized component, and (ii) collecting the resulting vaporized component by condensing into a collection vessel.

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London, United Kingdom

Erik Arstad