Abstract: 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.

Abstract: 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.

Abstract: The invention relates to novel 18F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. The 18F-labelled compounds of the invention comprise a [18F]fluoroalkenyl group.

Abstract: The invention relates to methods and apparatus for drying [18F]fluoride which comprises (i) passing a [18F]fluoride solution comprising water, a solvent, [18F]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.

Abstract: 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.

Abstract: A method for coating the internal surfaces of a reaction vessel having a small internal diameter comprises the steps of (i) introducing into the reaction vessel a solution of one or more monomers in a suitable solvent; (ii) introducing a flow of an inert gas through the reaction vessel; and (iii) initiating polymerization of the monomer solution.

Abstract: The present invention relates to the field of [18F] radiofluorination chemistry for the preparation of Positron Emission Tomography (PET) radioligands and [18F] radiofluorinating reagents. The invention further provides kits for preparation of the same.

Abstract: 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.

Abstract: The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4 alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C]C1-4 alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C]C1-4 alkyl or [18F]—C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.

Abstract: 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.

Abstract: 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.

Abstract: The present invention relates to 18F 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 of 18F-labelled positron emission tomography (PET) tracers.

Abstract: 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-N3 (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.

Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.

Abstract: The present invention provides a method for determination of neural activity in a sample. The method of the invention is useful for the determination of neural activity in both in vivo and in vitro samples and is particularly useful in providing diagnostic information in subjects suspected to have a neurological condition that leads to disturbed neurological signalling. Also provided by the invention are compounds suitable for use in the method of the invention, and a pharmaceutical composition useful for carrying out the method of the invention.

Abstract: The invention relates to a compound of formula (I) having use for in vivo imaging of the NR2B subtype of the NMDA receptor.

Abstract: The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C] C1-4alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C] C1-4alkyl or [18F]—C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.

Abstract: The invention relates to methods and apparatus for labelling a biologically active vector such as a peptide with reporter moiety such as a radionuclide. The methods comprise reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N3 (II) or, a compound of formula (III) with a compound of formula (IV) wherein: L1, L2, L3, and L4 are each Linker groups; R* is a reporter moiety; in a narrow bore copper vessel. Microfluidic devices for performing the methods of the invention are also claimed.

Abstract: 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.

Abstract: The present invention relates to methods of synthesising radiolabelled compounds, to the precursors useful in such methods and to the radiolabelled compounds obtainable by such methods. More particularly, the present invention relate to methods, precursors and radiolabelled compounds useful in Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) especially for imaging neuroreceptors with radiolabelled agonists.