Radiofluorinated compounds and their preparation
AssigneeHammersmith Imanet Limited
InventorsERIK ARSTAD, MATTHIAS EBERHARD GLASER
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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.
Claims12
1-26. (canceled)
A method of diagnosis comprising examining a human or animal body with a diagnostic device and compiling data from the examination, wherein the body is preadministrated with a compound of formula (7):
- wherein R1 denotes H or C1-C4 alkyl, Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom, R2 denotes a bio-molecule residue having at least one free amino function, and X denotes a physiological acceptable anion.
A method of diagnosis comprising administration of a compound of formula (7):
- wherein R1 denotes H or C1-C4 alkyl, Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom, R2 denotes a bio-molecule residue having at least one free amino function, and X denotes a physiological acceptable anion,
- to a human or animal body, examining the body with a diagnostic device and compiling data from the examination.
Radiopharmaceutical composition comprising a compound of formula (7)
- wherein R1 denotes H or C1-C4 alkyl, Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom, R2 denotes a bio-molecule residue having at least one free amino function, and X denotes a physiological acceptable anion, optionally together with a solvent or excipient.
Compound of formula (6)
- wherein R1 denotes H or C1-C4 alkyl, Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom, and X denotes a physiological acceptable anion.
Compound of formula (4)
- wherein R1 denotes H or C1-C4 alkyl and Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom.
Compound of formula (3):
- wherein R1 denotes H or C1-C4 alkyl and Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom.
Compound of formula (2):
- wherein R1 denotes H or C1-C4 alkyl, Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom, and A denotes an amino protection group such as BOC (tert-butyl ester).
Compound of formula (5)
- wherein R1 denotes H or C1-C4 alkyl, Spacer denotes a C1-C4 alkylene group optionally interrupted by an oxygen atom, or R1 and Spacer together with the adjacent nitrogen atom forms a 4-azonia-spiro[3.5]nonyl group, and X denotes a physiological acceptable anion.
Dependencies are inferred from the claim text.