Homoglutamic acid derivatives

摘要

This invention relates to homoglutamic acid derivatives suitable for labeling or already labeled with 18F or 19F, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.

主权项

1. A compound of formula (II): wherein - - - indicates a single or double bond between the C-4 and C-5 positions of the compound; R2 and R3 are Hydrogen; R1 is X, wherein X is
a fluorine atom, F, with the proviso that there is no double bond between C-4 and C-5,branched or straight-chain F—C1-C10 alkyl wherein the alkyl chain is optionally interrupted by 1 or 2 oxygen atoms with the proviso that there are at least two methylene groups between two oxygen atoms,branched or straight-chain F—C1-C10 alkoxy with the proviso that there is no double bond between C-4 and C-5 and wherein the carbon chain is optionally interrupted by 1 additional oxygen atom with the proviso that there are at least two methylene groups between two oxygen atoms,F—C6-C10 mono- or bicyclic aryl-(CH2)n wherein n=1 to 3,F-mono- or bicyclic heteroaryl-(CH2)n wherein n=1 to 3,F—C3-C6 cycloalkyl with the proviso that F is attached to one of the CH2 groups of the ring,F—C3-C6 cycloalkyl-(CH2)n, wherein n=1 to 3, with the proviso that F is attached to one of the CH2 groups of the ring,F—C6-C10 mono- or bicyclic aryl-(CH2)n—O, wherein n=1 to 3 with the proviso that there is no double bond between C-4 and C-5, orF-mono- or bicyclic heteroaryl-(CH2)n—O wherein n=1 to 3, with the proviso that there is no double bond between C-4 and C-5; R4=Hydrogen or O-protecting group; R5=Hydrogen or O-protecting group; R6=Hydrogen or N-protecting group; R7=Hydrogen or N-protecting group; or the group NR6R7 is a 1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl (phthalimido) or an azido group, wherein heteroaryl comprises 5 to 10 ring atoms wherein 1 or 2 ring atoms are heteroatoms, wherein the fluorine atom, F, means fluorine optionally in an isotope form, and encompassing single isomers, E and Z-isomers, diastereomers, enantiomers, mixtures thereof and suitable salts thereof.