Methods of imaging inflammatory diseases by ligands conjugated to fluorescent compounds

摘要

The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods of imaging of inflammatory diseases using the compounds.

主权项

1. A method of imaging an inflammatory disease comprising the steps of:
a. administering to a patient in need of an effective amount of a compound capable of binding to an inflammatory cell having the formula: or a pharmaceutically acceptable salt or isotope thereof, wherein:
X is an single amino acid or a single amino acid derivative thereof, wherein the single amino acid or single amino acid derivative contains an —OH, —NH2, or —SH functional group wherein the amino acid of the compound is selected from the group consisting of tyrosine, cysteine, serine, lysine, a derivative of tyrosine, a derivative of cysteine, a derivative of serine and a derivative of lysine, andY is a dye that has a fluorescence excitation and emission spectra in the near infra red range, wherein Y is represented by the formula: wherein, X′ is independently selected from the group consisting of O, S, N and C, andR′ is independently selected from the group consisting of CH2 and CH2CH2,and the compound enhances the fluorescence of the dye, Y; and b. fluorescent imaging of an area of the inflammatory disease in the patient's body where the compound has been bound to an inflammatory cell.