This disclosure provides a family of compounds that absorb and fluoresce in the short wave infrared region (SWIR, optionally 1000 nm to 1300 nm), including hydrophilic compounds that exhibit absorption and emission spectral profiles in aqueous solutions substantially similar to those observed in organic solvents such as methanol or DMSO. The compounds can be chemically linked to biomolecules including proteins, nucleic acids, and therapeutic small molecules. The compounds are useful for imaging in a variety of medical, biological and diagnostic applications, including SWIR in vivo imaging of regions of interest within a mammal.

Multinuclear complexes and methods for preparing them are provided. The discrete multinuclear complexes include a one or more transition metals and a radioisotope having the same coordination geometry as the transition metal. A bridging ligand is coordinated to the transition metal and the radioisotope to link the transition metal and the radioisotope and pendent ligands are coordinated to each of the transition metal and the radioisotope to stabilise the complex. The multinuclear complexes may include a radioisotope or radioelement that can be detected by medical equipment and may find use in therapy and/or the diagnosis of disease in patients.

The present invention relates to radiolabeled compounds of formula I ##STR00001##
wherein either A, B, R.sub.1, R.sub.2, is labeled with a radionuclide selected from .sup.3H, .sup.11C and .sup.18F and its use for imaging alpha synuclein and/or Abeta deposits in mammals.

A cancer targeting composition, kit, and method for treatment of cancer cells overexpressing somatostatin receptors is disclosed. The composition includes a radioisotope, a chelator, and a targeting moiety. The chelator includes a nitrogen ring structure including a tetraazacyclododecane, a triazacyclononane, and/or a tetraazabicyclo [6.6.2] hexadecane derivative. The targeting moiety includes a somatostatin receptor targeting peptide. The somatostatin receptor targeting peptide includes an octreotide derivative. The targeting moiety is chelated to the radioisotope by the chelator whereby the cancer cells are targeted for elimination.

6-[.sup.18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [.sup.18F]DCFPyL, [.sup.68Ga]HBED-CC-PSMA, [.sup.18F]PSMA-1007 and [Al.sup.18F]HBED-CC-PSMA. Unexpectedly, the 6-[.sup.18F]fluoro-2-alkoxy and 6-[.sup.18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [.sup.18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the .sup.18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[.sup.18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [.sup.68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

Provided herein are methods for treating metastatic prostate cancer using anti-androgen compounds and radionuclide-labeled androgens.

The present invention provides a radiopharmaceutical composition comprising the following four components: (i) a radio-labelled compound; (ii) ethanol; (iii) a stabilizer of the radio-labelled compound; and (iv) a cyclodextrin.

The present invention also provides a radiopharmaceutical composition comprising: (i) a radio-labelled compound; (ii) a stabilizer of the radio-labelled compound, wherein the stabilizer comprises: ascorbic acid, aspartic acid, cysteine, maleic acid, gentisic acid, glutathione, glutamic acid, mannitol, nicotinamide, calcium chloride, N-t-butyl-alpha-phenylnitrone (PBN), tartaric acid, para-aminobenzoic acid (pABA), chloride ions or salts or combinations thereof; and (iii) a cyclodextrin.

Fibroblast activation protein (FAP)-targeting compounds (e.g., conjugates); a method for imaging cancer or fibrosis; and methods for treating an inflammatory disease/disorder and cancer.

Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds. ##STR00001##

Methods of ex vivo labeling of a biological material for in vivo imaging, methods of labeling a biological material in vivo, methods for preparing a labeling agent, and methods for in vivo imaging of a subject using a biological material labeled with a labeling agent are disclosed. In one non-limiting example, the biological material is selected from cells and the labeling agent is a .sup.89Zr-Desferrioxamine-NCS labeling agent.