Abstract: The labeling of biologically important molecules via a bifunctional chelator can result in the formation of isomers or multiple species, which can have significant impact on the biological properties of the radiopharmaceutical. For receptor-based radiopharmaceuticals, the target uptake is largely dependent on the receptor binding affinity of the targeting molecule and the blood clearance of the labeled molecule, which is determined by the physical properties of both the targeting molecule and the metal chelate. Hence, the presence of isomers for the metal chelate can have significant impact on the radiopharmaceutical. Therefore, in the development of a radiopharmaceutical or metallodrug, it is necessary to separate the isomers and evaluate the biological activities of each individual isomer. It would therefore be desirable to develop chelators that predominately form only a single stereoisomeric species upon coordination to a metal center.

Abstract: A peptide-chelator conjugate that is useful for imaging sites of inflammation in humans comprises a metal chelator coupled to a glycopeptide antibiotic. The metal chelator and the glycopeptide are coupled by a linking group. The linking group may be the divalent radical NH--(CH.sub.2).sub.3 --NH. Alternatively the linking group may be .beta.Ala.sub.3 LysGly-OH and the glycopeptide may be coupled to the N.sup..epsilon. of Lys. A method of imaging a site of inflammation is also provided. The method comprises the step of administering a diagnostically effective amount of a composition comprising a glycopeptide-chelator conjugate comprising a metal chelator coupled to a glycopeptide antibiotic. The glycopeptide-chelator conjugate is in a form complexed with a diagnostically useful metal or an oxide or nitride thereof.

Abstract: Described herein are D4 receptor-selective compounds of the formula: ##STR1## wherein R.sup.1 is selected from H and an acid labile protecting group; and R.sup.2 and R.sup.3 are independently selected from H, radioisotopic halo, loweralkoxy and tri(loweralkyl)tin; and salts, solvates or hydrates thereof.Also described is the use of these compounds as pharmaceuticals to treat indications for which a dopamine D4 receptor antagonist is indicated. Radiolabeled compounds are useful particularly to image localization of D4 receptor in the human brain, and can therefore aid in the diagnosis of schizophrenia and other medical conditions in which the D4 receptor is implicated.

Abstract: For use in imaging sites of diagnostic interest within the body, the present invention provides radionuclide chelators of formula (I), wherein X is a linear or branched, saturated or unsaturated C.sub.1-4 alkyl chain that is optionally interrupted by one or two heteroatoms selected from N, O and S; and is optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl C.sub.1-4 alkyl, aryl and C(O)Z; Y is H or a substituent defined by X; X and Y may together form a 5- to 8-membered saturated or unsaturated heterocyclic ring optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl oxo, C.sub.1-4 alkyl, aryl and C(O)Z; R.sup.1 through R.sup.4 are selected independently from H; carboxyl; C.sub.1-4 alkyl; C.sub.1-4 alkyl substituted with a group selected from hydroxyl, amino, sulfhydryl, halogen, carboxyl, C.sub.1-4 alkoxycarbonyl and aminocarbonyl; an alpha carbon side chain of a D- or L-amino acid other than proline; and C(O)Z; R.sup.5 and R.

Abstract: Peptide-chelator conjugates are provided that when labelled with a traceable metal are useful for diagnostic imaging of sites of inflammation. The peptide component is an antagonist of the naturally occurring tetrapeptide tuftsin while the chelator component serves as a labelling site for metals, in particular radionuclide metals such as technetium-99 m.

Abstract: Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.

Abstract: Detectably labelled non-receptor mediated cell-associating compounds are provided for use in the diagnostic imaging of target sites in a mammal. Cell-associating compounds may be directly labelled, or labelled via a chelating compound to form a conjugate. Such cell-associating compounds are particularly useful to image target sites such as tumour sites and sites of infection.

Abstract: Compounds useful for high resolution diagnostic imaging incorporate an imaging agent having a chelator that is linked by a metal-cleavable bond to a ligand that has affinity for a site removed from the site of diagnostic interest. Upon labelling, the ligand is cleaved leaving the labelled imaging agent free to localize at the site of diagnostic interest unhindered, while the ligand and any unlabelled imaging agent is sequestered to the removed site. By sequestering unlabelled imaging agent, the labelled imaging agent does not compete to occupy the site of interest, resulting in images of enhanced resolution.

Abstract: Described is a process for labelling ligands with metals comprising the steps of covalently coupling the ligand to a solid support via a metal-cleavable linker; introducing a complex-forming metal to the support; and collecting the metal-ligand complex released from the support. The metal catalyzes cleavage of the ligand from the support upon complex formation resulting in a solution substantially free of unlabelled ligand.

Abstract: For use in imaging sites of diagnostic interest within the body, the present invention provides radionuclide chelators, optionally coupled to targeting molecules such as peptides of the formula: ##STR1##

Abstract: Herein described are radiolabeled compounds and their precursors useful to image D4 receptors in vivo, of the formula: ##STR1## wherein R is selected from iodo, tri(loweralkyl)tin and a radioisotopically labeled iodide and R.sup.1 is selected from H and alkoxycarbonyl, with the proviso that R is not iodo when R.sup.1 is H.The radiopharmaceutical compounds are useful particularly to image localization of D4 receptor in the human brain, and can therefore aid in the diagnosis of schizophrenia and other medical conditions in which the D4 receptor is implicated.

Abstract: Detectably labelled non-receptor mediated cell-associating compounds are provided for use in the diagnostic imaging of target sites in a mammal. Cell-associating compounds may be directly labelled, or labelled via a chelating compound to form a conjugate. Such cell-associating compounds are particularly useful to image target sites such as tumour sites and sites of infection.

Abstract: Peptide-chelator conjugates are provided that when labelled with a traceable metal are useful for diagnostic imaging of sites of inflammation. The peptide component is an antagonist of the naturally occurring tetrapeptide tuftsin while the chelator component serves as a labelling site for metals, in particular radionuclide metals such as technetium-99m.

Abstract: For use in imaging sites of diagnostic interest within the body, the present invention provides radionuclide chelators, optionally coupled to targeting molecules such as peptides of the formula: ##STR1##

Abstract: Radionuclide chelating compounds are provided for conjugation to targeting molecules such as proteins, peptides or antibodies. The resulting labeled targeting molecules may be used in diagnosis and therapy.

Abstract: Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.

Abstract: Peptide-chelator conjugates are provided that when labelled with a traceable metal are useful for diagnostic imaging of sites of inflammation. The peptide component is an antagonist of the naturally occurring tetrapeptide tuftsin while the chelator component serves as a labelling site for metals, in particular radionuclide metals such as technetium-99m.

Abstract: Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.