There is provided bombesin-derived compounds of Formula Ia (R.sup.X-L-Xaa.sup.1-Gln-Trp-Ala-Val-Xaa.sup.2-His-Xaa.sup.3-ψ-Xaa.sup.4-NH.sub.2). R.sup.X comprises a radionuclide chelator or a trifluoroborate-containing prosthetic group. L is a linker. Xaa.sup.1 is D-Phe, Cpa (4-chlorophenylalanine), D-Cpa, Tpi (2,3,4,9-tetrahydro-1H-pyrido[3,4b]indol-3-carboxylic acid), D-Tpi, Nal (naphthylalanine), or D-Nal. Xaa.sup.2 is Gly, N-methyl-Gly or D-Ala. Xaa.sup.3 is Leu, Pro, D-Pro, or Phe. Xaa.sup.4 is Pro, Phe, Tac (thiazolidine-4-carboxylic acid), Nle (norleucine), 4-oxa-L-Pro (oxazolidine-4-carboxylic acid). The symbol ψ represents a reduced peptide bond between Xaa.sup.3 and Xaa.sup.4 in which ψ is CH.sub.2—N when Xaa.sup.4 is Pro, Tac or 4-oxa-L-Pro, or ψ is CH.sub.2N(R) when Xaa.sup.4 is Phe or Nle wherein R is H or C.sub.1-C.sub.5 linear or branched alkyl. There is also provided the use of such compounds as imaging agents or therapeutic agents.

The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue via .sup.18F-labeled peptide ligands disclosed herein.

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula ##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

The present invention relates to compounds that can complex a radionuclide and formulations and kits comprising compounds that can complex a radionuclide. The compounds, formulations and kits are of use in radiotherapy and diagnostic imaging.

The invention relates to methods for obtaining liposomes externally modified with a targeting peptide able to selectively drive liposomal doxorubicin on membrane receptors over expressed in tumours.

The invention is based on a kit containing a first vial filled with a sterile, translucent, red dispersion of the liposomal doxorubicin drug; a second vial filled with a modified phospholipid with a reactive function such as DSPEPegmaleimide in lyophilized form; and a third vial filled with a peptide modified with an appropriate reactive function, in a 1:1 stoichiometric amount respect to modified phospholipid and in lyophilized form.

The kit could also contain an additional fourth vial with the targeting peptide modified with a chelating agent able to complex radioactive metal ions for diagnostic and imaging purposes. The patients to be treated with the peptide modified liposomal doxorubicin could be selected on the basis of the over expression of the targeting receptors.

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula

##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

Provided are a novel compound, in which a bombesin derivative known as having selectivity with respect to prostate cancer bonds with a ligand via aminomethyl galacturonic acid, a complex compound that covalently bonds with a radioactive isotope via the ligand of the novel compound, methods of preparing the compounds, and a nuclear-based molecular imaging agent including the complex compound.

The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue via .sup.18F-labeled peptide ligands disclosed herein.

The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue via .sup.18F-labeled peptide ligands disclosed herein.