Abstract: To provide a diagnostic and therapeutic medicament, a bombesin analog peptide antagonist conjugate is provided which has general Formula (I), wherein A is a metal chelator comprising at least one radionuclide metal, B is a spacer linked to N-terminal of C or a covalent bond and C is a bombesin analog peptide antagonist having a sequence as claimed, where further x is an Integer from 1 to 3 and n is an integer from 1 to 6.

Abstract: To provide a diagnostic and therapeutic medicament, a bombesin analog peptide antagonist conjugate is provided which has general Formula (I), wherein A is a metal chelator comprising at least one radionuclide metal, B is a spacer linked to N-terminal of C or a covalent bond and C is a bombesin analog peptide antagonist having a sequence as claimed, where further x is an integer from 1 to 3 and n is an integer from 1 to 6.

Abstract: The invention relates to a method of imaging pancreatic ?-cells, endocrine gastroenteropancreatic tumors and bronchial and thyroid neuroendocrine tumors and a method of treating endocrine gastroenteropancreatic tumors and bronchial and thyroid neuroendocrine tumors by targeting of glucose-independent insulinotropic polypeptide receptors (GIP receptors). Compounds considered are GIP or a GIP analog, each carrying a radionuclide, optionally complexed through a chelator. Non-radioactive GIP receptor antagonists as such are also considered in the long-term treatment of the mentioned tumors. The invention also relates to the use of a combination of GIP or a GIP analog, each carrying a radionuclide, with a GLP-1 agonist and/or somatostatin analogs, also carrying a radionuclide.

Abstract: The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.

Abstract: SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates.

Abstract: Peptidic NPY antagonists selective for Y1 having an organic chelator, such as DOTA, coupled thereto which are useful for diagnostic procedures and receptor-mediated radiotherapy.

Abstract: SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates.

Abstract: SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.

Abstract: To provide a diagnostic and therapeutic medicament, a bombesin analog peptide antagonist conjugate is provided which has general Formula (I), wherein A is a metal chelator comprising at least one radionuclide metal, B is a spacer linked to N-terminal of C or a covalent bond and C is a bombesin analog peptide antagonist having a sequence as claimed, where further x is an integer from 1 to 3 and n is an integer from 1 to 6.

Abstract: In one embodiment, a method for treating a cancerous disease is provided which includes characterizing a disease by an overexpression of one or more somatostatin receptors, and exposing the one or more somatostatin receptors to a pharmaceutical composition comprising a somatostatin analogue which binds to the one or more somatostatin receptors.

Abstract: The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.

Abstract: SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.

Abstract: Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,C?Me-L-2Nal8]-SRIF, and counterparts incorporating D-Cys3 and/or D-Trp8 and/or Ala11, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.

Abstract: In one embodiment, a composition of somatostatin analogues having the general formula: is provided wherein Z may be absent or present and when present is selected from DOTA- and DTPA-based chelators, NOTA-based chelators, carbonyl compounds, hydrazino nicotinamide, N4-chelators, desferrioxamine, NxSy-chelators, optionally complexed or labeled with a radioisotope, tyrosine for halogenation, a fluorescent dye, or biotin. The composition further provides that L may or may not be present and when present is a linker molecule, X1 is glutamic acid or a symmetric or asymmetric diamino acid containing 3 or 4 consecutive C atoms, X2 is a positively charged natural or unnatural amino acid, an arginine mimic, citrulline, or a neutral amino acid, X3 is phenylalanine, Ala-[3-(2-thienyl)], ?-naphthylalanine, or ?-naphthylalanine, X4 is an aromatic amino acid, X5 is threonine or serine, and X6 is phenylalanine, Ala-[3-(2-thienyl)], ?-naphthylalanine, or ?-naphthylalanine.

Abstract: Radionuclide labelled conjugates based on substance P and analogues thereof with the chelator (DOTAGA) (1-(1-rarboxy-3-carboxy-propyl)-4,7,10(carboxymethyl)-1,4,7,10-tetraazacyclo-dodecane, DOTASA (1-(1-carboxy-2carboxy-ethyl)-4,7,10(carboxymethyl)1,4,7,10-tetraazacyclo-dodecane, or chelator (DOTA) [1,4,7,10 tetraazaacyclo-dodecane 1,4,7,10-tetra(acetic acid)] are useful radiopharmaceutical substances for targeting and treatment of brain tumors, especially gliomas.

Abstract: The invention relates to a peptide compound having an improved binding affinity to somatostatin receptors, comprising a somatostatin analogue as the peptide and a chelating group covalently linked to the N-terminal free amino group of said peptide, wherein said somatostatin analogue carries an 1-naphthylalanine or a 3-benzothienylalanine residue in its 3-position. The invention further relates to said peptide compound labeled with a detectable element or with a therapeutic radionuclide, as well as to a diagnostic method and to a method for the therapeutic treatment of tumors, by using the labeled compounds.

Abstract: Analogs of SRIF which are selective for SSTR1 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR1 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,5[D-Trp8, N?MeIAmp9, Tyr11]-SRIF and counterparts incorporating Cbm at the N-terminus and/or N?Ser13, inhibit the binding of a universal SRIF radioligand to the cloned human receptor SSTR1, but they do not bind with significant affinity to human SSTR2, SSTR3, SSTR4 or SSTR5. By incorporating an iodinated tyrosine in position-2 or in position-11 in these SSTR1-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. The N-terminus accommodates bulky moieties without loss of selectivity, and a carbamoyl moiety or a conjugating agent that will accept a radioactive nuclide or will link to a cytotoxin may be present at the N-terminus.

Abstract: Compounds and methods for the diagnosis and treatment of tumors, including breast and prostate tumors and metastases thereof using radiolabelled peptides that bind to GRP receptors. The peptides are Bombesin analogs wherein the first and optionally the third amino acid are modified.

Abstract: The present invention relates to novel somatostatin analogues of the general formula (I) wherein Z may be absent or present and when present is selected from the group consisting of DOTA- and DTPA-based chelators, NOTA-based chelators, cabonyl compounds, hydrazino nicotinamide (hynic), N4-chelators, desferrioxamin, NxSy-chelators, all optionally complexed or labeled with a radioisotope, Tyrosine (Tyr) for halogenation, a fluorescent dye or biotin; L may or may not be present and is a linker molecule; X1 is a symmetric or asyrnmetric diamino acid, containing 3 or 4 consecutive C atoms with a linker to the chelating agent, for example D/L-diamino butyric acid (D/L-Dab) for a more basic character or D/L-Glu for coupling to primary and secondary amino groups; X2 is a positively charged natural or unnatural amino acid or arginine mimic or citrulline, or a neutral amino acid like Asn; X3 is phenylalanine (Phe), Ala-[3-(2-thienyl)] or &agr;-,&bgr;-naphthylalanine; X4 is an aromatic amino acid, optionally h

Abstract: The invention relates to a method of detecting and localizing malignant tumours and their metastases in tissues, which in healthy condition do not contain disturbing quantities of CCK-receptors, in the body of a human being, which comprises (i) administering to said being a composition comprising, in a quantity sufficient for external imaging, a labelled peptide derived from a compound of the general formula 1   ⁢ ( I ) H - ( Xaa ) n - ( Xbb ) m - Tyr - Xcc - Gly 5 - Trp - Xdd - Asp - Phe - R 2