Abstract: The invention provides a method for producing radiolabeled tyrosine derivatives with good purity and stability, by a safe method suitable for industrial production of pharmaceuticals. The invention relates to a method for producing Compound (5) and Radiolabeled Compound (6) as follows: wherein each symbol is as defined in the description.

Abstract: The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is 211At, 210At, 123I, 124I, 125I, or 131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)2) or an ester group thereof, with a radionuclide selected from 211At, 210At, 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.

Abstract: The invention provides a method for producing a solution containing 211At? (astatide ion) at a high radiochemical purity by using 211At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from 211At. The invention also provides a solution containing 211At? (astatide ion) at a radiochemical purity of not less than 30%.

Abstract: The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is 211At, 210At, 123I, 124I, 125I, or 131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)2) or an ester group thereof, with a radionuclide selected from 211At, 210At, 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.

Abstract: The invention provides a method for producing a solution containing 211At? (astatide ion) at a high radiochemical purity by using 211At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from 211At. The invention also provides a solution containing 211At? (astatide ion) at a radiochemical purity of not less than 30%.

Abstract: To develop a compound which is highly accumulated in cancer cells and capable of emitting an ?-ray and provide a pharmaceutical composition for cancer treatment including the compound. A pharmaceutical composition for cancer treatment including a compound having a structure in which 211At is introduced as a substituent into an amino acid derivative having an affinity with an amino acid transporter LAT1 or a pharmaceutically acceptable salt of the compound.

Abstract: To develop a compound which is highly accumulated in cancer cells and capable of emitting an ?-ray and provide a pharmaceutical composition for cancer treatment including the compound. A pharmaceutical composition for cancer treatment including a compound having a structure in which 211At is introduced as a substituent into an amino acid derivative having an affinity with an amino acid transporter LAT1 or a pharmaceutically acceptable salt of the compound.

Abstract: The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is 211At, 210At, 123I, 124I, 125I, or 131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)2) or an ester group thereof, with a radionuclide selected from 211At, 210At, 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.

Abstract: The invention provides a method for producing a solution containing 211At? (astatide ion) at a high radiochemical purity by using 211At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from 211At. The invention also provides a solution containing 211At? (astatide ion) at a radiochemical purity of not less than 30%.

Abstract: A stabilized radiopharmaceutical composition, a kit including same, and a method for making same, where the radiopharmaceutical is (i) susceptible to either reductive degradation or radiolysis and which includes a metal complex of a radionuclide with a ligand, (ii) a first stabilizer for the radiopharmaceutical which is an amino-substituted aromatic carboxylic acid or a salt, ester or amide thereof, and (iii) a second stabilizer for the radiopharmaceutical which is a diphosphonic acid or salt thereof. The first and second stabilizers are present in an amount effective to stabilize the radiopharmaceutical, and the radiopharmaceutical is not a metal complex of the diphosphonic acid.

Abstract: A compound that comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr that increases the binding ratio to monocytes and lymphocytes in all leukocytes, a group that can be labeled with a radioactive metal or a paramagnetic metal, and spacers binding the three moieties together shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro. Owing to this characteristic, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and the like, for imaging sites of inflammation.

Abstract: A compound binding to leukocytes, which comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr elevating the binding ratios to monocytes and lymphocytes in all leukocytes, a group which can be labeled with a radioactive metal or a paramagnetic metal, and a spacer binding them shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro and can be labeled with a radioactive metal or a paramagnetic metal. Owing to these characteristics, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and so on wherein imaging is performed in a site with vigorous leukocyte infiltration accompanied by an immune reaction in an individual.

Abstract: The present invention provides an improved stabiliser for radiopharmaceuticals which inhibits impurities from being produced by two kinds of decomposition mechanisms and exhibits such an effect that the shelf life of a radiopharmaceutical after its preparation is prolonged as compared with conventional ones. The improvement comprises a combination of an amino-substituted aromatic carboxylic acid or its salt, ester or amide in combination with a diphosphonic acid or its salt.

Abstract: A peptide having affinity with tumor or a salt thereof, which comprises an amino acid sequence containing 20 or less amino acid residues, said amino acid sequence being described as X.sub.1 -YCAREPPT-X.sub.2 wherein A, C, E, P, R, T and Y represent amino acid residues expressed by standard one-letter symbols, each of amino acid residues A, C, R and Y in the amino acid sequence YCAR may be in either L-form or D-form, X.sub.1 represents a basic organic compound having 1-3 amino groups, and X.sub.2 represents any given amino acid sequence, is provided together with a radioactive diagnostic agent and a radioactive therapeutic agent containing the above peptide or a salt thereof. The present tumor affinity peptide is high in radioactive metal labeling yield, useful for imaging and treating pathological tissues such as of breast cancer, ovarian cancer and colon cancer of mammals including human, and difficult to be readily metabolized in organisms and to accumulate in normal tissues especially at kidney and liver.

Abstract: A peptide having affinity with inflammation is disclosed, which contains at least one of the following amino acid sequences:LLGGPS (SEQ ID NO:1),LLGGPSV (SEQ ID NO:2),KEYKAKVSNKALPAPIEKTISK (SEQ ID NO:3),KEYKCKVSNKALPAPIEKTISK (SEQ ID NO:4),KTKPREQQYNSTYR (SEQ ID NO:5), andKTKPREQQYNSTYRVV (SEQ ID NO:6),wherein A, C, E, G, I, K, L, N, P, Q, R, S, T, V, and Y represent amino acid residues expressed by standard one-letter symbols. According to the present invention, a peptide and its chemically modified substances, radioactive metal labeled peptides derived therefrom, and radioactive diagnostics comprising such peptide are provided, which are useful for imaging inflammation region and easy in preparation handling, and accumulate at inflammation site immediately after administration while being excellent in clearance into urine. The imaging is possible in several ten minutes after administration.

Abstract: The invention provides, inter alia, metal radionuclide-labelled reagent comprising a metal radionuclide coordinated with a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an Asp residue, a Tyr residue or a Lys residue; X2 represents an amino acid residue other than a Cys residue and a Pro residue, provided that X2 does not represent a Gly residue when X1 represents an Asp residue; wherein functional groups at the N-terminus, C-terminus and side chain may be optionally substituted with protecting groups; and wherein each of the amino acid residues may be either D-form or L-form.

Abstract: The invention provides a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an amino acid residue other than Cys residue; X2 represents an amino acid residue other than Cys residue and Pro residue; functional groups at the N-terminus, C-terminus and side chain may be substituted with protecting groups; and each of the amino acid residues may be any of D-form and L-form. Further, the invention provides a complex of the peptide with a physiologically active peptide, protein or other substance; a labeled reagent obtained by labeling the peptide or the complex with a metal radionuclide; and a radiodiagnostic and radiotherapeutic composition comprising the metal radionuclide-labeled reagent.

Abstract: A radioactive diagnostic or therapeutic agent, which comprises a metallic element-labeled high molecular compound which comprises one unit of (1) a polyamine compound having at least three amino groups in the side chains per molecule, at least two units of (2) a chelate-forming compound having a carboxyl group, at least one unit of (3) a physiologically active substance and (4) at least two radioactive metallic elements, each unit of the chelate-forming compound (2) and the physiologically active substance (3) being combined to any of the amino groups in the side chains of the polyamine compound (1) and each of the radioactive metallic element (4) being chelate-bonded to the chelate-forming compound (2).