Nihon Medi-physics Company, Limited

Kyoto University

Ikuya Seki

Hideo Saji

Masahiro Ono

Yoshifumi Shirakami

Yoshitoshi Itaya

Koichi Hanaoka

Masafumi Ihara

Takayoshi Kawaguchi

Hiroyuki Kimura

Hiroki Matsumoto

Komei Washino

Marino Maemura

The present invention relates to a radioactive halogen-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a specific general formula or a salt thereof, or a radiopharmaceutical comprising the same.

Radioactive halogen-labeled pyrido [1,2-A] benzimidazole derivative compound

The present invention relates to a radioactive iodine-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a definite general formula or a salt thereof, or a radiopharmaceutical comprising the same.

Radioactive iodine labeled pyrido[1,2-a]benzoimidazole derivative compound

Embodiments of the invention provide a compound accumulating in an inflammatory site, a diagnostic agent containing the compound in labeled state and its precursor compound for labeling. Such a compound accumulating in inflammatory site may be represented by the following formula (1):Z&#x2014;Y-Leu-Phe-(X)-Lys(-(Lys)-HalB)-(Lys)-NH&#x2003;&#x2003;(1)

Compound accumulating in inflammatory site, diagnostic agent containing the compound in labeled state and its precursor compound for labeling

The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), Ris a radioactive iodine. 

Radioactive iodine labeled organic compound or salt thereof

By preliminarily dissolving a basic organic compound in an aqueous solvent in which a peptide usable in metal-labeling is to be dissolved, the solubility of the peptide is improved and thus metal-labeling can be carried out without heating. A composition for medical use containing a peptide usable in metal-labeling and a basic organic compound acceptable as a pharmaceutical additive can be utilized as a preparation useful in image diagnosis, radiotherapy and so on.

Composition for medical use having improved water-solubility of peptide and metal-labeling efficiency and preparation for medical use comprising metal-labeled peptide

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.

Compound binding to leukocytes and medicinal composition containing the compound in labeled state as the active ingredient

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.

Tumor affinity peptide, and radioactive diagnostic agent and radioactive

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.

Metal chelate forming peptides and use thereof represented by three

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.

Growing community of inventors

Tokyo, Japan

Ikuya Seki