Compound binding to leukocytes and medicinal composition...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/02 (2006.01) A61K 38/00 (2006.01) A61K 38/08 (2006.01) A61K 49/00 (2006.01) A61K 49/14 (2006.01) A61K 51/00 (2006.01) A61K 51/08 (2006.01) A61N 5/10 (2006.01) A61P 37/00 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2498826

A compound binding to leukocytes, which comprises Met 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., neutrophilic leukocytes, 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.

L'invention concerne un composé se liant aux leucocytes, qui comprend Met ou Nle-Leu-Phe comme site de liaison de leucocyte de récepteur de peptide formyle, une partie de liaison renfermant Ser ou Thr qui élève les degrés de liaison aux monocytes et aux lymphocytes dans tous les leucocytes, un groupe susceptible d'être marqué avec un métal radioactif ou paramagnétique, et un espaceur qui les lie montrant des propriétés de liaison spécifiques à tous les leucocytes, à savoir leucocytes neutrophiles, monocytes et lymphocytes in vivo et in vitro, et capable d'être marqué avec un métal radioactif ou paramagnétique. Par ces caractéristiques, le composé est très utile en diagnostic d'image SPECT, diagnostic d'image PET, diagnostic d'image IRM, etc., l'imagerie intervenant dans un site à infiltration vigoureuse de leucocyte accompagnée par une réaction immunitaire chez l'individu.

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