Diagnostic or therapeutic somatostatin or bombesin analog...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/655 (2006.01) A61B 1/00 (2006.01) A61K 31/165 (2006.01) A61K 31/4745 (2006.01) A61K 31/519 (2006.01) A61K 38/00 (2006.01) A61K 38/10 (2006.01) A61K 38/31 (2006.01) A61K 47/42 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 51/00 (2006.01) A61P 1/00 (2006.01) A61P 9/00 (2006.01) A61P 11/00 (2006.01) A61P 13/08 (2006.01) A61P 15/00 (2006.01) A61P 25/00 (2006.01) A61P 27/02 (2006.01) A61P 35/00 (2006.01) C07K 7/08 (2006.01)

Patent

CA 2461099

Disclosed are peptide agents and uses thereof that are analogs of biologically active peptides such as somatostatin and bombesin. The compounds of the invention have the general formula X-Y-Z-Q, where X is a cytotoxic agent, therapeutic agent, detectable label or chelating group, and Q is a biologically active peptide. In peptide agents of the invention Y is optionally a hydrophilic polymer or peptide, and Z is a linking peptide bonded to Q at the amino terminus of Q, having two, three, four, or five, amino acid residues selected to link X to Q, while retaining the biological activity of Q. Methods of using these peptide agents in the diagnosis and treatment of diseases are also disclosed.

L'invention concerne des agents peptidiques et leurs utilisations. Il s'agit d'analogues de peptides biologiquement actifs du type somatostatine et bombesine. Les composés considérés sont représentés par la formule générale X-Y-Z-Q. Dans ladite formule, X est un agent cytotoxique, un agent thérapeutique, un marqueur détectable ou un groupe chélateur, et Q est un peptide biologiquement actif. Dans les agents peptidiques décrits, Y est éventuellement un polymère ou un peptide hydrophile, et Z est un peptide de liaison qui est fixé en terminaison amino de Q, avec deux, trois, quatre ou cinq résidus d'acides aminés choisis pour la liaison entre X et Q, sans perte de l'activité biologique de Q. L'invention concerne également des procédés relatifs à l'utilisation des agents peptidiques en question pour le diagnostic et le traitement de maladies.

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