Biological targeting agents

Details Biological targeting agents Biological targeting agents

C - Chemistry, Metallurgy

07

K

C07K 1/13 (2006.01) A61K 51/08 (2006.01) C07K 5/00 (2006.01) C07K 7/00 (2006.01) C07K 7/06 (2006.01) C07K 14/00 (2006.01) C07K 14/655 (2006.01)

Patent

CA 2179990

A conjugate comprises a linear or cyclic synthetic peptide of 3-50 amino acids linked via one of its carboxyl groups and optionally via a linking group, to a polydentate metal chelating group, with the result that endo- or exo-peptidase metabolism of the peptide is substantially inhibited, with the provisos that: a) the peptide chain contains a biological targeting sequence which is biologically active; b) when the spacer is absent the metal chelating group does not comprise solely peptide moieties; c) the metal chelating group does not contain thiol donors. A complex of the conjugate with a metal atom chelated by the metal chelating group is useful in medicine.

Un conjugué comprend un peptide synthétique linéaire ou cyclique possédant de 3 à 50 acides aminés liés, par l'intermédiaire d'un de ses groupes carboxyle et facultativement par un groupe de liaison, à un groupe chélateur de métal polydenté, ceci afin d'inhiber sensiblement le métabolisme endo ou exo-peptidase du peptide, aux conditions que: a) la chaîne peptidique contienne une séquence de ciblage biologique qui soit biologiquement active; b) lorsque l'espaceur est absent, le groupe chélateur de métal ne comprennent pas seulement des fractions peptidiques; et c) que le groupe chélateur de métal ne contienne pas de donneurs de thiol. Un complexe de ce conjugué avec un atome de métal chélateur par le groupe chélatem de métal est utile en médecine.

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