Conjugated moieties for chelating paramagnetic metals

Details Conjugated moieties for chelating paramagnetic metals Conjugated moieties for chelating paramagnetic metals

C - Chemistry, Metallurgy

07

K

C07K 14/00 (2006.01) A61K 47/48 (2006.01) A61K 49/08 (2006.01) C07C 323/41 (2006.01) C07C 323/60 (2006.01) C08G 69/10 (2006.01)

Patent

CA 2090033

In this method, one attaches one or more chelatant molecules to a mono- or polyamino intermediate compound which is temporarily immobilized on a solid phase by a splittable bond. Thereafter, the bond is split to release the desired conjugate moiety, whereby a reactive site is generated at the splitting site. The conjugate can be coupled to a protein homing factor using that reactive site; the latter being single per chelatant molecule, undesirable cross-linking during conjugation is substantially avoided.

Selon ce procédé, une ou plusieurs molécules chélatrices sont fixées à un composé (I) intermédiaire mono ou polyamino qui est immobilisé sur une phase solide par une liaison pouvant se scinder. Ensuite, ladite liaison est scindée pour libérer la fraction conjuguée désirée, par laquelle un site réactif est généré au site de scission. Le conjugué peut être couplé à un facteur de guidage protéinique par utilisation dudit site de réaction; ce dernier étant unique par molécule chélatrice, on évite ainsi la réticulation indésirable lors de la liaison conjuguée.

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