Method for the selective and quantitative functionalization...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 51/10 (2006.01)

Patent

CA 2503647

The invention provides chemical conjugates between an immunoglobulin Fab fragment and molecular entities imparting diagnostic or therapeutic utility, whereby the only sites of conjugation on the Fab fragment are one s or both of the sulfhydryl groups deriving from the selective and quantitative reduction of the inter-chain disulfide bond of said Fab fragment and whereby said molecular entities imparting diagnostic or therapeutic utility have at least one free sulfllydryl-reactive group, characterized in that the conjugation stoichiometric molar ratio molecular entity to Fab fragment is in the range from 0.95 to 1.05 or in the range from 1.95 to 2.05. The invention also provides a process for preparing said conjugates and pharmaceutical compositions thereof.

L'invention concerne des conjugués chimiques venant entre un fragment FAB d'immunoglobuline et des entités moléculaires apportant une utilité diagnostique ou thérapeutique. Les seuls sites de conjugaison du fragment FAB sont constitués d'un ou de deux groupes sulfhydryle dérivés de la réduction sélective et quantitative de la liaison bisulfure interchaîne dudit fragment FAB, et les entités moléculaires d'utilité diagnostique ou thérapeutique possèdent au moins un groupe réagissant au sulfhydryle libre, caractérisés en ce que le rapport molaire stoïchïométrique de conjugaison entre l'entité moléculaire et le fragment FAB oscille entre 0,95 et 1,05 ou entre 1,95 et 2,05. L'invention concerne également un procédé de préparation desdits conjugués et de leurs compositions pharmaceutiques.

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