Cross-linkers with high reactivity and solubility and their...

Details Cross-linkers with high reactivity and solubility and their... Cross-linkers with high reactivity and solubility and their...

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 47/48 (2006.01) C07K 16/18 (2006.01) C07K 16/28 (2006.01)

Patent

CA 2495795

Disclosed is a method of making conjugates of cell binding agents and small molecule drugs comprising reacting a cell binding agent with a bifunctional cross- linking moiety to thereby provide the cell binding agent with a reactive disulfide group and then reacting the modified cell binding agent with a small molecule drug comprising a free thiol group. Bifunctional cross-linking moieties are also disclosed. (see formula I)

L'invention concerne une méthode de fabrication de conjugués d'agents de liaison cellulaire et de médicaments à petites molécules, consistant à faire réagir un agent de liaison cellulaire avec un fragment de réticulation bifonctionnel pour fournir ainsi à l'agent de liaison cellulaire un groupe disulfure réactif, puis à faire réagir l'agent de liaison cellulaire modifié avec un médicament à petite molécule comprenant un groupe thiol libre. L'invention concerne également des fragments de réticulation bifonctionnels.

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