C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 491/12 (2006.01) C07D 498/18 (2006.01)
Patent
CA 2417858
The present invention discloses a one-step process for the production of cytotoxic conjugates of maytansinoids and cell binding agents. Maytansinoids having a disulfide linker that bears a reactive moiety are linked to cell binding agents, such as antibodies, without prior modification of the cell binding agent. DM1-S-S-CR1R2-(CH2)n-CO2-X represents a maytansinoid having disulfide moiety that bears a reactive group. These conjugates are useful as therapeutic agents which are delivered specifically to target cells and are cytotoxic.
La présente invention concerne un procédé de préparation en une étape de conjugués cytotoxiques à base de maytansinoïdes et d'agents de fixation des cellules. Ces maytansinoïdes comprennent un élément de liaison disulfure renfermant un fragment réactif et sont liés à des agent de fixation des cellules, tels que des anticorps, sans modification préalable de l'agent de fixation des cellules. Ces conjugués sont destinés à être utilisés comme agents thérapeutiques dirigés spécifiquement contre des cellules cibles et sont cytotoxiques.
Chari Ravi V. J.
Widdison Wayne C.
Gowling Lafleur Henderson Llp
Immunogen Inc.
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