Improved cytotoxic agents comprising new maytansinoids

A technology of maytansine and cells, which is applied in the direction of medical preparations containing active ingredients, antiviral agents, and medical preparations with non-active ingredients, which can solve problems such as instability
CN1956722AInactive Publication Date: 2007-05-02IMMUNOGEN INC
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
IMMUNOGEN INC
Publication Date
2007-05-02
Estimated Expiration
Not applicable · inactive patent

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Abstract

New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the alpha-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
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Description

[0001] This application claims the benefit of Provisional Application No. 60 / 471,739, filed May 20, 2003, the disclosure of which is hereby incorporated by reference. technical field

[0002]

[01] The present invention relates to methods of preparing improved cytotoxic conjugates comprising maytansinoids and cell-binding agents. These conjugates are therapeutically useful when delivered to specific cell populations in a targeted manner. The present invention also relates to methods of preparing maytansinoids with thiol moiety, which can be used to prepare cytotoxic conjugates. The present invention further relates to novel maytansinoids, and novel intermediates in the synthesis of novel maytansinoids. Background technique

[0003]

[02] There are many reports trying to specifically target tumor cells with monoclonal antibody-drug conjugates (Sela et al., Immunoconjugates 189-216 (C.Vogel, ed.1987); Ghose et al, Targeted Drugs 1-22 (E.Goldberg, ed.1983); Diener et al, Antibo...

Claims

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