Potent conjugates and hydrophilic linkers

A technology of conjugates and compounds, applied in the field of hydrophilic linkers and preparation of maytansinoids, which can solve the problems of low yield of final conjugates, heterogeneity of conjugates, expensive and other problems
CN102596922AInactive Publication Date: 2012-07-18IMMUNOGEN INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
IMMUNOGEN INC
Publication Date
2012-07-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.
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Description

[0001] This application is a continuation-in-part of US Formal Application No. 12 / 433,668, filed April 30, 2009, which claims priority to US Provisional Application No. 61 / 049,289, filed April 30, 2008. The entire disclosures of the prior applications (Application Nos. 12 / 433,668 and 61 / 049,289) are considered part of the disclosure of the appended continuation applications and are hereby incorporated by reference. field of invention

[0002] The present invention relates to novel linkers that link a drug (eg, a cytotoxic agent) to a cell-binding agent (eg, an antibody) in such a way that the linker contributes to increasing the activity of the drug. In particular, the present invention relates to the use of novel hydrophilic linkers, wherein such linkers increase the potency or potency of cell-binding agent-drug conjugates several-fold in various cancer cell types that Cell types include cancer cells that express low numbers of antigens on the cell surface or cancers that are...

Claims

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