Immunogen, Inc.

Wayne Charles Widdison

Ravi V J Chari

Robert Yongxin Zhao

Yelena V Kovtun

Rajeeva Singh

Ravi Vankeepuram Jagannatha Chari

Michael Louis Miller

Wei Li

Ravi Chari

Viktor S Goldmakher

Robert J Lutz

Rita M Steeves

John M Lambert

Graham S Byng

Hans K Erickson

Sharon D Wilhelm

David P Pleynet

Cynthia Kuo

Rita Steeves

Walter Blaettler

Yelena Kovtun

Ravi Vankeepuram Chari

Ravi Vj Chari

Ravi VJ Chari

The invention relates to novel cell-binding agent-maytansinoid conjugate having a self-immolative peptide linker and more specifically to conjugates of formula (I). The invention also provides novel maytansinoid compounds of formula (II), (III), (IV) or (V). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Maytansinoid derivatives with self-immolative peptide linkers and conjugates thereof

Disclosed herein are novel cytotoxic compounds, and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this disclosure relates to novel camptothecin derivatives thereof, intermediates thereof, conjugates thereof, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents (anticancer agents).

Camptothecin derivatives

Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

Cross-linkers and their uses

Disclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence of a drying agent. Also disclosed is an improved method of preparing an amino acid ester of maytansinol in which a nucleophile is added to the reaction mixture after completion of the reaction between maytansinol and an N-carboxyanhydride of an amino acid.

Methods for the acylation of maytansinol

The invention relates to novel cell-binding agent-cytotoxic agent conjugate having a peptide linkers and more specifically to conjugates of formula (I). The invention also provides novel cytotoxic agents of formula (II), linker compounds represented by formula (III), and drug-linker compounds represented by formula (IV). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Maytansinoid derivatives with peptide linker and conjugates thereof

The invention provides linker compounds containing a disulfide group, and maytansin-derived cytotoxic compounds that are useful for forming a CBA-drug conjugates, and conjugates so formed. Such conjugates and/or cytotoxic compounds may be effective for treating a range of diseases, such as cancer, with a relatively high activity at a relatively low, non-toxic dose.

Conjugates comprising cell-binding agents and maytansinoids as cytotoxic agents

The invention provides linker compounds and cytotoxic compounds that are useful for forming a CBA-drug conjugates; and conjugates so formed. Such conjugates and/or cytotoxic compounds may be effective for treating a range of diseases, such as cancer, with a relatively high activity at a relatively low, non-toxic dose.

Conjugates comprising cell-binding agents and cytotoxic agents

The present invention is directed to a method of separating a monocarboxylic represented by the following structural formula: (I) from a dicarboxylic acid represented by the following structural formula: (II) using silica chromatography. 

Purification of intermediates used in the preparation of heterobifunctional linkers

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Belmont, MA, United States of America

Wayne Charles Widdison