The General Hospital Corporation

Immunogen, Inc.

Scott A Hilderbrand

Ralph Weissleder

Benjamin M Hutchins

Neal K Devaraj

Mark R Karver

Peter Panizzi

Jason R McCarthy

Daniel F Milano

Balazs R Varga

Fangwei Shao

The present invention provides methods of preparing a cell-binding agent-cytotoxic agent conjugate comprising a cell-binding agent (CysCBA) having one or more unpaired cysteine residues covalently linked to a cytotoxic agent. Also provided are conjugates prepared by the methods described herein and pharmaceutical composition and methods of use thereof.

Methods of preparing cell-binding agent-drug conjugates

The invention relates to novel methods of preparing cell-binding agent-cytotoxic agent conjugates, wherein the cytotoxic agent is an imine-containing cytotoxic agent bearing a maleimide group. In some embodiments, the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an engineered Cys, such as an engineered Cys in the heavy chain CH3 domain, at a position corresponds to the EU/OU numbering position 442 (or C442) on an antibody CBA. The invention also provides conjugates prepared by the methods of the present invention, compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.

Selective sulfonation of benzodiazepine derivatives

The present application relates to functionalized 1,2,4,5-tetrazine compounds. The compounds are useful in compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reactions for the rapid and specific covalent delivery of a 'payload' to a ligand bound to a biological target.

Functionalized 1,2,4,5-tetrazine compounds for use in bioorthogonal coupling reactions

The present invention provides methods and compositions based on optical sensor conjugates that are useful for detecting reactive oxygen, reactive nitrogen, or both species that are a direct result of inflammation caused by tissue damage.

Optical sensor conjugates for detecting reactive oxygen and/or reactive nitrogen species in vivo

This disclosure relates to trans-cyclooctene compounds and methods of using the same in bioorthogonal labeling experiments.

Cyclooctenes for bioorthogonol reactions

The present invention provides symmetric carbocyanine dyes and dye precursors useful for fluorescence microscopy, and methods of making and using same.

Monofunctional carbocyanine dyes for in vivo and in vitro imaging

The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a 'payload' to a ligand bound to a biological target.

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Swampscott, MA, United States of America

Scott A Hilderbrand