Regeneron Pharmaceuticals, Inc.

Celgene Corporation

Polytherics Limited

Nareshkumar Jain

Thomas Nittoli

Thomas P Markotan

Sanjeevani Ghone

John Fitzgerald Traverse

Fu-An Kang

Sean Wesley Smith

Ian Glassford

Sylvia J Degrado

Srinath Thirumalairajan

Senzhi Zhao

Srinath Thirumalai Rajan

A scaled process of preparing maytansinol, FORMULA II, is provided by reacting a compound of Formula I, wherein R is selected from the group consisting essentially of alkyl, branched alkyl, aryl, alkenyl, alkynyl, as well as substituted variations thereof, with at least one organometallic reagent to produce the compound of Formula II; and, isolating the compound of Formula II.

Preparation of maytansinol

The disclosure relates to compositions comprising diastereomer of a macrolide exhibiting improved therapeutic profile in the context of inhibiting cell proliferation compared to the corresponding compositions comprising mixture of diastereomers. The disclosure further provides drug-ligand conjugates formed using diastereomer of the macrolide. The disclosure also provides novel method of preparation of diastereomer of the macrolide and their therapeutic uses.

Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses

Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.

Cytotoxic agents and conjugates thereof

Provided herein are compounds useful for appending amino acids to nucleophiles.

Amino acid acylation reagents and methods of using the same

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Ringoes, NJ, United States of America

Nareshkumar Jain