Onyx Therapeutics, Inc.

Amgen Inc.

Shabbir T Anik

Pasit Phiasivongsa

Ge Peng

Gary W Luehr

Kolbot By

Irina Dotsenko

Dante Romanini

The present invention provides a method of treating multiple myeloma using polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts thereof, of Formula I wherein R, R, linker, PEG, n and o are as defined herein.

Pegylated carfilzomib compounds

This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.

Prodrugs of peptide epoxy ketone protease inhibitors

The present invention provides polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts thereof, of Formula I wherein R, R, linker, PEG, n and o are as defined herein. The invention also provides methods of making and using these compounds to treat cancer, and particularly to treat hematological malignancies including multiple myeloma.

Provided herein are compounds of formula (I): which are pro-drugs of epoxy ketone protease inhibitors. The compounds disclosed herein include one or more moieties that (i) confer enhanced solubility, permeability, pharmacokinetics, and/or pharmacodynamics properties to epoxy ketone protease inhibitors, and (ii) can be released in vivo. Also provided herein are pharmaceutical compositions of the compounds of formula (I), and methods of using the compounds of formula (I) to treat diseases and conditions.

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San Francisco, CA, United States of America

Shabbir T Anik