Pharmacia & Upjohn Company

Onyx Therapeutics, Inc.

Amgen Inc.

Pfizer Corporation

Altos Therapeutics, LLC

Other

Millennium Pharmaceuticals Limited

Gary W Luehr

Mikhail Fedorovich Gordeev

Dinesh Vinoobhai Patel

Pasit Phiasivongsa

Ge Peng

Shabbir T Anik

Adam Renslo

Kolbot By

Eric M Gordon

Michael R Barbachyn

Richard Charles Thomas

Zhi-Jie Ni

Toni-Jo Poel

Irina Dotsenko

Upinder Singh

Dante Romanini

Pascal Jean Druzgala

Robert C Gadwood

Vara Prasad Venkata Nagendra Josyula

Priyadarshini Jaishankar

Philip W Payne

Arathi Sundaram

Neil E Westlund

Stuart Lam

Mikhail Fedor Gordeev

Vara Prasad Venkata Negandra Josyula

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.

Provided are Dor Dantagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R, Rand Rare as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine Dor Dreceptor from the compounds of the invention.

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The present invention provides antibacterial agents having the formulae I, II, and III described herein.

N-aryl-2-oxazolidinone-5-carboxamides and their derivatives

The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein Ris Calkyl, optionally substituted with a fluoro atom, or Ris a cyclopropyl or cyclopropylmethyl; and Ris methyl or ethyl. These compounds are useful as antibacterial agents.

7-Fluoro-1,3-dihydro-indol-2-one oxazolidinones as antibacterial agents

The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein Y is &#x2014;S(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;NR)&#x2014;, or &#x2014;S(&#x2550;NR)(&#x2550;O)&#x2014;; Z is &#x2014;NHC(&#x2550;O)R, &#x2014;NHC(&#x2550;S)R, &#x2014;NH-het, &#x2014;O-het, &#x2014;S-het, or -het. The compounds of formula I are useful as antibacterial agents.

Antimicrobial dihydrothiazine and dihydrothiopyran oxazolidinones

Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

Oxazolidinone combinatorial libraries, compositions and methods of preparation

N-Aryl-2-oxazolidinone-5-carboxamides and their derivatives

Growing community of inventors

Fremont, CA, United States of America

Gary W Luehr