Kezar Life Sciences

Onyx Therapeutics, Inc.

Henry Johnson

Dustin L McMinn

Sean Dalziel

David C Moebius

Simeon Bowers

Evan Lewis

Dustin Mcminn

John Walter Schnell

Jie Liu

Edward A Pomeroy

Essam Namouz

Liguo Ma

Hailing Lin

Jinlin Zhou

Xinghong Li

Ziqiang Cao

Disclosed herein are methods for preparing [(2S,3R)—N—[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound “G”): and precursors thereof.

Process of preparing a peptide epoxyketone immunoproteasome inhibitor, and precursors thereof

Provided herein is a peptide epoxyketone immunoproteasome inhibitor, crystal forms, salts, and processes for making the same, and formulations thereof.

Crystalline salts of peptide epoxyketone immunoproteasome inhibitor

Provided herein are triazacyclododecansulfonamide ('TCD')-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer. 

Triazacyclododecansulfonamide ('TCD')-based protein secretion inhibitors

Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound 'G'): and precursors thereof.

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

Tripeptide epoxy ketone protease inhibitors

Provided herein is a peptide epoxyketone immunoproteasome inhibitor having a structure: Formula (I) wherein X&#x2014; is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof. 

Disclosed herein are methods for preparing [(2S,3R)&#x2014;N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound 'G'): and precursors thereof. 

Peptide epoxyketone immunoproteasome inhibitors

Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases. 

Growing community of inventors

San Bruno, CA, United States of America

Henry Johnson