Amgen Inc.

Sloan-kettering Institute for Cancer Research

Krishnakumar Ranganathan

Sheng Cui

Ying Chen

Richard Crockett

Kevin Crossley

Liang Huang

Sian Jones

Asher Lower

Jeroen Bezemer

Samuel J Danishefsky

Bin Wu

Zihao Hua

J David Warren

Qian Wan

Etienne Moniotte

Zhongping Tan

Cindy Kan

Yu Yuan

John D Trzupek

Gong Chen

Jiehao Chen

Karel Decroos

Yun Shi

Aleksander Swietlow

A method for preparing AMG 416, or a pharmaceutically acceptable salt thereof, is provided.

Method for preparing AMG 416 (etelcalcetide)

The instant disclosure is directed to solution phase fragment coupling methods for preparing etelcalcetide and its pharmaceutically acceptable salts.

Solution phase method for preparing etelcalcetide

A method for preparing AMG 416, or a pharmaceutically acceptable salt thereof, is provided. AMG 416 is a synthetic, eight amino-acid selective peptide agonist of the calcium sensing receptor. It is being developed as an intravenous treatment of secondary hyperparathyroidism (SHPT) in hemodialysis patients with chronic kidney disease-mineral and bone disorder (CKD-MBD).

Method for preparing AMG 416

The present invention provides isolated homogeneous polyfunctionalized proteins (e.g., erythropoietin), isolated glycopeptides, and a method for preparing polyfunctionalized peptides and/or proteins via cysteine-free native chemical ligation. In certain embodiments, the invention provides an isolated homogeneous polyfunctionalized protein having the structure (I). In certain other embodiments, the invention provides an isolated glycopeptide having Formula (II). In certain other embodiments, the inventive method is a method for preparing a polyfunctionalized peptide comprising a peptidic backbone made up of four or more amino acids, wherein two or more non-adjacent amino acids are independently substituted with a moiety having the structure (III) -LH. wherein A and L1 are as defined herein.

Compositions comprising homogeneously glycosylated erythropoietin

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Thousand Oaks, CA, United States of America

Krishnakumar Ranganathan