Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines

Christopher S Burgey; Craig M Potteiger; James Z Deng; Scott D Mosser; Christopher A Salvatore; Sean Yu; Shane Roller; Stefanie A Kane; Joseph P Vacca; Theresa M Williams

doi:10.1016/j.bmcl.2009.09.066

Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6368-72. doi: 10.1016/j.bmcl.2009.09.066. Epub 2009 Sep 22.

Authors

Christopher S Burgey¹, Craig M Potteiger, James Z Deng, Scott D Mosser, Christopher A Salvatore, Sean Yu, Shane Roller, Stefanie A Kane, Joseph P Vacca, Theresa M Williams

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_burgey@merck.com

PMID: 19818613
DOI: 10.1016/j.bmcl.2009.09.066

Abstract

Several novel spiropiperidine-based CGRP receptor antagonists have been developed that maintain good potency and have reduced potential for metabolism.

MeSH terms

Amino Acid Sequence
Animals
Calcitonin Gene-Related Peptide / chemistry
Calcitonin Gene-Related Peptide / pharmacology*
Calcitonin Gene-Related Peptide Receptor Antagonists*
Circular Dichroism
Cloning, Molecular
Humans
Molecular Sequence Data
Peptide Fragments / chemistry
Peptide Fragments / pharmacology*
Piperidines / chemistry
Piperidines / pharmacology*
Protein Binding
Signal Transduction
Spiro Compounds / chemistry
Spiro Compounds / pharmacology*
Structure-Activity Relationship

Substances

Calcitonin Gene-Related Peptide Receptor Antagonists
Peptide Fragments
Piperidines
Spiro Compounds
Calcitonin Gene-Related Peptide