title: Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
abstract: Several novel spiropiperidine-based CGRP receptor antagonists have been developed that maintain good potency and have reduced potential for metabolism.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_burgey@merck.com
authors.forename: Christopher S
authors.initials: CS
authors.lastname: Burgey
authors.forename: Craig M
authors.initials: CM
authors.lastname: Potteiger
authors.forename: James Z
authors.initials: JZ
authors.lastname: Deng
authors.forename: Scott D
authors.initials: SD
authors.lastname: Mosser
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Salvatore
authors.forename: Sean
authors.initials: S
authors.lastname: Yu
authors.forename: Shane
authors.initials: S
authors.lastname: Roller
authors.forename: Stefanie A
authors.initials: SA
authors.lastname: Kane
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Vacca
authors.forename: Theresa M
authors.initials: TM
authors.lastname: Williams
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D015740:Calcitonin Gene-Related Peptide / Q000737:chemistry / Q000494:pharmacology*; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D002942:Circular Dichroism; D003001:Cloning, Molecular; D006801:Humans; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D011485:Protein Binding; D015398:Signal Transduction; D013141:Spiro Compounds / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D010446:Peptide Fragments; D010880:Piperidines; D013141:Spiro Compounds; D015740:Calcitonin Gene-Related Peptide