Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
Several novel spiropiperidine-based CGRP receptor antagonists have been developed that maintain good potency and have reduced potential for metabolism.
Burgey
Christopher S
CS
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_burgey@merck.com
Potteiger
Craig M
CM
Deng
James Z
JZ
Mosser
Scott D
SD
Salvatore
Christopher A
CA
Yu
Sean
S
Roller
Shane
S
Kane
Stefanie A
SA
Vacca
Joseph P
JP
Williams
Theresa M
TM
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
D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D010446:Peptide Fragments; D010880:Piperidines; D013141:Spiro Compounds; D015740:Calcitonin Gene-Related Peptide