Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist

[Image: see text] Incorporation of polar functionality into a series of highly potent calcitonin gene-related peptide (CGRP) receptor antagonists was explored in an effort to improve pharmacokinetics. This strategy identified piperazinone analogues that possessed improved solubility at acidic pH and...

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Hauptverfasser: Bell, Ian M., Gallicchio, Steven N., Wood, Michael R., Quigley, Amy G., Stump, Craig A., Zartman, C. Blair, Fay, John F., Li, Chi-Chung, Lynch, Joseph J., Moore, Eric L., Mosser, Scott D., Prueksaritanont, Thomayant, Regan, Christopher P., Roller, Shane, Salvatore, Christopher A., Kane, Stefanie A., Vacca, Joseph P., Selnick, Harold G.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2010
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4007836/
https://ncbi.nlm.nih.gov/pubmed/24900170
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml900016y
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