Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate

[Image: see text] The identification of potent, highly selective orally bioavailable ghrelin receptor inverse agonists from a spiro-azetidino-piperidine series is described. Examples from this series have promising in vivo pharmacokinetics and increase glucose-stimulated insulin secretion in human w...

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Main Authors: Bhattacharya, Samit K., Andrews, Kim, Beveridge, Ramsay, Cameron, Kimberly O., Chen, Chiliu, Dunn, Matthew, Fernando, Dilinie, Gao, Hua, Hepworth, David, Jackson, V. Margaret, Khot, Vishal, Kong, Jimmy, Kosa, Rachel E., Lapham, Kimberly, Loria, Paula M., Londregan, Allyn T., McClure, Kim F., Orr, Suvi T. M., Patel, Jigna, Rose, Colin, Saenz, James, Stock, Ingrid A., Storer, Gregory, VanVolkenburg, Maria, Vrieze, Derek, Wang, Guoqiang, Xiao, Jun, Zhang, Yingxin
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2014
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027753/
https://ncbi.nlm.nih.gov/pubmed/24900864
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400473x
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