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Challenges in the development of an M(4) PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides

Herein we describe the continued optimization of M(4) positive allosteric modulators (PAMs) within the 5-amino-thieno[2,3-c]pyridazine series of compounds. In this letter, we disclose our studies on tertiary amides derived from substituted azetidines. This series provided excellent CNS penetration,...

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發表在:Bioorg Med Chem Lett
Main Authors: Tarr, James C., Wood, Michael R., Noetzel, Meredith J., Melancon, Bruce J., Lamsal, Atin, Luscombe, Vincent B., Rodriguez, Alice L., Byers, Frank W., Chang, Sichen, Cho, Hyekyung P., Engers, Darren W., Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
格式: Artigo
語言:Inglês
出版: 2017
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在線閱讀:https://ncbi.nlm.nih.gov/pmc/articles/PMC6542369/
https://ncbi.nlm.nih.gov/pubmed/29089231
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.10.053
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