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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 |
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Main Authors: | , , , , , , , , , , , , , , , , , , |
格式: | Artigo |
語言: | Inglês |
出版: |
2017
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主題: | |
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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