☆ 4.7 Article

Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986)

JOURNAL OF MEDICINAL CHEMISTRY (2016)

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JOURNAL OF MEDICINAL CHEMISTRY

卷 59, 期 20, 页码 9457-9472

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AMER CHEMICAL SOC

DOI: 10.1021/acs.jmedchem.6b01127

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Chemistry, Medicinal

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A novel series of second generation DPP1 inhibitors free from aorta binding liabilities found for earlier compound series was discovered. This work culminated in the identification of compound 30 (AZD7986) as a highly potent, reversible, and selective clinical candidate for COPD, with predicted human PK properties suitable for once daily human dosing.

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