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

Kevin Doyle, Hans Lönn, Helena Käck, Amanda Van de Poël, Steve Swallow, Philip Gardiner, Stephen Connolly, James Root, Cecilia Wikell, Göran Dahl, Kristina Stenvall, Petra Johannesson

Journal of medicinal chemistry 2016 Oct 27

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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.

Citation

Kevin Doyle, Hans Lönn, Helena Käck, Amanda Van de Poël, Steve Swallow, Philip Gardiner, Stephen Connolly, James Root, Cecilia Wikell, Göran Dahl, Kristina Stenvall, Petra Johannesson. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). Journal of medicinal chemistry. 2016 Oct 27;59(20):9457-9472