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J Med Chem. 2016 Oct 27;59(20):9457-9472. Epub 2016 Oct 11.

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

Author information

1
Discovery, Charles River , Chesterford Research Park, Saffron Walden, Essex CB10 1XL, U.K.
2
AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
3
AstraZeneca Alderley Park , Macclesfield, Cheshire SK10 4TG, U.K.

Abstract

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.

PMID:
27690432
DOI:
10.1021/acs.jmedchem.6b01127
[Indexed for MEDLINE]

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