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Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Doyle, Kevin; Lönn, Hans; Käck, Helena; Van de Poël, Amanda; Swallow, Steve; Gardiner, Philip; Connolly, Stephen; Root, James; Wikell, Cecilia; Dahl, Göran; Stenvall, Kristina; Johannesson, Petra.
Afiliación
  • Doyle K; Discovery, Charles River , Chesterford Research Park, Saffron Walden, Essex CB10 1XL, U.K.
  • Lönn H; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Käck H; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Van de Poël A; Discovery, Charles River , Chesterford Research Park, Saffron Walden, Essex CB10 1XL, U.K.
  • Swallow S; AstraZeneca Alderley Park , Macclesfield, Cheshire SK10 4TG, U.K.
  • Gardiner P; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Connolly S; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Root J; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Wikell C; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Dahl G; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Stenvall K; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
  • Johannesson P; AstraZeneca Gothenburg , Pepparedsleden 1, Mölndal 431 83, Sweden.
J Med Chem ; 59(20): 9457-9472, 2016 Oct 27.
Article en En | MEDLINE | ID: mdl-27690432
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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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxazepinas / Inhibidores de Proteasas / Benzoxazoles / Catepsina C / Descubrimiento de Drogas Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Estados Unidos
Buscar en Google
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxazepinas / Inhibidores de Proteasas / Benzoxazoles / Catepsina C / Descubrimiento de Drogas Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Estados Unidos