Discovery of AZD3199, An Inhaled Ultralong Acting ?2 Receptor Agonist with Rapid Onset of Action

Stocks, Michael; Alcaraz, Lilian; Bailey, Andrew; Bonnert, Roger; Cadogan, Elaine; Christie, Jadeen; Dixon, John; Connolly, Stephen; Cook, Anthony; Fisher, Adrian; Flaherty, Alice; Humphries, Alexander; Ingall, Anthony; Jordan, Stephen; Lawson, Mandy; Mullen, Alex; Nicholls, David; Paine, Stuart; Pairaudeau, Garry; Young, Alan

doi:10.1021/ml4005232

All Outputs (3)

Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate (2014)
Journal Article
Schwehm, C., Lewis, W., Blake, A. J., Kellam, B., & Stocks, M. J. (2014). Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate. Acta Crystallographica Section C: Structural Chemistry, 70(12), 1161-1168. https://doi.org/10.1107/s205322961402436x

Bicycle ring closure on a mixture of (4aS,8aR)- and (4aR,8aS)-ethyl 2-oxodecahydro-1,6-naphthyridine-6-carboxylate, followed by conversion of the separated cis and trans isomers to the corresponding thioamide derivatives, gave (4aSR,8aRS)-ethyl 2-sul... Read More about Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate.

Chiral Phosphoric Acid-Catalyzed Enantioselective Three- Component Aza-Diels-Alder Reactions of Aminopyrroles and Aminopyrazoles (2014)
Journal Article
Brioche, J., Stocks, M., Courant, T., Alcaraz, L., Furber, M., Zhu, J., & Masson, G. (2014). Chiral Phosphoric Acid-Catalyzed Enantioselective Three- Component Aza-Diels-Alder Reactions of Aminopyrroles and Aminopyrazoles. Advanced Synthesis and Catalysis, 356(8), 1719-1724. https://doi.org/10.1002/adsc.201400093

Discovery of AZD3199, An Inhaled Ultralong Acting ?2 Receptor Agonist with Rapid Onset of Action (2014)
Journal Article
Stocks, M., Alcaraz, L., Bailey, A., Bonnert, R., Cadogan, E., Christie, J., …Young, A. (2014). Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action. ACS Medicinal Chemistry Letters, 5(4), 416-421. https://doi.org/10.1021/ml4005232

A series of dibasic des-hydroxy ?2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human ?-adrenoreceptors demonstrated a series of highly potent and se... Read More about Discovery of AZD3199, An Inhaled Ultralong Acting ?2 Receptor Agonist with Rapid Onset of Action.