Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP 2 Receptor Antagonist for Treatment of Asthma

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP 2 Receptor Antagonist for Treatment of Asthma

Further optimization of an initial DP receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1 -pyrrolo[2,3- ]pyridin-3-yl)acetic acid (compound , NVP-QAW039, fevipiprant), which exhibits improved po...

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Veröffentlicht in:ACS medicinal chemistry letters 2017-05, Vol.8 (5), p.582-586
Hauptverfasser: Sandham, David A, Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Charlton, Steven J, Chatterjee, Devnandan, Cox, Brian, Dubois, Gerald, Duggan, Nicholas, Hall, Edward, Hatto, Julia, Maas, Janet, Manini, Jodie, Profit, Rachael, Riddy, Darren, Ritchie, Catherine, Sohal, Bindi, Shaw, Duncan, Stringer, Rowan, Sykes, David A, Thomas, Matthew, Turner, Katharine L, Watson, Simon J, West, Ryan, Willard, Elisabeth, Williams, Gareth, Willis, Jennifer
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Sprache:eng
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Zusammenfassung:Further optimization of an initial DP receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1 -pyrrolo[2,3- ]pyridin-3-yl)acetic acid (compound , NVP-QAW039, fevipiprant), which exhibits improved potency on human eosinophils and Th2 cells, together with a longer receptor residence time, and is currently in clinical trials for severe asthma.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.7b00157