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Discovery of Fevipiprant (NVP-QAW039), a potent and selective CRTh2 receptor antagonist for treatment of allergic diseases

Sandham, David, Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Charlton, Steven, Chatterjee, Devnandan, Cox, Brian, Dubois, Gerald, Duggan, Nicholas, Hall, Edward, Hatto, Julia, Maas, David, Manini, Jodie, Profit, Rachael, Riddy, Darren, Ritchie, Cathy, Sohal, Bindi, Shaw, Duncan, Stringer, Rowan, Sykes, David, Turner, Katharine, Watson, Simon, West, Ryan, Willard, Elizabeth, Williams, Gareth and Willis, Jennifer (2017) Discovery of Fevipiprant (NVP-QAW039), a potent and selective CRTh2 receptor antagonist for treatment of allergic diseases. ACS Medicinal Chemistry Letters.

Abstract

Further optimization of an initial CRTh2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compound 11, 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 eosinophilic asthma and atopic dermatitis.

Item Type: Article
Date Deposited: 30 May 2017 00:45
Last Modified: 30 May 2017 00:45
URI: https://oak.novartis.com/id/eprint/30505

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