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

Sandham, David and Barker, Lucy and Brown, Lyndon and Brown, Zarin and Budd, David and Charlton, Steven and Chatterjee, Devnandan and Cox, Brian and Dubois, Gerald and Duggan, Nicholas and Hall, Edward and Hatto, Julia and Maas, David and Manini, Jodie and Profit, Rachael and Riddy, Darren and Ritchie, Cathy and Sohal, Bindi and Shaw, Duncan and Stringer, Rowan and Sykes, David and Turner, Katharine and Watson, Simon and West, Ryan and Willard, Elizabeth and 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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