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