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Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma

Sandham, David A.; Barker, Lucy; Brown, Lyndon; Brown, Zarin; Charlton, Steven J.; Budd, David; Chatterjee, Devnanden; Cox, Brian; Dubois, Gerald; Hall, Edward; Duggan, Nicholas; Hatto, Julia; Maas, Janet; Manini, Jodie; Profit, Rachael; Riddy, Darren; Ritchie, Catherine; Shaw, Duncan; Sohal, Bindi; Sykes, David A.; Stringer, Rowan; Thomas, Matthew; Turner, Katherine L.; Watson, Simon J.; West, Ryan; Willard, Elisabeth; Williams, Gareth; Willis, Jennifer

Authors

David A. Sandham

Lucy Barker

Lyndon Brown

Zarin Brown

Steven J. Charlton

David Budd

Devnanden Chatterjee

Brian Cox

Gerald Dubois

Edward Hall

Nicholas Duggan

Julia Hatto

Janet Maas

Jodie Manini

Rachael Profit

Darren Riddy

Catherine Ritchie

Duncan Shaw

Bindi Sohal

David A. Sykes

Rowan Stringer

Matthew Thomas

Katherine L. Turner

Simon J. Watson

Ryan West

Elisabeth Willard

Gareth Williams

Jennifer Willis



Abstract

Further optimization of an initial DP2 receptor antagonist clinical candidate NVPQAV680 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 asthma.

Journal Article Type Article
Publication Date May 11, 2017
Journal ACS Medicinal Chemistry Letters
Print ISSN 1948-5875
Electronic ISSN 1948-5875
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 8
Issue 5
Pages 582-586
APA6 Citation Turner, K. L., Chatterjee, D., Sandham, D. A., Barker, L., Brown, L., Brown, Z., …Willis, J. (2017). Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma. ACS Medicinal Chemistry Letters, 8(5), 582-586. https://doi.org/10.1021/acsmedchemlett.7b00157
DOI https://doi.org/10.1021/acsmedchemlett.7b00157
Keywords DP2 receptor antagonist, severe asthma, clinical candidate
Publisher URL http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.7b00157
Copyright Statement Copyright information regarding this work can be found at the following address: http://eprints.nottingh.../end_user_agreement.pdf
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