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10.1021/acsmedchemlett.7b00157

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suck abstract from ncbi


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pmid28523115
      ACS+Med+Chem+Lett 2017 ; 8 (5 ): 582-586
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  • Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP(2) Receptor Antagonist for Treatment of Asthma #MMPMID28523115
  • Sandham DA ; Barker L ; Brown L ; Brown Z ; Budd D ; Charlton SJ ; Chatterjee D ; Cox B ; Dubois G ; Duggan N ; Hall E ; Hatto J ; Maas J ; Manini J ; Profit R ; Riddy D ; Ritchie C ; Sohal B ; Shaw D ; Stringer R ; Sykes DA ; Thomas M ; Turner KL ; Watson SJ ; West R ; Willard E ; Williams G ; Willis J
  • ACS Med Chem Lett 2017[May]; 8 (5 ): 582-586 PMID28523115 show ga
  • Further optimization of an initial DP(2) 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 asthma.
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