1255099-47-8Relevant articles and documents
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,Budd, David,Charlton, Steven J.,Chatterjee, Devnandan,Cox, Brian,Dubois, Gerald,Duggan, Nicholas,Hall, Edward,Hatto, Julia,Maas, Janet,Manini, Jodie,Profit, Rachael,Riddy, Darren,Ritchie, Catherine,Sohal, Bindi,Shaw, Duncan,Stringer, Rowan,Sykes, David A.,Thomas, Matthew,Turner, Katharine L.,Watson, Simon J.,West, Ryan,Willard, Elisabeth,Williams, Gareth,Willis, Jennifer
, p. 582 - 586 (2017/05/17)
Further optimization of an initial DP2 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 (compou
Highly functionalized 7-azaindoles as selective PPARγ modulators
Debenham, Sheryl D.,Chan, Audrey,Lau, Fiona WaiYu,Liu, Weiguo,Wood, Harold B.,Lemme, Karen,Colwell, Lawrence,Habulihaz, Bahanu,Akiyama, Taro E.,Einstein, Monica,Doebber, Thomas W.,Sharma, Neelam,Wang, Chaunlin F.,Wu, Margaret,Berger, Joel P.,Meinke, Peter T.
supporting information; experimental part, p. 4798 - 4801 (2009/06/17)
A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARγ modulators (SPPARγMs). Addition of substituents at the 6-position of the 7-azaindoles improves in vitro potency and pharmacokinetics. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series.