Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma
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
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)
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists
Monocyclic and bicyclic ring systems were investigated as the "core" section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists. A range of potencies were observed and single-digit nanomolar potencies were obtained in both the monocyclic and bicyclic cores. Residence times for the monocyclic compounds were very short. Some of the bicyclic cores displayed better residence times. A methyl group in the northern part of the core, between the head and tail was a necessary requirement for the beginnings of long residence times. Variations of the tail substitution maximised potencies and residence times.
Buil, Maria Antonia,Calbet, Marta,Castillo, Marcos,Castro, Jordi,Esteve, Cristina,Ferrer, Manel,Forns, Pilar,González, Jacob,López, Sara,Roberts, Richard S.,Sevilla, Sara,Vidal, Bernat,Vidal, Laura,Vilaseca, Pere
p. 102 - 133
(2016/03/04)
Highly functionalized 7-azaindoles as selective PPARγ modulators
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.
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)
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