118089-89-7Relevant academic research and scientific papers
Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases
Sandham, David A.,Arnold, Nicola,Aschauer, Heinrich,Bala, Kamlesh,Barker, Lucy,Brown, Lyndon,Brown, Zarin,Budd, David,Cox, Brian,Docx, Cerys,Dubois, Gerald,Duggan, Nicholas,England, Karen,Everatt, Brian,Furegati, Marcus,Hall, Edward,Kalthoff, Frank,King, Anna,Leblanc, Catherine J.,Manini, Jodie,Meingassner, Josef,Profit, Rachael,Schmidt, Alfred,Simmons, Jennifer,Sohal, Bindi,Stringer, Rowan,Thomas, Matthew,Turner, Katharine L.,Walker, Christoph,Watson, Simon J.,Westwick, John,Willis, Jennifer,Williams, Gareth,Wilson, Caroline
, p. 6582 - 6591 (2013)
Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
TEAD INHIBITORS AND USES THEREOF
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Paragraph 00465; 00810, (2020/12/11)
The present invention provides compounds, compositions thereof, and methods of using the same.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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, (2008/06/13)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
A novel synthesis of deactivated benzylic triflones
Goumont, Regis,Faucher, Nicolas,Moutiers, Gilles,Tordeux, Marc,Wakselman, Claude
, p. 691 - 695 (2007/10/03)
A two-step synthesis of benzylic triflones, based on the reaction of 2.4.6-trisubstituted phenyl halides 3a-f with the anion of ethyl (trifluoromethanesulfonyl)acetate 1 followed by a decarboxylation reaction, is reported. The structural assignments are s
