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Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases

Sandham, David and Arnold, Nicola and Aschauer, Heinrich and Bala, Kamlesh and Barker, Lucy and Brown, Lyndon and Brown, Zarin and Budd, David and Cox, Brian and Dubois, Gerald and Docx, Cerys and Duggan, Nicholas and England, Karen and Everatt, Brian and Furegati, Markus and Hall, Edward and Kalthoff, Frank and King, Anna and Leblanc, Catherine and Manini, Jodie and Meingassner, Josef and Profit, Rachael and Stringer, Rowan and Schmidt, Alfred and Simmons, Jennifer and Sohal, Bindi and Thomas, Matthew and Turner, Katharine and Walker, Christoph and Watson, Simon and Westwick, John and Willis, Jennifer and Williams, Gareth and Wilson, Caroline (2013) Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases. Bioorganic and Medicinal Chemistry.

Abstract

Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished NVP-QAV680, a highly selective compound 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.

Item Type: Article
Additional Information: Disclosure of the QAV680 compound code is approved by the QAW039 Global Project Team
Keywords: QAV680 CRTH2
Date Deposited: 26 Apr 2016 23:46
Last Modified: 26 Apr 2016 23:46
URI: https://oak.novartis.com/id/eprint/10962

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