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

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.

Sandham DA; Novartis Institutes for Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom. Electronic address: david.sandham@novartis.com.

Bioorg Med Chem ; 21(21): 6582-91, 2013 Nov 01.

Article en En | MEDLINE | ID: mdl-24021582

Asunto(s)

Indolizinas/química; Receptores Inmunológicos/antagonistas & inhibidores; Receptores de Prostaglandina/antagonistas & inhibidores; Administración Oral; Animales; Células CHO; Cricetinae; Cricetulus; Dermatitis por Contacto/tratamiento farmacológico; Modelos Animales de Enfermedad; Evaluación Preclínica de Medicamentos; Eosinófilos/efectos de los fármacos; Eosinófilos/metabolismo; Semivida; Humanos; Hipersensibilidad/tratamiento farmacológico; Indolizinas/farmacocinética; Indolizinas/uso terapéutico; Ratones; Ratones Endogámicos BALB C; Unión Proteica; Ratas; Ratas Sprague-Dawley; Receptores Inmunológicos/genética; Receptores Inmunológicos/metabolismo; Receptores de Prostaglandina/genética; Receptores de Prostaglandina/metabolismo; Relación Estructura-Actividad; Células Th2/inmunología; Células Th2/metabolismo

Palabras clave

13,14-dihydro-15-keto-PGD(2); 2-tert-butylimino-2-diethylamino-1,3-dimethyl-perhydro-1,3,2-diazaphosphorine; Allergy; BAL; BEMP; CC chemokine receptor 3; CCR-3; CRTh2; CRTh2 receptor antagonist; DK-PGD(2); ELSD; FITC; GLP; PGD(2); SC; bronchoalveolar lavage; chemoattractant receptor homologous expressed on Th2 cells; evaporative light scattering detection; fluorescein isothiocyanate; good laboratory practice; prostaglandin D(2); shape change

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Receptores de Prostaglandina / Receptores Inmunológicos / Indolizinas Límite: Animals / Humans Idioma: En Año: 2013 Tipo del documento: Article

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