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

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 21, 2013, Pages 6582-6591

  Sandham, David A ^a   Arnold, Nicola ^a   Aschauer, Heinrich ^b   Bala, Kamlesh ^a   Barker, Lucy ^a   Brown, Lyndon ^a   Brown, Zarin ^a   Budd, David ^a   Cox, Brian ^a   Docx, Cerys ^a   Dubois, Gerald ^a   Duggan, Nicholas ^a   England, Karen ^a   Everatt, Brian ^a   Furegati, Marcus ^c   Hall, Edward ^a   Kalthoff, Frank ^b   King, Anna ^a   Leblanc, Catherine J ^c   Manini, Jodie ^a   Meingassner, Josef ^b   Profit, Rachael ^a   Schmidt, Alfred ^c   Simmons, Jennifer ^a   Sohal, Bindi ^a   Stringer, Rowan ^a   Thomas, Matthew ^a   Turner, Katharine L ^a   Walker, Christoph ^a   Watson, Simon J ^a   Westwick, John ^a   Willis, Jennifer ^a   Williams, Gareth ^a   Wilson, Caroline ^a   more..

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b Novartis Institutes for BioMedical Research Vienna   (Austria)

^c NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Allergy; CRTh2 receptor antagonist

Indexed keywords

7 AZAINDOLE 3 ACETIC ACID; ACETIC ACID DERIVATIVE; INTERLEUKIN 13; INTERLEUKIN 5; MACROGOL 200; NEW DRUG; NVP QAV 680; PHOSPHATE BUFFERED SALINE; PROSTAGLANDIN D2; PROSTAGLANDIN D2 RECEPTOR BLOCKING AGENT; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ALLERGIC ASTHMA; ALLERGIC DISEASE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL INFILTRATION; CONTROLLED STUDY; CYTOKINE PRODUCTION; CYTOKINE RELEASE; DRUG ADMINISTRATION ROUTE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; EOSINOPHIL; EXPERIMENTAL RAT; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; LOEFFLER PNEUMONIA; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PROCESS OPTIMIZATION; RAT; SKIN ALLERGY; STRUCTURE ACTIVITY RELATION; T LYMPHOCYTE ACTIVATION; TH2 CELL; TIME TO MAXIMUM PLASMA CONCENTRATION;

RATTUS; RODENTIA;

2-TERT-BUTYLIMINO-2-DIETHYLAMINO-1,3-DIMETHYL-PERHYDRO-1,3,2-DIAZAPHOSPHORINE; 13,14-DIHYDRO-15-KETO-PGD(2); ALLERGY; BAL; BEMP; BRONCHOALVEOLAR LAVAGE; CC CHEMOKINE RECEPTOR 3; CCR-3; CHEMOATTRACTANT RECEPTOR HOMOLOGOUS EXPRESSED ON TH2 CELLS; CRTH2; CRTH2 RECEPTOR ANTAGONIST; DK-PGD(2); ELSD; EVAPORATIVE LIGHT SCATTERING DETECTION; FITC; FLUORESCEIN ISOTHIOCYANATE; GLP; GOOD LABORATORY PRACTICE; PGD(2); PROSTAGLANDIN D(2); SC; SHAPE CHANGE;

ADMINISTRATION, ORAL; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DERMATITIS, CONTACT; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; EOSINOPHILS; HALF-LIFE; HUMANS; HYPERSENSITIVITY; INDOLIZINES; MICE; MICE, INBRED BALB C; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, IMMUNOLOGIC; RECEPTORS, PROSTAGLANDIN; STRUCTURE-ACTIVITY RELATIONSHIP; TH2 CELLS;

EID: 84885185747     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.08.025     Document Type: Article

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