Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases

Journal of Medicinal Chemistry

Volumn 54, Issue 20, 2011, Pages 7299-7317

  Crosignani, Stefano ^a   Prêtre, Adeline ^a   Jorand Lebrun, Catherine ^a   Fraboulet, Gaële ^a   Seenisamy, Jeyaprakashnarayanan ^b   Augustine, John Kallikat ^b   Missotten, Marc ^a   Humbert, Yves ^a   Cleva, Christophe ^a   Abla, Nada ^a   Daff, Hamina ^a   Schott, Olivier ^a   Schneider, Manfred ^a   Burgat Charvillon, Fabienne ^a   Rivron, Delphine ^a   Hamernig, Ingrid ^a   Arrighi, Jean François ^a   Gaudet, Marilène ^a   Zimmerli, Simone C ^a   Juillard, Pierre ^a   Johnson, Zoe ^a   more..

^a MERCK SERONO S A   (Switzerland)

^b SYNGENE INTERNATIONAL LTD   (India)

Author keywords

[No Author keywords available]

Indexed keywords

[4 CHLORO 2 (PYRIDIN 3 YLETHYNYL)PHENOXY]ACETIC ACID; [4 CHLORO 2 [(3 CHLOROPHENYL)ETHYNYL]PHENOXY]ACETIC ACID; [4 CHLORO 2 [(5,5 DIOXIDODIBENZO[B,D]THIEN 3 YL)ETHYNYL]ACETIC ACID; [4 CHLORO 2 [[2 FLUORO 5 (PROPYLSULFONYL)PHENYL]ETHYNYL]PHENOXY]ACETIC ACID; [4 CHLORO 2 [[2 METHYL 5 (PROPYLSULFONYL)PHENYL]ETHYNYL]PHENOXY]ACETIC ACID; [4 CHLORO 2 [[3 (PROPYLSULFONYL)PHENYL]ETHYNYL]PHENOXY]ACETIC ACID; [4 CHLORO 2 [[5 [(DIMETHYLAMINO)SULFONYL] 2 FLUOROPHENYL]ETHYNYL]ACETIC ACID; ANTIALLERGIC AGENT; ANTIINFLAMMATORY AGENT; CHEMOATTRACTANT RECEPTOR HOMOLOGOUS EXPRESSED ON TH2 LYMPHOCYTE BLOCKING AGENT; DEXAMETHASONE; OVALBUMIN; PHENOXYACETIC ACID DERIVATIVE; PROSTAGLANDIN D2; PROSTAGLANDIN INHIBITOR; TERT BUTYL(4 CHLORO 2 ETHYNYLPHENOXY)ACETIC ACID; TERT BUTYL[4 CHLORO 2 [(TRIMETHYLSILYL)ETHYNYL]PHENOXY]ACETIC ACID; UNCLASSIFIED DRUG;

ALLERGIC DISEASE; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; CELL SHAPE; CONTACT ALLERGY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STABILITY; DRUG SYNTHESIS; EOSINOPHIL; FEMALE; HUMAN; HUMAN CELL; IC 50; INFLAMMATORY DISEASE; LIVER MICROSOME METABOLISM; LOEFFLER PNEUMONIA; MOUSE; NONHUMAN; PLASMA PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION;

ACETIC ACIDS; ADMINISTRATION, ORAL; ALKYNES; ANIMALS; ANTI-ALLERGIC AGENTS; ANTI-INFLAMMATORY AGENTS; BINDING, COMPETITIVE; BLOOD PROTEINS; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; CELL SHAPE; CHEMOTAXIS, LEUKOCYTE; DERMATITIS, CONTACT; EOSINOPHILS; FEMALE; HEK293 CELLS; HUMANS; MICE; MICE, INBRED BALB C; MICROSOMES, LIVER; OVALBUMIN; PROTEIN BINDING; PULMONARY EOSINOPHILIA; RADIOLIGAND ASSAY; RATS; RECEPTORS, IMMUNOLOGIC; RECEPTORS, PROSTAGLANDIN; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES;

EID: 80054959577     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200866y     Document Type: Article

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