1112985-96-2Relevant academic research and scientific papers
Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases
Crosignani, Stefano,Prêtre, Adeline,Jorand-Lebrun, Catherine,Fraboulet, Ga?le,Seenisamy, Jeyaprakashnarayanan,Augustine, John Kallikat,Missotten, Marc,Humbert, Yves,Cleva, Christophe,Abla, Nada,Daff, Hamina,Schott, Olivier,Schneider, Manfred,Burgat-Charvillon, Fabienne,Rivron, Delphine,Hamernig, Ingrid,Arrighi, Jean-Fran?ois,Gaudet, Marilène,Zimmerli, Simone C.,Juillard, Pierre,Johnson, Zoe
, p. 7299 - 7317 (2011/12/15)
New phenoxyacetic acid antagonists of CRTH2 are described. Following the discovery of a hit compound by a focused screening, high protein binding was identified as its main weakness. Optimization aimed at reducing serum protein binding led to the identification of several compounds that showed not only excellent affinities for the receptor (41 compounds with Ki 50 100 nM; PGD2-induced eosinophil shape change). Additional optimization of the PK characteristics led to the identification of several compounds suitable for in vivo testing. Of these, 19k and 19s were tested in two different pharmacological models (acute FITC-mediated contact hypersensitivity and ovalbumin-induced eosinophilia models) and found to be active after oral dosing (10 and 30 mg/kg).
Quinazoline Compounds
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Page/Page column 41, (2010/12/26)
Disclosed are quinazoline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): in which R1, R2, R3, R4, R5, R6, R7,
PHENOXY ACETIC ACID DERIVATIVES
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Page/Page column 60-61, (2010/09/03)
The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE
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Page/Page column 196, (2010/09/18)
The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
POLAR QUINAZOLINES AS LIVER X RECEPTORS ( LXRS ) MODULATORS
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Page/Page column 65-66, (2010/07/10)
Disclosed are polar quinazoline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): INSERT FORMULA HERE AS IT APPEARS IN WRITTEN FORM IN THE SPECIFICATION (I) in which, R1, R2, R3, R4, R5, R6,
FUSED BICYCLIC COMPOUNDS AND USE THEREOF AS PI3K INHIBITORS
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, (2009/12/05)
The invention relates to compounds of formula (I), for the regulation of phosphoinositides 3-kinases activity and related diseases.
