153435-83-7Relevant 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).
FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE
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Page/Page column 200, (2010/09/18)
The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
FUSED BICYCLIC COMPOUNDS AND USE THEREOF AS PI3K INHIBITORS
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Page/Page column 112, (2009/12/05)
The invention relates to compounds of formula (I), for the regulation of phosphoinositides 3-kinases activity and related diseases.
BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES
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Page/Page column 148, (2008/06/13)
The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non receptor kinases.
