1420070-69-4Relevant articles and documents
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: Lead optimization
Alonso, Juan Antonio,Andrs, Miriam,Bravo, Mnica,Calbet, Marta,Eastwood, Paul R.,Eichhorn, Peter,Esteve, Cristina,Ferrer, Manel,Gmez, Elena,Gonzlez, Jacob,Mir, Marta,Moreno, Imma,Petit, Silvia,Roberts, Richard S.,Sevilla, Sara,Vidal, Bernat,Vidal, Laura,Vilaseca, Pere,Zanuy, Miriam
, p. 5123 - 5126 (2015/01/08)
Extensive structure-activity relationship (SAR) and structure-kinetic relationship (SKR) studies in the bicyclic heteroaromatic series of CRTh2 antagonists led to the identification of several molecules that possessed both excellent binding and cellular potencies along with long receptor residence times. A small substituent in the bicyclic core provided an order of magnitude jump in dissociation half-lives. Selected optimized compounds demonstrated suitable pharmacokinetic profiles.
NEW CRTH2 ANTAGONISTS
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, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.