Literature DB >> 21106375

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.

Michel Gallant1, Christian Beaulieu, Carl Berthelette, John Colucci, Michael A Crackower, Chad Dalton, Danielle Denis, Yves Ducharme, Richard W Friesen, Daniel Guay, François G Gervais, Martine Hamel, Robert Houle, Connie M Krawczyk, Birgit Kosjek, Stephen Lau, Yves Leblanc, Ernest E Lee, Jean-François Levesque, Christophe Mellon, Carmela Molinaro, Wayne Mullet, Gary P O'Neill, Paul O'Shea, Nicole Sawyer, Susan Sillaots, Daniel Simard, Deborah Slipetz, Rino Stocco, Dan Sørensen, Vouy Linh Truong, Elizabeth Wong, Jin Wu, Helmi Zaghdane, Zhaoyin Wang.   

Abstract

In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences enabling the preparation of this novel class of CRTH2 antagonist are reported. Finally, the pharmacokinetic and metabolic profile of MK-7246 is disclosed.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21106375     DOI： 10.1016/j.bmcl.2010.11.015

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.

Authors:  Xianhai Huang; Jason Brubaker; Wei Zhou; Purakkattle J Biju; Li Xiao; Ning Shao; Ying Huang; Li Dong; Zhidan Liu; Rema Bitar; Alexei Buevich; Joon Jung; Scott L Peterson; John W Butcher; Joshua Close; Michelle Martinez; Rachel N MacCoss; Hongjun Zhang; Scott Crawford; Kevin D McCormick; Robert Aslanian; Ravi Nargund; Craig Correll; Francois Gervais; Hongchen Qiu; Xiaoxin Yang; Charles Garlisi; Diane Rindgen; Kevin M Maloney; Phieng Siliphaivanh; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2018-06-23       Impact factor: 4.345

2.  PET Imaging of GPR44 by Antagonist [11C]MK-7246 in Pigs.

Authors:  Pierre Cheung; Bo Zhang; Emmi Puuvuori; Sergio Estrada; Mohammad A Amin; Sofie Ye; Olle Korsgren; Luke R Odell; Jonas Eriksson; Olof Eriksson
Journal:  Biomedicines       Date:  2021-04-16

3.  UGT2B17 genetic polymorphisms dramatically affect the pharmacokinetics of MK-7246 in healthy subjects in a first-in-human study.

Authors:  Y-H Wang; M Trucksis; J J McElwee; P H Wong; C Maciolek; C D Thompson; T Prueksaritanont; G C Garrett; R Declercq; E Vets; K J Willson; R C Smith; J A Klappenbach; G J Opiteck; J A Tsou; C Gibson; T Laethem; P Panorchan; M Iwamoto; P M Shaw; J A Wagner; J C Harrelson
Journal:  Clin Pharmacol Ther       Date:  2012-06-06       Impact factor: 6.875

4.  The Industrial Age of Biocatalytic Transamination.

Authors:  Michael Fuchs; Judith E Farnberger; Wolfgang Kroutil
Journal:  European J Org Chem       Date:  2015-09-23

Review 5.  GPR44 as a Target for Imaging Pancreatic Beta-Cell Mass.

Authors:  Olof Eriksson
Journal:  Curr Diab Rep       Date:  2019-06-27       Impact factor: 4.810

Review 6.  The Current State of Beta-Cell-Mass PET Imaging for Diabetes Research and Therapies.

Authors:  Pierre Cheung; Olof Eriksson
Journal:  Biomedicines       Date:  2021-12-03
  6 in total

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