Literature DB >> 19804971

Discovery and optimization of CRTH2 and DP dual antagonists.

Jiwen Liu1, Zice Fu, Yingcai Wang, Mike Schmitt, Alan Huang, Derek Marshall, George Tonn, Lisa Seitz, Tim Sullivan, H Lucy Tang, Tassie Collins, Julio Medina.   

Abstract

A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles in mediating responses of asthma and other immune diseases, this series was optimized to increase the dual antagonistic activities and improve pharmacokinetic properties. These efforts led to selection of AMG 009 as a clinical candidate.

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Year:  2009        PMID: 19804971     DOI: 10.1016/j.bmcl.2009.09.052

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


  4 in total

1.  Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.

Authors:  Jiwen Liu; An-Rong Li; Yingcai Wang; Mike G Johnson; Yongli Su; Wang Shen; Xuemei Wang; Sarah Lively; Matthew Brown; SuJen Lai; Felix Gonzalez Lopez De Turiso; Qingge Xu; Bettina Van Lengerich; Mike Schmitt; Zice Fu; Ying Sun; Shanna Lawlis; Lisa Seitz; Jay Danao; Jill Wait; Qiuping Ye; Hua Lucy Tang; Mark Grillo; Tassie L Collins; Timothy J Sullivan; Julio C Medina
Journal:  ACS Med Chem Lett       Date:  2011-03-02       Impact factor: 4.345

2.  Benzodiazepinone Derivatives as CRTH2 Antagonists.

Authors:  Jiwen Jim Liu; Alan C Cheng; H Lucy Tang; Julio C Medina
Journal:  ACS Med Chem Lett       Date:  2011-04-17       Impact factor: 4.345

3.  Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.

Authors:  Stefano Crosignani; Catherine Jorand-Lebrun; Gordon Campbell; Adeline Prêtre; Tania Grippi-Vallotton; Anna Quattropani; Gwenaelle Bouscary-Desforges; Agnes Bombrun; Marc Missotten; Yves Humbert; Christèle Frémaux; Mikaël Pâquet; Kamel El Harkani; Charles G Bradshaw; Christophe Cleva; Nada Abla; Hamina Daff; Olivier Schott; Pierre-André Pittet; Jean-François Arrighi; Marilène Gaudet; Zoë Johnson
Journal:  ACS Med Chem Lett       Date:  2011-10-10       Impact factor: 4.345

4.  Methyl 2-(4-chloro-3,5-dinitro-benz-amido)-acetate.

Authors:  Xiang-Xiang Wu; Xue-Fen Wu; Yi-Min Hou; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-11-30
  4 in total

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