Celia Dominguez

Summary

Affiliation: Amgen Inc
Country: USA

Publications

  1. ncbi request reprint p38 MAP kinase inhibitors: many are made, but few are chosen
    Celia Dominguez
    Amgen Inc, Chemistry Research and Discovery, Medicinal Chemistry, One Amgen Center Drive, MS 29 1 B, Thousand Oaks, CA 91320 179, USA
    Curr Opin Drug Discov Devel 8:421-30. 2005
  2. doi request reprint Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)
    Longbin Liu
    Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 51:3688-91. 2008
  3. doi request reprint Design, synthesis, and biological evaluation of potent c-Met inhibitors
    Noel D D'Angelo
    Department of Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320 1799, USA
    J Med Chem 51:5766-79. 2008
  4. doi request reprint Azole-based inhibitors of AKT/PKB for the treatment of cancer
    QingPing Zeng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
    Bioorg Med Chem Lett 20:1559-64. 2010
  5. ncbi request reprint Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties
    Hui Ling Wang
    Department of Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320 1799, USA
    J Med Chem 50:3528-39. 2007
  6. doi request reprint Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives
    Mark H Norman
    Department of Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 55:1858-67. 2012
  7. doi request reprint Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series
    Longbin Liu
    Department of Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 55:1868-97. 2012
  8. ncbi request reprint High-content screening analysis of the p38 pathway: profiling of structurally related p38alpha kinase inhibitors using cell-based assays
    Sandra Ross
    Amgen Inc, Thousand Oaks, CA 91320 1799, USA
    Assay Drug Dev Technol 4:397-409. 2006
  9. ncbi request reprint A soluble base for the copper-catalyzed imidazole N-arylations with aryl halides
    Longbin Liu
    Chemical Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Org Chem 70:10135-8. 2005
  10. ncbi request reprint MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein
    Matthew R Lee
    Department of Molecular Structure, Amgen Inc One Amgen Center Drive Thousand Oaks, CA 91320 1799, USA
    Curr Med Chem 12:2979-94. 2005

Collaborators

Detail Information

Publications16

  1. ncbi request reprint p38 MAP kinase inhibitors: many are made, but few are chosen
    Celia Dominguez
    Amgen Inc, Chemistry Research and Discovery, Medicinal Chemistry, One Amgen Center Drive, MS 29 1 B, Thousand Oaks, CA 91320 179, USA
    Curr Opin Drug Discov Devel 8:421-30. 2005
    ....
  2. doi request reprint Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)
    Longbin Liu
    Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 51:3688-91. 2008
    ..Blocking this metabolic hot spot led to the discovery of 17 (AMG 458). When dosed orally, 17 significantly inhibited tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight...
  3. doi request reprint Design, synthesis, and biological evaluation of potent c-Met inhibitors
    Noel D D'Angelo
    Department of Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320 1799, USA
    J Med Chem 51:5766-79. 2008
    ..Novel c-Met inhibitors have been designed, developed, and found to be potent in vitro and in vivo...
  4. doi request reprint Azole-based inhibitors of AKT/PKB for the treatment of cancer
    QingPing Zeng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
    Bioorg Med Chem Lett 20:1559-64. 2010
    ..One compound was shown to have acceptable pharmacokinetic properties and to be a potent inhibitor of AKT signaling and of in vivo xenograft tumor growth in a preclinical model of glioblastoma...
  5. ncbi request reprint Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties
    Hui Ling Wang
    Department of Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320 1799, USA
    J Med Chem 50:3528-39. 2007
    ..o). Based on its improved overall profile, compound 16p (AMG 628) was selected as a second-generation candidate for further evaluation in human clinical trials as a potential new treatment for chronic pain...
  6. doi request reprint Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives
    Mark H Norman
    Department of Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 55:1858-67. 2012
    ..These investigations resulted in the identification of a potent and novel class of pyrazolone c-Met inhibitors with good in vivo activity...
  7. doi request reprint Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series
    Longbin Liu
    Department of Medicinal Chemistry, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 55:1868-97. 2012
    ..Compound 59e (AMG 458) was ultimately advanced into preclinical safety studies...
  8. ncbi request reprint High-content screening analysis of the p38 pathway: profiling of structurally related p38alpha kinase inhibitors using cell-based assays
    Sandra Ross
    Amgen Inc, Thousand Oaks, CA 91320 1799, USA
    Assay Drug Dev Technol 4:397-409. 2006
    ..We also found that the choice of cells and inducer can profoundly affect cellular potency results. High-content analysis may reveal signaling details, enriching our understanding of the mechanism of action of p38alpha inhibitors...
  9. ncbi request reprint A soluble base for the copper-catalyzed imidazole N-arylations with aryl halides
    Longbin Liu
    Chemical Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Org Chem 70:10135-8. 2005
    ..Preliminary results with aryl chlorides are also reported...
  10. ncbi request reprint MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein
    Matthew R Lee
    Department of Molecular Structure, Amgen Inc One Amgen Center Drive Thousand Oaks, CA 91320 1799, USA
    Curr Med Chem 12:2979-94. 2005
    ..However, our focus will be on the binding modes of these inhibitors and other p38 inhibitors in the recent literature...
  11. ncbi request reprint Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles
    Vassil I Ognyanov
    Department of Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320 1799, USA
    J Med Chem 49:3719-42. 2006
    ..Compound 46ad also reversed thermal hyperalgesia in a model of inflammatory pain, which was induced by complete Freund's adjuvant (CFA)...
  12. doi request reprint 2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics
    QingPing Zeng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 20:1652-6. 2010
    ..Compound 30 was advanced to a mouse liver PD assay, where it showed dose-dependent inhibition of AKT activity, as measured by the inhibition of phospho-PRAS40...
  13. ncbi request reprint Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr
    Celia Dominguez
    Chemistry Research and Discovery, One Amgen Center Drive Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 17:6003-8. 2007
    ..The clinical utility of inhibitors of this receptor tyrosine kinase is currently under intense investigation. Herein we report our efforts in this arena...
  14. ncbi request reprint Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase
    Nuria Tamayo
    Chemistry Research and Discovery, Amgen, Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 15:2409-13. 2005
    ..They demonstrated potent inhibition of LPS-induced TNF-alpha production in mice and exhibited good efficacy in the rat collagen induced arthritis model...
  15. ncbi request reprint Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate
    Elizabeth M Doherty
    Department of Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320 1799, USA
    J Med Chem 50:3515-27. 2007
    ..o.). Based on its in vivo efficacy and pharmacokinetic profile, compound 23 (N-{4-[6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yloxy]-benzothiazol-2-yl}-acetamide; AMG 517) was selected for further evaluation in human clinical trials...
  16. ncbi request reprint N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists
    Ning Xi
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Dr, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 14:2905-9. 2004
    ..The effects of the conformation and configuration of the gamma-lactam core on the binding were also assessed...