Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck:  Synthesis, SAR, and in Vivo Anti-Inflammatory Activity

  • Erin F. DiMauro
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • John Newcomb
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Joseph J. Nunes
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Jean E. Bemis
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Christina Boucher
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • John L. Buchanan
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • William H. Buckner
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Victor J. Cee
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Lilly Chai
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Holly L. Deak
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Linda F. Epstein
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Ted Faust
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Paul Gallant
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Stephanie D. Geuns-Meyer
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Anu Gore
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Yan Gu
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Brad Henkle
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Brian L. Hodous
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Faye Hsieh
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Xin Huang
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Joseph L. Kim
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Josie H. Lee
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Matthew W. Martin
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Craig E. Masse
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • David C. McGowan
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Daniela Metz
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Deanna Mohn
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Kurt A. Morgenstern
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Antonio Oliveira-dos-Santos
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Vinod F. Patel
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • David Powers
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Paul E. Rose
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Stephen Schneider
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Susan A. Tomlinson
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Yan-Yan Tudor
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Susan M. Turci
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Andrew A. Welcher
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Ryan D. White
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Huilin Zhao
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Li Zhu
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799
  • Xiaotian Zhu
    Department of Medicinal Chemistry, Department of HTS and Molecular Pharmacology and Department of Molecular Structure, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, and Department of Inflammation, Department of Pharmaceutics, and Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799

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