Daniel S La

Summary

Affiliation: Amgen Inc
Country: USA

Publications

  1. doi request reprint Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis
    Daniel S La
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1695-705. 2008
  2. doi request reprint Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation
    Jean Christophe Harmange
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1649-67. 2008
  3. doi request reprint Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors
    Thomas A Dineen
    Chemical Research and Discovery, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142, United States
    J Med Chem 55:9025-44. 2012
  4. doi request reprint Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors
    Matthew M Weiss
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1668-80. 2008
  5. doi request reprint Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease
    Hongbing Huang
    Department of Medicinal Chemistry, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142, United States
    J Med Chem 55:9156-69. 2012
  6. doi request reprint Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid
    Matthew M Weiss
    Department of Chemistry Research and Discovery, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142, United States
    J Med Chem 55:9009-24. 2012
  7. doi request reprint Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors
    Emily A Peterson
    Medicinal Chemistry, Amgen Inc, 360 Binney St, Cambridge, MA 02142, USA
    Bioorg Med Chem Lett 22:4967-74. 2012

Collaborators

Detail Information

Publications7

  1. doi request reprint Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis
    Daniel S La
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1695-705. 2008
    ..In addition, this series of molecules is typically well-absorbed orally, further demonstrating the 2,3-dihydro-1,4-benzoxazine moiety as a promising platform for generating kinase-based antiangiogenic therapeutic agents...
  2. doi request reprint Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation
    Jean Christophe Harmange
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1649-67. 2008
    ..A full account of the preparation, structure-activity relationships, pharmacokinetic properties, and pharmacology of analogues within this series is presented...
  3. doi request reprint Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors
    Thomas A Dineen
    Chemical Research and Discovery, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142, United States
    J Med Chem 55:9025-44. 2012
    ..Several of these compounds caused robust reduction of Aβ levels in rat CSF and brain following oral dosing, and compound 37 exhibited an improved cardiovascular safety profile relative to 1...
  4. doi request reprint Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors
    Matthew M Weiss
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1668-80. 2008
    ..Once-daily oral administration of 22 for 14 days led to 85% inhibition of established HT29 colon cancer and Calu-6 lung cancer xenografts at doses of 10 and 20 mg/kg, respectively...
  5. doi request reprint Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease
    Hongbing Huang
    Department of Medicinal Chemistry, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142, United States
    J Med Chem 55:9156-69. 2012
    ..Our efforts resulted in the identification of a potent, orally bioavailable CNS penetrant compound that exhibited in vivo efficacy. A single oral dose of compound 11a resulted in a significant reduction of CNS Aβ40 in naive rats...
  6. doi request reprint Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid
    Matthew M Weiss
    Department of Chemistry Research and Discovery, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142, United States
    J Med Chem 55:9009-24. 2012
    ....
  7. doi request reprint Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors
    Emily A Peterson
    Medicinal Chemistry, Amgen Inc, 360 Binney St, Cambridge, MA 02142, USA
    Bioorg Med Chem Lett 22:4967-74. 2012
    ....