Steven M Seiler

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. ncbi request reprint Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues
    Jagabandhu Das
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:41-4. 2002
  2. ncbi request reprint Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664
    Jagabandhu Das
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:45-9. 2002
  3. ncbi request reprint Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity
    Edwin J Iwanowicz
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3183-6. 2002
  4. ncbi request reprint Peptide-derived protease-activated receptor-1 (PAR-1) antagonists
    Steven M Seiler
    Department of Vascular Biology, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08534, USA
    Curr Med Chem Cardiovasc Hematol Agents 1:1-11. 2003
  5. ncbi request reprint Synthesis of potent and highly selective inhibitors of human tryptase
    William A Slusarchyk
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3235-8. 2002
  6. ncbi request reprint Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
    James C Sutton
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 14:2233-9. 2004
  7. ncbi request reprint Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase
    Gregory S Bisacchi
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:2227-31. 2004
  8. doi request reprint Synthesis and evaluation of acylguanidine FXa inhibitors
    Stephen P O'Connor
    Department of Discovery Chemistry, Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:4696-9. 2008
  9. ncbi request reprint Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
    Guohua Zhao
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:309-12. 2004
  10. ncbi request reprint Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
    James C Sutton
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3229-33. 2002

Collaborators

Detail Information

Publications11

  1. ncbi request reprint Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues
    Jagabandhu Das
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:41-4. 2002
    ..BMS-189090 (5) is identified as a potent, selective, and reversible inhibitor of human alpha-thrombin that is efficacious in vivo in a mice lethality model, and in inhibiting both arterial and venous thrombosis in a rat model...
  2. ncbi request reprint Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664
    Jagabandhu Das
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:45-9. 2002
    ....
  3. ncbi request reprint Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity
    Edwin J Iwanowicz
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3183-6. 2002
    ..Compounds 9 and 11, orally active inhibitors of thrombin catalytic activity, were identified to be efficacious in a thrombin-induced lethality model in mice...
  4. ncbi request reprint Peptide-derived protease-activated receptor-1 (PAR-1) antagonists
    Steven M Seiler
    Department of Vascular Biology, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08534, USA
    Curr Med Chem Cardiovasc Hematol Agents 1:1-11. 2003
    ..The use of peptide agonists and antagonists has made possible much progress in our understanding of the role of this receptor...
  5. ncbi request reprint Synthesis of potent and highly selective inhibitors of human tryptase
    William A Slusarchyk
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3235-8. 2002
    ..7 nM) with high selectivity (>3000-fold) for tryptase versus related serine proteases including trypsin...
  6. ncbi request reprint Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
    James C Sutton
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 14:2233-9. 2004
    ..From these studies, potent inhibitors with improved specificity were discovered...
  7. ncbi request reprint Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase
    Gregory S Bisacchi
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:2227-31. 2004
    ..In particular, BMS-354326 (4) is a highly potent tryptase inhibitor (IC(50)=1.8 nM), which has excellent selectivity against trypsin and most other related serine proteases...
  8. doi request reprint Synthesis and evaluation of acylguanidine FXa inhibitors
    Stephen P O'Connor
    Department of Discovery Chemistry, Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:4696-9. 2008
    ..Conditions for the rapid synthesis and purification of these compounds are described along with their ability to inhibit FXa. The best FXa inhibitor is 1 with a FXa IC(50) of 6 nM...
  9. ncbi request reprint Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
    Guohua Zhao
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:309-12. 2004
    ..A member of this series, 8t, was identified as a potent inhibitor of human tryptase (IC(50)=38 nM) with selectivity >/=330-fold versus related serine proteases (trypsin, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa) [corrected]...
  10. ncbi request reprint Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
    James C Sutton
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3229-33. 2002
    ....
  11. ncbi request reprint Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors
    Yan Shi
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 15:5453-8. 2005
    ..N,N'-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors...