Gregory S Bisacchi

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. ncbi request reprint Structure of the complex of trypsin with a highly potent synthetic inhibitor at 0.97 A resolution
    Manashi Sherawat
    Department of Biophysics, All India Institute of Medical Sciences, New Delhi 110029, India
    Acta Crystallogr D Biol Crystallogr 63:500-7. 2007

Collaborators

  • Steven M Seiler
  • William A Slusarchyk
  • Guohua Zhao
  • Wei Meng
  • William A Schumacher
  • Markus Perbandt
  • Stephen P O'Connor
  • James C Sutton
  • Robert Zahler
  • Karen S Hartl
  • Manashi Sherawat
  • Yan Shi
  • Scott A Bolton
  • Martin L Ogletree
  • Chiehying Chang
  • Tej P Singh
  • Punit Kaur
  • Howard M Einspahr
  • Christian Betzel
  • Bruce L Jacobson
  • Tara L Peterson
  • Karnail S Atwal
  • Chi Li
  • Jeffrey M Bozarth
  • Andrew T Pudzianowski
  • Alan R Rendina
  • Philip D Stein
  • Sonia Youssef
  • Ge Zhang
  • Sharon N Bisaha
  • Mengxiao Shi
  • Eddie C Liu
  • Doree Sitkoff
  • Jing Zhang
  • Thomas E Steinbacher
  • Bruce Jacobson
  • Arvind Mathur
  • Malcolm E Davis
  • Ming Hsing Huang
  • Glenn Jacobs
  • Zulan Pi
  • Uwe Treuner

Detail Information

Publications7

  1. 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
    ....
  2. 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...
  3. 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...
  4. 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...
  5. 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]...
  6. 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...
  7. ncbi request reprint Structure of the complex of trypsin with a highly potent synthetic inhibitor at 0.97 A resolution
    Manashi Sherawat
    Department of Biophysics, All India Institute of Medical Sciences, New Delhi 110029, India
    Acta Crystallogr D Biol Crystallogr 63:500-7. 2007
    ....