Madhu Chintala

Summary

Affiliation: Schering-Plough Research Institute
Country: USA

Publications

  1. ncbi Basic and translational research on proteinase-activated receptors: antagonism of the proteinase-activated receptor 1 for thrombin, a novel approach to antiplatelet therapy for atherothrombotic disease
    Madhu Chintala
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    J Pharmacol Sci 108:433-8. 2008
  2. ncbi SCH 602539, a protease-activated receptor-1 antagonist, inhibits thrombosis alone and in combination with cangrelor in a Folts model of arterial thrombosis in cynomolgus monkeys
    Madhu Chintala
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Arterioscler Thromb Vasc Biol 30:2143-9. 2010
  3. ncbi Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists
    Mariappan V Chelliah
    Central Nervous System and Cardiovascular Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 50:5147-60. 2007
  4. ncbi Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core
    Martin C Clasby
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 17:3647-51. 2007
  5. ncbi Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring
    Yan Xia
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 17:4509-13. 2007
  6. ncbi Metabolism-based identification of a potent thrombin receptor antagonist
    Martin C Clasby
    Central Nervous System and Cardiovascular Chemical Research, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    J Med Chem 50:129-38. 2007
  7. ncbi Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity
    Samuel Chackalamannil
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    J Med Chem 51:3061-4. 2008
  8. ncbi Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists
    Martin C Clasby
    Central Nervous System and Cardiovascular Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 16:1544-8. 2006
  9. ncbi Discovery of a vorapaxar analog with increased aqueous solubility
    Yan Xia
    Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 20:6676-9. 2010
  10. ncbi Discovery of nor-seco himbacine analogs as thrombin receptor antagonists
    Mariappan V Chelliah
    Central Nervous System and Cardiovascular Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 22:2544-9. 2012

Detail Information

Publications11

  1. ncbi Basic and translational research on proteinase-activated receptors: antagonism of the proteinase-activated receptor 1 for thrombin, a novel approach to antiplatelet therapy for atherothrombotic disease
    Madhu Chintala
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    J Pharmacol Sci 108:433-8. 2008
    ....
  2. ncbi SCH 602539, a protease-activated receptor-1 antagonist, inhibits thrombosis alone and in combination with cangrelor in a Folts model of arterial thrombosis in cynomolgus monkeys
    Madhu Chintala
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Arterioscler Thromb Vasc Biol 30:2143-9. 2010
    ....
  3. ncbi Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists
    Mariappan V Chelliah
    Central Nervous System and Cardiovascular Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 50:5147-60. 2007
    ..A detailed profile of 28b, a benchmark compound in this series, with a Ki of 4.3 nM, is presented...
  4. ncbi Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core
    Martin C Clasby
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 17:3647-51. 2007
    ..This series of compounds showed excellent in vitro and in vivo potency. The most potent compound 40 had an IC(50) of 7.6 nM and showed robust inhibition of platelet aggregation in a cynomolgus monkey model after oral administration...
  5. ncbi Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring
    Yan Xia
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 17:4509-13. 2007
    ..One of the newly discovered analogs bearing a 5-(3-pyridyl) substituent showed excellent PAR-1 affinity (Ki = 22 nM) and oral activity with reduced ClogP and improved off-target selectivity compared to an earlier development candidate...
  6. ncbi Metabolism-based identification of a potent thrombin receptor antagonist
    Martin C Clasby
    Central Nervous System and Cardiovascular Chemical Research, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    J Med Chem 50:129-38. 2007
    ..Compound 4 showed a superior rat enzyme induction profile relative to compound 1, allowing it to replace compound 1 as a development candidate...
  7. ncbi Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity
    Samuel Chackalamannil
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    J Med Chem 51:3061-4. 2008
    ....
  8. ncbi Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists
    Martin C Clasby
    Central Nervous System and Cardiovascular Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 16:1544-8. 2006
    ..Compound 30 is a highly potent thrombin receptor antagonist (IC(50)=6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study...
  9. ncbi Discovery of a vorapaxar analog with increased aqueous solubility
    Yan Xia
    Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 20:6676-9. 2010
    ..Also presented are in vivo evaluations of this compound in a cynomolgus monkey platelet aggregation assay and in a Folts model of thrombosis in anesthetized monkeys...
  10. ncbi Discovery of nor-seco himbacine analogs as thrombin receptor antagonists
    Mariappan V Chelliah
    Central Nervous System and Cardiovascular Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 22:2544-9. 2012
    ..Following this discovery, the metabolite series was optimized to obtain analogs that showed very good ex vivo efficacy along with excellent pharmacokinetic profile in c. monkey...
  11. ncbi Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents
    Samuel Chackalamannil
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 48:5884-7. 2005
    ....