Paul D Leeson

Summary

Affiliation: AstraZeneca R and D

Publications

  1. ncbi request reprint The influence of drug-like concepts on decision-making in medicinal chemistry
    Paul D Leeson
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough LE15 5RH, UK
    Nat Rev Drug Discov 6:881-90. 2007
  2. ncbi request reprint Time-related differences in the physical property profiles of oral drugs
    Paul D Leeson
    Department of Medicinal Chemistry, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK
    J Med Chem 47:6338-48. 2004
  3. ncbi request reprint A comparison of physiochemical property profiles of development and marketed oral drugs
    Mark C Wenlock
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, United Kingdom
    J Med Chem 46:1250-6. 2003
  4. ncbi request reprint Lessons learned from candidate drug attrition
    James R Empfield
    AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    IDrugs 13:869-73. 2010
  5. doi request reprint The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS)
    David R Cheshire
    Department of Chemistry, AstraZeneca Charnwood, Bakewell Road, Loughborough LE11 5RH, United Kingdom
    Bioorg Med Chem Lett 21:2468-71. 2011
  6. doi request reprint The influence of the 'organizational factor' on compound quality in drug discovery
    Paul D Leeson
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK
    Nat Rev Drug Discov 10:749-65. 2011
  7. ncbi request reprint From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis
    Brian Springthorpe
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK
    Bioorg Med Chem Lett 17:6013-8. 2007
  8. doi request reprint Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules
    Tim Luker
    AstraZeneca R and D, Medicinal Chemistry, Charnwood, Loughborough, Leicestershire LE11 5RH, UK
    Bioorg Med Chem Lett 21:5673-9. 2011
  9. ncbi request reprint 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1
    Robert W Carling
    Department of Medicinal Chemistry, The Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    J Med Chem 47:1807-22. 2004

Collaborators

Detail Information

Publications9

  1. ncbi request reprint The influence of drug-like concepts on decision-making in medicinal chemistry
    Paul D Leeson
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough LE15 5RH, UK
    Nat Rev Drug Discov 6:881-90. 2007
    ..Tackling the threat of compound-related toxicological attrition needs to move to the mainstream of medicinal chemistry decision-making...
  2. ncbi request reprint Time-related differences in the physical property profiles of oral drugs
    Paul D Leeson
    Department of Medicinal Chemistry, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK
    J Med Chem 47:6338-48. 2004
    ..The results suggest that the balance between polar and nonpolar drug properties is an important, unchanging feature of oral drug molecules...
  3. ncbi request reprint A comparison of physiochemical property profiles of development and marketed oral drugs
    Mark C Wenlock
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, United Kingdom
    J Med Chem 46:1250-6. 2003
    ..It is also clear that the most lipophilic compounds are being discontinued from development...
  4. ncbi request reprint Lessons learned from candidate drug attrition
    James R Empfield
    AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    IDrugs 13:869-73. 2010
    ..Separating the key scientific experiment--proof-of-concept clinical trials in humans--from commercial development imperatives is a necessary step for the industry...
  5. doi request reprint The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS)
    David R Cheshire
    Department of Chemistry, AstraZeneca Charnwood, Bakewell Road, Loughborough LE11 5RH, United Kingdom
    Bioorg Med Chem Lett 21:2468-71. 2011
    ..By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8...
  6. doi request reprint The influence of the 'organizational factor' on compound quality in drug discovery
    Paul D Leeson
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK
    Nat Rev Drug Discov 10:749-65. 2011
    ..On the basis of our analysis, we conclude that a substantial sector of the pharmaceutical industry has not modified its drug design practices and is still producing compounds with suboptimal physicochemical profiles...
  7. ncbi request reprint From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis
    Brian Springthorpe
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK
    Bioorg Med Chem Lett 17:6013-8. 2007
    ..The leading compound, 17 (AZD6140), is currently in a large phase III clinical trial for the treatment of acute coronary syndromes and prevention of thromboembolic clinical sequelae...
  8. doi request reprint Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules
    Tim Luker
    AstraZeneca R and D, Medicinal Chemistry, Charnwood, Loughborough, Leicestershire LE11 5RH, UK
    Bioorg Med Chem Lett 21:5673-9. 2011
    ..The themes within this work provide additional guidance for medicinal design chemists and complement other literature property guidelines...
  9. ncbi request reprint 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1
    Robert W Carling
    Department of Medicinal Chemistry, The Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    J Med Chem 47:1807-22. 2004
    ....