Thomas Ryckmans

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. doi Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis
    Thomas Ryckmans
    Pfizer Discovery Chemistry, Ramsgate Road, Sandwich CT139NJ Kent, United Kingdom
    Bioorg Med Chem Lett 19:4406-9. 2009
  2. doi Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel
    Thomas Ryckmans
    Pfizer Worldwide Medicinal Chemistry, Ramsgate Road, Sandwich, Kent CT139NJ, United Kingdom
    Bioorg Med Chem Lett 21:4857-9. 2011
  3. ncbi Modulation of the vasopressin system for the treatment of CNS diseases
    Thomas Ryckmans
    Pfizer Worldwide Research and Development, 500 2 190 Ramsgate Road ipc 432, Sandwich, Kent, CT13 9NJ, UK
    Curr Opin Drug Discov Devel 13:538-47. 2010
  4. doi N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration
    Florian Wakenhut
    Department of Genitourinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, UK
    Bioorg Med Chem Lett 19:5078-81. 2009
  5. doi Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template
    Paul V Fish
    Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 19:4579-83. 2009
  6. doi Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition
    Paul V Fish
    Department of Genitourinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 18:2562-6. 2008
  7. doi Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity
    Paul V Fish
    Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 18:4355-9. 2008
  8. doi 2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology
    Dafydd R Owen
    Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, CT13 9NJ, UK
    Bioorg Med Chem Lett 19:1702-6. 2009
  9. ncbi Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives
    Thomas Ryckmans
    Chemical Research, R and D, UCB Pharma SA, Chemin du Foriest, B 1420, Braine l Alleud, Belgium
    Bioorg Med Chem Lett 12:3195-8. 2002
  10. doi Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability
    Patrick S Johnson
    Pfizer Worldwide Medicinal Chemistry, Ramsgate Road, Sandwich Kent CT139NJ, UK
    Bioorg Med Chem Lett 21:5684-7. 2011

Collaborators

Detail Information

Publications11

  1. doi Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis
    Thomas Ryckmans
    Pfizer Discovery Chemistry, Ramsgate Road, Sandwich CT139NJ Kent, United Kingdom
    Bioorg Med Chem Lett 19:4406-9. 2009
    ..Analysis of the Lipophilic Efficiency (LipE) of potent compounds provided new insight for the design of potent, metabolically stable CB2 agonists...
  2. doi Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel
    Thomas Ryckmans
    Pfizer Worldwide Medicinal Chemistry, Ramsgate Road, Sandwich, Kent CT139NJ, United Kingdom
    Bioorg Med Chem Lett 21:4857-9. 2011
    ..Compound 16a (PF-4840154) is a potent, selective agonist of the rat and human TrpA1 channel and elicited TrpA1-mediated nocifensive behaviour in mouse...
  3. ncbi Modulation of the vasopressin system for the treatment of CNS diseases
    Thomas Ryckmans
    Pfizer Worldwide Research and Development, 500 2 190 Ramsgate Road ipc 432, Sandwich, Kent, CT13 9NJ, UK
    Curr Opin Drug Discov Devel 13:538-47. 2010
    ..Given the large unmet medical need in these areas, a renewed interest in the field of CNS-penetrant AVP receptors modulators is expected...
  4. doi N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration
    Florian Wakenhut
    Department of Genitourinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, UK
    Bioorg Med Chem Lett 19:5078-81. 2009
    ..Evaluation in an in vivo preclinical model of stress urinary incontinence showed 9 significantly increased urethral tone at free plasma concentrations consistent with its in vitro primary pharmacology...
  5. doi Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template
    Paul V Fish
    Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 19:4579-83. 2009
    ..Benzamide 11e was differentiated from previous NRIs as it was significantly less lipophilic (DeltaclogP -0.9)...
  6. doi Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition
    Paul V Fish
    Department of Genitourinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 18:2562-6. 2008
    ..Consequently, selective SRI, selective NRI and dual SNRIs were all identified. One of these compounds, a potent and selective dual SNRI, (SS)-5a was selected as a candidate for further pre-clinical evaluation...
  7. doi Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity
    Paul V Fish
    Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 18:4355-9. 2008
    ..Evaluation in vivo, in rat microdialysis experiments, showed 11b increased noradrenaline levels by 400% confirming good CNS penetration...
  8. doi 2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology
    Dafydd R Owen
    Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, CT13 9NJ, UK
    Bioorg Med Chem Lett 19:1702-6. 2009
    ..The structure-activity relationship of the series against the hERG ion channel proved to be a key selectivity hurdle for the series...
  9. ncbi Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives
    Thomas Ryckmans
    Chemical Research, R and D, UCB Pharma SA, Chemin du Foriest, B 1420, Braine l Alleud, Belgium
    Bioorg Med Chem Lett 12:3195-8. 2002
    ..This class of compounds potentially represents a new generation of antidepressants...
  10. doi Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability
    Patrick S Johnson
    Pfizer Worldwide Medicinal Chemistry, Ramsgate Road, Sandwich Kent CT139NJ, UK
    Bioorg Med Chem Lett 21:5684-7. 2011
    ..This effort culminated in the discovery of PF-184563, a novel, selective V1a antagonist with excellent in vitro and in vivo properties...
  11. doi [4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors
    Paul V Fish
    Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 18:1795-8. 2008
    ..Compound 31 demonstrated potent NRI activity combined with good selectivity over serotonin and dopamine reuptake and no significant off-target pharmacology...