J Dumas

Summary

Affiliation: Bayer HealthCare
Country: USA

Publications

  1. ncbi Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor
    Jacques Dumas
    Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 12:1559-62. 2002
  2. ncbi Protein kinase inhibitors from the urea class
    Jacques Dumas
    Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA
    Curr Opin Drug Discov Devel 5:718-27. 2002
  3. ncbi Recent developments in the discovery of protein kinase inhibitors from the urea class
    Jacques Dumas
    Bayer Research Center, Bayer Pharmaceutical Corporation, West Haven, CT 06516, USA
    Curr Opin Drug Discov Devel 7:600-16. 2004
  4. ncbi Recent advances in the research and development of RAF kinase inhibitors
    Roger A Smith
    Bayer Research Center, Bayer Pharmaceuticals Corporation, West Haven, CT 06516, USA
    Curr Top Med Chem 6:1071-89. 2006
  5. ncbi Discovery and development of sorafenib: a multikinase inhibitor for treating cancer
    Scott Wilhelm
    Department of Cancer Research, Bayer Pharmaceuticals Corp, West Haven, Connecticut 06516, USA
    Nat Rev Drug Discov 5:835-44. 2006
  6. ncbi Discovery of a new class of p38 kinase inhibitors
    J Dumas
    Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 10:2047-50. 2000
  7. ncbi 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors
    J Dumas
    Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 10:2051-4. 2000
  8. ncbi Growth factor receptor kinase inhibitors: recent progress and clinical impact
    J Dumas
    Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA
    Curr Opin Drug Discov Devel 4:378-89. 2001
  9. ncbi Small molecule inhibitors of the class 1 receptor tyrosine kinase family
    G Stuart Cockerill
    Drug Discovery, Arrow Therapeutics, Britannia House, 7 Trinity Street, London SE1 1DS UK and GlaxoSmithKline, Discovery Research Kinase Chemistry, 5 Moore Dr, Research Triangle Park, NC 27709, USA
    Curr Top Med Chem 2:1001-10. 2002
  10. ncbi p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas
    A M Redman
    Department of Chemistry Research, Bayer Research Center, Pharmaceutical Division, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 11:9-12. 2001

Collaborators

  • R A Smith
  • A M Redman
  • David Gunn
  • P A Trail
  • J Chen
  • D Young
  • Timothy B Lowinger
  • Karen E Lackey
  • Michael Brands
  • Uday R Khire
  • Jeffrey S Johson
  • Scott Wilhelm
  • M Vicente
  • D Auclair
  • Philip Wickens
  • Robert Schoenleber
  • Beatriz Lara
  • Robert Sibley
  • G Stuart Cockerill
  • Y Chang
  • Charles Kreiman
  • Donald Bierer
  • D Miller
  • R Gedrich
  • Lei Wang
  • Chih Yuan Chuang
  • Ronda Ott-Morgan
  • X Zhang
  • Louise Perkins
  • H Shi
  • Barton Phillips
  • H Vasavada
  • Gloria Hofilena
  • S Rocks
  • Tim Housley
  • Mingbao Zhang
  • D Wilkie
  • Christopher Carter
  • Julie Dixon
  • V Yatsula
  • Debbie Braun
  • Antonella Bacchiocchi
  • Elizabeth Sullivan
  • M Lynch
  • Ian Taylor
  • Harold Kluender
  • W Pickett
  • A Burd
  • Xiaomei Zhang
  • William J Scott
  • Don Bankston
  • Catherine Brennan
  • Ellalahewage Kumarasinghe
  • C Carter
  • Zhenqiu Hong
  • Benjamin Jones
  • Melissa S Brown
  • Joan Levy
  • Furahi Achebe
  • Xiuying Sun
  • Ryan Sheeler
  • L Abriola
  • Istvan Enyedy
  • Mark Miglarese
  • Jesus Mingorance
  • Antonella Santona
  • Orietta Massidda
  • Sabrina Petruzzelli
  • Ana Isabel Rico
  • Jacques Biton
  • Diana Marrero
  • Holia Hatoum-Mokdad
  • Laszlo Musza
  • Hong Xiao
  • William Stirtan
  • William Carley

Detail Information

Publications19

  1. ncbi Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor
    Jacques Dumas
    Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 12:1559-62. 2002
    ..This compound is orally active in two acute models of cytokine release (TNF-induced IL-6 and LPS-induced TNF) and a chronic model of arthritis (20-day murine collagen-induced arthritis)...
  2. ncbi Protein kinase inhibitors from the urea class
    Jacques Dumas
    Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA
    Curr Opin Drug Discov Devel 5:718-27. 2002
    ..The present review summarizes available data, and provides an overview of the structure-activity relationships against a variety of kinase targets, including p38, Raf-1 and cyclin-dependent kinases...
  3. ncbi Recent developments in the discovery of protein kinase inhibitors from the urea class
    Jacques Dumas
    Bayer Research Center, Bayer Pharmaceutical Corporation, West Haven, CT 06516, USA
    Curr Opin Drug Discov Devel 7:600-16. 2004
    ..This review focuses on the most recent developments in the discovery of urea-based protein kinase inhibitors...
  4. ncbi Recent advances in the research and development of RAF kinase inhibitors
    Roger A Smith
    Bayer Research Center, Bayer Pharmaceuticals Corporation, West Haven, CT 06516, USA
    Curr Top Med Chem 6:1071-89. 2006
    ..Preclinical and clinical data for the RAF kinase inhibitor sorafenib (BAY 43-9006 tosylate), that was recently approved in the US for the treatment of advanced renal cell carcinoma, are also outlined...
  5. ncbi Discovery and development of sorafenib: a multikinase inhibitor for treating cancer
    Scott Wilhelm
    Department of Cancer Research, Bayer Pharmaceuticals Corp, West Haven, Connecticut 06516, USA
    Nat Rev Drug Discov 5:835-44. 2006
    ....
  6. ncbi Discovery of a new class of p38 kinase inhibitors
    J Dumas
    Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 10:2047-50. 2000
    ..Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and exhibit activity in the nanomolar range. Very steep structure-activity relationships are observed within this class...
  7. ncbi 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors
    J Dumas
    Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 10:2051-4. 2000
    ..Optimization for cellular potency led to the discovery of a new class of potent and selective p38 kinase inhibitors, exemplified by the 1-phenyl-5-pyrazolyl urea 7 (IC50 = 13 nM)...
  8. ncbi Growth factor receptor kinase inhibitors: recent progress and clinical impact
    J Dumas
    Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA
    Curr Opin Drug Discov Devel 4:378-89. 2001
    ..This review focuses on the most recent progress in this area, and gives an overview of the compounds currently in the clinic, as well as key preclinical analogs...
  9. ncbi Small molecule inhibitors of the class 1 receptor tyrosine kinase family
    G Stuart Cockerill
    Drug Discovery, Arrow Therapeutics, Britannia House, 7 Trinity Street, London SE1 1DS UK and GlaxoSmithKline, Discovery Research Kinase Chemistry, 5 Moore Dr, Research Triangle Park, NC 27709, USA
    Curr Top Med Chem 2:1001-10. 2002
    ..The readers' attention is drawn to common issues of selectivity and potency generally encountered with kinase inhibitors...
  10. ncbi p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas
    A M Redman
    Department of Chemistry Research, Bayer Research Center, Pharmaceutical Division, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 11:9-12. 2001
    ..A series of thienyl, furyl, and pyrrolyl ureas has been identified as potent p38 inhibitors, displaying in vitro activity in the nanomolar range...
  11. ncbi Preparation of 5-substituted 3-aminofuran-2-carboxylate esters
    A M Redman
    Department of Chemistry Research, Bayer Research Center, West Haven, Connecticut 06516, USA
    Org Lett 2:2061-3. 2000
    ..Currently, this method is limited to the synthesis of 5-alkyl-, 5-aryl-, and 4,5-fused bicyclic furans...
  12. ncbi Discovery and parallel synthesis of a new class of cathepsin K inhibitors
    R A Smith
    Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 11:2951-4. 2001
    ..Traditional and high-speed parallel synthesis techniques were applied to investigate this series. Structure-activity relationships were established, and certain analogues were characterized with IC(50) values in the range 200-500 nM...
  13. ncbi Antitumor activity of sorafenib in FLT3-driven leukemic cells
    D Auclair
    Department of Cancer Biology, Bayer Pharmaceuticals Corporation, West Haven, CT 06516, USA
    Leukemia 21:439-45. 2007
    ..The demonstration that sorafenib exhibits potent target inhibition and efficacy in FLT3-driven models suggests that this compound may have a therapeutic benefit for patients with FLT3-driven leukemias...
  14. ncbi Design and discovery of small molecules targeting raf-1 kinase
    Timothy B Lowinger
    Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA
    Curr Pharm Des 8:2269-78. 2002
    ..The present review summarizes the medicinal chemistry development of ureas as highly potent inhibitors of Raf-1 kinase...
  15. ncbi 4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 2. SAR
    David Gunn
    Bayer Research Center, Bayer HealthCare Pharmaceuticals, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 15:3053-7. 2005
    ..4,5-Disubstituted cis-pyrrolidinones were investigated as inhibitors of type II 17beta-hydroxysteroid dehydrogenase (17beta-HSD). Early structure-activity relationship patterns for this class of compounds are discussed...
  16. ncbi Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent
    Uday R Khire
    Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 14:783-6. 2004
    ..Based on this finding, we hypothesize that this portion of the molecule is directed towards the solvent in Raf-1...
  17. ncbi A novel estrogen receptor ligand template
    Robert Sibley
    Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 13:1919-22. 2003
    ..3.1]-nonene core have been investigated. The prototype compound exhibits potent binding at the ERbeta receptor and promising estrogen receptor subtype selectivity...
  18. ncbi SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer
    Philip Wickens
    Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 17:4378-81. 2007
    ..Corresponding thiophene, pyrazole, and thiazole core analogs were prepared as VEGFR-2 inhibitors with c-KIT, and B-RAF activity. Compounds in the phenyl, thiophene, and thiazole series are in vivo active...
  19. ncbi Cell division in cocci: localization and properties of the Streptococcus pneumoniae FtsA protein
    Beatriz Lara
    Aventis Pharma, 102 route de Noisy, F 93235 Romainville cedex, France
    Mol Microbiol 55:699-711. 2005
    ..Consistent with the absence of an ATPase activity, the polymers are highly stable and not dynamic. These results suggest that the FtsA protein could also polymerize in vivo and the polymers participate in septation...