R A Smith

Summary

Affiliation: Bayer HealthCare
Country: USA

Publications

  1. ncbi request reprint Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis
    Roger A Smith
    Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 12:1303-6. 2002
  2. ncbi request reprint Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives
    Roger A Smith
    Department of Chemistry Research, Bayer HealthCare, Pharmaceuticals Division, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 17:673-8. 2007
  3. ncbi request reprint Recent advances in the research and development of CB1 antagonists
    Roger A Smith
    Bayer Research Center, Bayer HealthCare, Pharmaceuticals Division, 400 Morgan Lane, West Haven, CT 06516, USA
    IDrugs 8:53-66. 2005
  4. ncbi request reprint Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach
    R A Smith
    Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 11:2775-8. 2001
  5. ncbi request reprint 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
  6. ncbi request reprint 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
  7. ncbi request reprint 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
  8. ncbi request reprint 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
  9. ncbi request reprint 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
  10. ncbi request reprint 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

Detail Information

Publications16

  1. ncbi request reprint Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis
    Roger A Smith
    Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 12:1303-6. 2002
    ..3-fold increase in activity (e.g., 4'-fluoro-2'-hydroxy analogue 33, IC50=190 nM). For efficient preparation of 2'-substituted phenylpyridines, a novel synthesis via pyrones and 4-methoxy-pyridines was developed...
  2. ncbi request reprint Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives
    Roger A Smith
    Department of Chemistry Research, Bayer HealthCare, Pharmaceuticals Division, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 17:673-8. 2007
    ..A representative analog was established to cause significant appetite suppression and reduction in body weight gain in industry-standard rat models used to develop new therapeutics for obesity...
  3. ncbi request reprint Recent advances in the research and development of CB1 antagonists
    Roger A Smith
    Bayer Research Center, Bayer HealthCare, Pharmaceuticals Division, 400 Morgan Lane, West Haven, CT 06516, USA
    IDrugs 8:53-66. 2005
    ....
  4. ncbi request reprint Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach
    R A Smith
    Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 11:2775-8. 2001
    ..7 microM. A combinatorial synthesis approach enabled the identification of a breakthrough lead (IC(50)=0.54 microM) for a second generation series of heterocyclic urea raf kinase inhibitors...
  5. ncbi request reprint 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...
  6. ncbi request reprint 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...
  7. ncbi request reprint 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...
  8. ncbi request reprint 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...
  9. ncbi request reprint 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
    ....
  10. ncbi request reprint 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...
  11. ncbi request reprint 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...
  12. ncbi request reprint Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists
    Gaetan H Ladouceur
    Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 12:3421-4. 2002
    ..A diastereoselective methylcopper reaction was developed to facilitate the synthesis, and single isomers were isolated with activities in the range IC(50)=10-25 nM...
  13. ncbi request reprint 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)...
  14. ncbi request reprint Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity
    Roger A Smith
    Department of Chemistry Research, Bayer HealthCare, Pharmaceuticals Division, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 17:2706-11. 2007
    ..7nM, and caused significant appetite suppression and robust, dose-dependent reduction of body weight gain in industry-standard rat models...
  15. ncbi request reprint 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...
  16. ncbi request reprint Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators
    Roger A Smith
    Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA
    Bioorg Med Chem Lett 12:2875-8. 2002
    ..Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay...