William N Washburn

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. doi Evolution of sodium glucose co-transporter 2 inhibitors as anti-diabetic agents
    William N Washburn
    Senior Research Fellow, Metabolic Diseases Chemistry, Research and Development, Bristol Myers Squibb Co, PO Box 5400, Princeton, NJ 08543, USA
    Expert Opin Ther Pat 19:1485-99. 2009
  2. doi Differentiating sodium-glucose co-transporter-2 inhibitors in development for the treatment of type 2 diabetes mellitus
    William N Washburn
    Metabolic Diseases Chemistry, Research and Development, Bristol Myers Squibb Co Princeton, NJ, USA
    Expert Opin Investig Drugs 22:463-86. 2013
  3. doi Sodium glucose co-transporter 2 (SGLT2) inhibitors: novel antidiabetic agents
    William N Washburn
    Metabolic Diseases Chemistry, Research and Development, Bristol Myers Squibb Co, P O Box 5400, Princeton, NJ 08543, USA
    Expert Opin Ther Pat 22:483-94. 2012
  4. ncbi Beta 3 agonists. Part 1: evolution from inception to BMS-194449
    W N Washburn
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 11:3035-9. 2001
  5. ncbi Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations
    W N Washburn
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 17:4290-6. 2007
  6. ncbi BMS-201620: a selective beta 3 agonist
    W N Washburn
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 14:3525-9. 2004
  7. doi Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2
    Bruce A Ellsworth
    Research and Development, Bristol Myers Squibb Co, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:4770-3. 2008
  8. doi Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes
    Wei Meng
    Drug Safety Evaluation and Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543, USA
    J Med Chem 51:1145-9. 2008
  9. doi Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats
    Songping Han
    Metabolic Diseases Biology, Bristol Myers Squibb Research and Development, Princeton, New Jersey, USA
    Diabetes 57:1723-9. 2008
  10. ncbi Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series
    Bruce A Ellsworth
    Pharmaceutical Research Institute, Bristol Myers Squibb Co, PO Box 5400 Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 17:3978-82. 2007

Detail Information

Publications12

  1. doi Evolution of sodium glucose co-transporter 2 inhibitors as anti-diabetic agents
    William N Washburn
    Senior Research Fellow, Metabolic Diseases Chemistry, Research and Development, Bristol Myers Squibb Co, PO Box 5400, Princeton, NJ 08543, USA
    Expert Opin Ther Pat 19:1485-99. 2009
    ..This capacity can be modulated by SGLT2 inhibitors thereby providing a unique insulin independent method of treatment of diabetes...
  2. doi Differentiating sodium-glucose co-transporter-2 inhibitors in development for the treatment of type 2 diabetes mellitus
    William N Washburn
    Metabolic Diseases Chemistry, Research and Development, Bristol Myers Squibb Co Princeton, NJ, USA
    Expert Opin Investig Drugs 22:463-86. 2013
    ..Sodium-glucose co-transporter-2 (SGLT2) inhibitors are a novel class of agents for the treatment of type 2 diabetes mellitus (T2DM). By inhibiting SGLT2, they prevent renal glucose reabsorption, resulting in glucosuria...
  3. doi Sodium glucose co-transporter 2 (SGLT2) inhibitors: novel antidiabetic agents
    William N Washburn
    Metabolic Diseases Chemistry, Research and Development, Bristol Myers Squibb Co, P O Box 5400, Princeton, NJ 08543, USA
    Expert Opin Ther Pat 22:483-94. 2012
    ..Clinical studies indicate that SGLT2 inhibitors provide an insulin-independent means to reduce the hyperglycemia that is the hallmark of type 2 diabetes mellitus (T2DM) with minimal risk of hypoglycemia...
  4. ncbi Beta 3 agonists. Part 1: evolution from inception to BMS-194449
    W N Washburn
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 11:3035-9. 2001
    ..This latter subset yielded a clinical candidate, BMS-194449 (35).(1)..
  5. ncbi Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations
    W N Washburn
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 17:4290-6. 2007
    ....
  6. ncbi BMS-201620: a selective beta 3 agonist
    W N Washburn
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 14:3525-9. 2004
    ..SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation...
  7. doi Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2
    Bruce A Ellsworth
    Research and Development, Bristol Myers Squibb Co, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:4770-3. 2008
    ..The lead C-arylglucoside (7a) demonstrates superior metabolic stability to its O-arylglucoside counterpart (4) and it promotes glucosuria when administered in vivo...
  8. doi Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes
    Wei Meng
    Drug Safety Evaluation and Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543, USA
    J Med Chem 51:1145-9. 2008
    ..These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2 diabetes...
  9. doi Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats
    Songping Han
    Metabolic Diseases Biology, Bristol Myers Squibb Research and Development, Princeton, New Jersey, USA
    Diabetes 57:1723-9. 2008
    ..We have identified dapagliflozin as a potent and selective inhibitor of the renal sodium-glucose cotransporter SGLT2 in vitro and characterized its in vitro and in vivo pharmacology...
  10. ncbi Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series
    Bruce A Ellsworth
    Pharmaceutical Research Institute, Bristol Myers Squibb Co, PO Box 5400 Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 17:3978-82. 2007
    ..Compound 35 elicits a 46% reduction in food intake in ad libidum fed rats 4-h post-dose...
  11. ncbi BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor
    A V Gavai
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 11:3041-4. 2001
    ..Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation...
  12. ncbi Addition of benzylic and allylic organozinc and Grignard reagents to resin-bound imines to provide alpha-branched secondary amines bearing a wide variety of functional groups. Utility in the synthesis of beta-3 adrenergic receptor agonists
    Gang Wu
    Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08543, USA
    J Comb Chem 7:99-108. 2005
    ..Three modules--a resin-bound primary amine, an aromatic aldehyde, and the organometallic--were independently varied to produce a combinatorial library of alpha-branched secondary amines designed as beta-3 adrenergic receptor agonists...