James J Li

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. ncbi Discovery of a potent and novel motilin agonist
    James J Li
    Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08643 5400, USA
    J Med Chem 47:1704-8. 2004
  2. ncbi Tetrazole based amides as growth hormone secretagogues
    James J Li
    Discovery Chemistry, Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:2536-9. 2008
  3. ncbi 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors
    James J Li
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 17:3208-11. 2007
  4. ncbi Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications
    James J Li
    Discovery Chemistry, Computer Assisted Drug Design, Metabolic Disease Research, Metabolism and Pharmacokinetics, Discovery Analytical Sciences, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543 5400, USA
    J Med Chem 50:3015-25. 2007
  5. ncbi Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain
    Jun Li
    Discovery Chemistry, Bristol Myers Squibb, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 18:1825-9. 2008
  6. ncbi Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180)
    Jun Li
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543, USA
    J Med Chem 50:5890-3. 2007
  7. ncbi Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)
    Haixia Wang
    Research and Development, Bristol Myers Squibb, PO Box 5400, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 21:4146-9. 2011
  8. ncbi Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
    Haixia Wang
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:3168-72. 2008
  9. ncbi A synthesis of N-bridged 5,6-bicylic pyridines via a mild cyclodehydration using the burgess reagent and discovery of a novel carbamylsulfonylation reaction
    Jie Jack Li
    Discovery Chemistry, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    Org Lett 10:2897-900. 2008
  10. ncbi Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues
    James J Li
    Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 15:1799-802. 2005

Collaborators

Detail Information

Publications11

  1. ncbi Discovery of a potent and novel motilin agonist
    James J Li
    Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08643 5400, USA
    J Med Chem 47:1704-8. 2004
    ..7 nM in the binding assay. In addition, compound 11A was shown to have a significantly reduced tendency to cause receptor desensitization as compared with the motilin receptor agonist ABT-229...
  2. ncbi Tetrazole based amides as growth hormone secretagogues
    James J Li
    Discovery Chemistry, Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:2536-9. 2008
    ..Among them, hydroxyl containing analog 31 displayed excellent in vivo activity by increasing plasma GH 10-fold in an anesthetized IV rat model...
  3. ncbi 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors
    James J Li
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 17:3208-11. 2007
    ..13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain...
  4. ncbi Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications
    James J Li
    Discovery Chemistry, Computer Assisted Drug Design, Metabolic Disease Research, Metabolism and Pharmacokinetics, Discovery Analytical Sciences, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543 5400, USA
    J Med Chem 50:3015-25. 2007
    ..5 h. On the basis of their preclinical profiles, the SARMs in this series are expected to provide beneficial anabolic effects on muscle with minimal androgenic effects on prostate tissue...
  5. ncbi Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain
    Jun Li
    Discovery Chemistry, Bristol Myers Squibb, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 18:1825-9. 2008
    ..A series of ortho-substituted compounds were synthesized with improved in-vitro and in-vivo activity. Among them, the biphenyl compound 2p shows twofold improvement in potency compared to its parent compound BMS-317180 (2)...
  6. ncbi Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180)
    Jun Li
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543, USA
    J Med Chem 50:5890-3. 2007
    ..Compound 2 is a potent, novel, orally effective GHS that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development...
  7. ncbi Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)
    Haixia Wang
    Research and Development, Bristol Myers Squibb, PO Box 5400, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 21:4146-9. 2011
    ..Optimization of substituents at the 3 and 8 position of the TZP core, with a special focus on enhancing metabolic stability, resulted in the identification of compound 38 as a potent and metabolically stable inhibitor of the enzyme...
  8. ncbi Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
    Haixia Wang
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:3168-72. 2008
    ..On the distal aryl group, a number of substitutions are well tolerated. A crystal structure was obtained for a complex between 11beta-HSD1 and the most potent inhibitor in this series...
  9. ncbi A synthesis of N-bridged 5,6-bicylic pyridines via a mild cyclodehydration using the burgess reagent and discovery of a novel carbamylsulfonylation reaction
    Jie Jack Li
    Discovery Chemistry, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    Org Lett 10:2897-900. 2008
    ..A novel addition product was observed between the resulting pyrrolo- or imidazopyridine and an additional equivalent of the Burgess reagent, producing the corresponding sulfonylcarbamate adduct...
  10. ncbi Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues
    James J Li
    Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 15:1799-802. 2005
    ..Among them, carbamate 12a-E2 displays excellent in vivo activity by increasing plasma GH 10-fold in an anesthetized IV rat model...
  11. ncbi Cofactor-specific modulation of 11beta-hydroxysteroid dehydrogenase 1 inhibitor potency
    Bhavana Sahni Arya
    Department of Chemical Enzymology, Bristol Myers Squibb, 311 Pennington Rocky Hill Rd, Pennington, NJ 08534, USA
    Biochim Biophys Acta 1774:1184-91. 2007
    ..This selectivity may translate to differences in the in vivo effects of 11beta-hydroxysteroid dehydrogenase 1 inhibitors...