Bristol-Myers Squibb

Summary

Organization: Bristol-Myers Squibb
Country: USA

Top Publications

  1. ncbi Investigation into the degree of variability in the solid-state properties of common pharmaceutical excipients-anhydrous lactose
    John F Gamble
    Exploratory Biopharmaceutics R and D, Bristol Myers Squibb, Reeds Lane, Moreton, Wirral, CH46 1QW, UK
    AAPS PharmSciTech 11:1552-7. 2010
  2. ncbi Beam me up Scotty: incorporating transporters in physiologically based pharmacokinetic-pharmacodynamic modeling
    Lois D Lehman-McKeeman
    Department of Discovery Toxicology, Bristol-Myers Squibb Co, Route 206, Province Line Road, Princeton, New Jersey 08543, USA
    Toxicol Sci 104:1-3. 2008
  3. ncbi Economic implications of entecavir treatment in suppressing viral replication in chronic hepatitis B (CHB) patients in China from a perspective of the Chinese Social Security program
    Yong Yuan
    Pharmaceutical Research Institute, Bristol Myers Squibb Company, Princeton, NJ 08543 4000, USA
    Value Health 11:S11-22. 2008
  4. ncbi Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase
    Gretchen M Schroeder
    Bristol Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 18:1945-51. 2008
  5. ncbi Amino Acid derived enamides: synthesis and aminopeptidase activity
    Richard R Cesati
    Pharmaceutical Research and Development, Bristol Myers Squibb Medical Imaging, North Billerica, Massachusetts 01862, USA
    Org Lett 9:5617-20. 2007
  6. ncbi An investigation of the thermodynamic miscibility between VeTPGS and polymers
    Jinjiang Li
    Department of Pharmaceutics, Boehringer Ingelheim Pharmaceuticals Inc, Ridgefield, CT 06887, USA
    Int J Pharm 350:212-9. 2008
  7. ncbi Urine acidification has no effect on peroxisome proliferator-activated receptor (PPAR) signaling or epidermal growth factor (EGF) expression in rat urinary bladder urothelium
    William E Achanzar
    Department of Drug Safety Evaluation, Bristol Myers Squibb Co, New Brunswick, NJ 08903, USA
    Toxicol Appl Pharmacol 223:246-56. 2007
  8. ncbi Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419)
    Scott H Watterson
    Bristol Myers Squibb Pharmaceutical Research Institute, Post Office Box 4000, Princeton, New Jersey 08543, USA
    J Med Chem 50:3730-42. 2007
  9. ncbi Development of an in silico model for predicting efflux substrates in Caco-2 cells
    Litai Zhang
    Bristol Myers Squibb Company PRI, Route 206 and Provinceline Road, P O Box 4000, Princeton, NJ 08543, USA
    Int J Pharm 343:98-105. 2007
  10. ncbi Respiratory syncytial virus fusion inhibitors. Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity
    Xiangdong Alan Wang
    Department of Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 17:4592-8. 2007

Detail Information

Publications62

  1. ncbi Investigation into the degree of variability in the solid-state properties of common pharmaceutical excipients-anhydrous lactose
    John F Gamble
    Exploratory Biopharmaceutics R and D, Bristol Myers Squibb, Reeds Lane, Moreton, Wirral, CH46 1QW, UK
    AAPS PharmSciTech 11:1552-7. 2010
    ....
  2. ncbi Beam me up Scotty: incorporating transporters in physiologically based pharmacokinetic-pharmacodynamic modeling
    Lois D Lehman-McKeeman
    Department of Discovery Toxicology, Bristol-Myers Squibb Co, Route 206, Province Line Road, Princeton, New Jersey 08543, USA
    Toxicol Sci 104:1-3. 2008
  3. ncbi Economic implications of entecavir treatment in suppressing viral replication in chronic hepatitis B (CHB) patients in China from a perspective of the Chinese Social Security program
    Yong Yuan
    Pharmaceutical Research Institute, Bristol Myers Squibb Company, Princeton, NJ 08543 4000, USA
    Value Health 11:S11-22. 2008
    ....
  4. ncbi Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase
    Gretchen M Schroeder
    Bristol Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 18:1945-51. 2008
    ..Acylurea pyrrolotriazines with substitution at C-5 demonstrated single digit nanomolar kinase activity. X-ray crystallography revealed that the C-5 substituted pyrrolotriazines bind to the Met kinase domain in an ATP-competitive manner...
  5. ncbi Amino Acid derived enamides: synthesis and aminopeptidase activity
    Richard R Cesati
    Pharmaceutical Research and Development, Bristol Myers Squibb Medical Imaging, North Billerica, Massachusetts 01862, USA
    Org Lett 9:5617-20. 2007
    ..Assessment of aminopeptidase activity revealed a preference for (E)-1,2-disubstituted constructs...
  6. ncbi An investigation of the thermodynamic miscibility between VeTPGS and polymers
    Jinjiang Li
    Department of Pharmaceutics, Boehringer Ingelheim Pharmaceuticals Inc, Ridgefield, CT 06887, USA
    Int J Pharm 350:212-9. 2008
    ..Results suggest that the miscibility between VeTPGS and PMMA is very likely due to a specific interaction between the hydrophobic portion of VeTPGS (Vitamin E) and PMMA...
  7. ncbi Urine acidification has no effect on peroxisome proliferator-activated receptor (PPAR) signaling or epidermal growth factor (EGF) expression in rat urinary bladder urothelium
    William E Achanzar
    Department of Drug Safety Evaluation, Bristol Myers Squibb Co, New Brunswick, NJ 08903, USA
    Toxicol Appl Pharmacol 223:246-56. 2007
    ..These results support the contention that urine acidification does not prevent PPARgamma agonist-induced bladder tumors by altering PPARalpha, gamma, or EGFR expression or PPAR signaling in rat bladder urothelium...
  8. ncbi Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419)
    Scott H Watterson
    Bristol Myers Squibb Pharmaceutical Research Institute, Post Office Box 4000, Princeton, New Jersey 08543, USA
    J Med Chem 50:3730-42. 2007
    ..This article will detail the discovery and SAR leading to a novel and potent acridone-based IMPDH inhibitor 4m and its efficacy and GI tolerability when administered orally in a rat adjuvant arthritis model...
  9. ncbi Development of an in silico model for predicting efflux substrates in Caco-2 cells
    Litai Zhang
    Bristol Myers Squibb Company PRI, Route 206 and Provinceline Road, P O Box 4000, Princeton, NJ 08543, USA
    Int J Pharm 343:98-105. 2007
    ....
  10. ncbi Respiratory syncytial virus fusion inhibitors. Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity
    Xiangdong Alan Wang
    Department of Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 17:4592-8. 2007
    ....
  11. ncbi Basic science for the clinician 43: the mitogen-activated protein kinase family in inflammatory signaling
    Leonard H Sigal
    Pharmaceutical Research Institute, Bristol Myers Squibb, Princeton, New Jersey 08543 4000, USA
    J Clin Rheumatol 13:96-9. 2007
    ..The human "kinome" (the various families of kinases) is very complex; we will limit ourselves in this discussion to the mitogen-activated protein kinases...
  12. ncbi Effect of DPC 333 [(2R)-2-{(3R)-3-amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide], a human tumor necrosis factor alpha-converting enzyme inhibitor, on the disposition of methotrexate: a transporter-bas
    Gang Luo
    Bristol Myers Squibb Company, Pennington, NJ 08534, USA
    Drug Metab Dispos 35:835-40. 2007
    ..These results suggest that the enhanced renal elimination of MTX may be due to the potent inhibition of biliary excretion and active renal reabsorption by DPC 333 and/or its metabolites...
  13. ncbi A simple strategy for mitigating the effect of data variability on the identification of active chemotypes from high-throughput screening data
    Stephen R Johnson
    Pharmaceutical Research Institute, Bristol Myers Squibb, Princeton, NJ 08543 4000, USA
    J Biomol Screen 12:276-84. 2007
    ..The individual steps of the Monte Carlo simulation provide insight into the correspondence between the percentage inhibition and eventual IC(50) curves...
  14. ncbi Use of cryopreserved transiently transfected cells in high-throughput pregnane X receptor transactivation assay
    Zhengrong Zhu
    Bristol Myers Squibb Company, Wallingford, CT 06492, USA
    J Biomol Screen 12:248-54. 2007
    ..In addition, cryopreserved HepG2 cells did not exhibit enhanced susceptibility to cytotoxic compounds compared to transiently transfected control cells. The use of cryopreserved cells enables this assay to run with enhanced efficiency...
  15. ncbi Current methods for predicting human food effect
    Kimberley A Lentz
    Pharmaceutical Candidate Optimization Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT, 06492 7660, USA
    AAPS J 10:282-8. 2008
    ....
  16. ncbi Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa
    Jennifer X Qiao
    Bristol Myers Squibb Company, Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 18:4118-23. 2008
    ..The potential structural basis for the high FXa potency in the phenylcyclopropyl P4 analogs and their improved FXa inhibitory activities compared with the biphenyl P4 counterparts are discussed...
  17. ncbi Therapeutic strategies for Alzheimer's disease
    Donna M Barten
    Bristol Myers Squibb, Neuroscience Drug Discovery, 5 Research Parkway, Wallingford, CT 06492, USA
    Mol Neurobiol 37:171-86. 2008
    ..In summary, plaques, tangles, neurodegeneration and dementia guide the development of multiple therapeutic approaches for AD and are the subject of this review...
  18. ncbi Morphological score assignment guidelines for the dechorionated zebrafish teratogenicity assay
    Julieta M Panzica-Kelly
    Discovery Toxicology, Bristol Myers Squibb Company, Princeton, New Jersey 08534, USA
    Birth Defects Res B Dev Reprod Toxicol 89:382-95. 2010
    ..2010: Birth Defects Res 89:66-77)...
  19. ncbi Smoothened antagonists for hair inhibition
    Jie Jack Li
    Department of Chemistry, Michigan Laboratories, Pfizer Global Research and Development, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 20:4932-5. 2010
    ....
  20. ncbi Is a distinctive single Tg a reliable indicator for the homogeneity of amorphous solid dispersion?
    Feng Qian
    Biopharmaceutics R and D, Bristol Myers Squibb Company, One Squibb Drive, 105 2 1A, New Brunswick, NJ 08903, USA
    Int J Pharm 395:232-5. 2010
    ....
  21. ncbi Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453)
    Jun Li
    Metabolic Diseases Chemistry, Bristol Myers Squibb, Building 13, P O Box 5400, Princeton, New Jersey 08543 5400, USA
    J Med Chem 53:2854-64. 2010
    ..The role of the crystal structure of compound 12 with PPARalpha in the development of the SAR that ultimately resulted in the discovery of compound 2 is discussed...
  22. ncbi An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis
    Suzanne J Suchard
    Department of Immunology and Inflammation Drug Discovery, Bristol Myers Squibb, Princeton, NJ 08543, USA
    J Immunol 184:3917-26. 2010
    ..These findings support the potential use of an LFA-1 small-molecule antagonist in rheumatoid arthritis, with the capacity for disease modification...
  23. ncbi Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents
    Saleem Ahmad
    Research and Development, Bristol Myers Squibb Co, PO Box 4000, Princeton, NJ 08543, United States
    Bioorg Med Chem Lett 20:1128-33. 2010
    ..Among these, compounds (+)-2a and (+)-3c were identified as potent and highly selective agonists which exhibited weight loss in a rat model upon oral dosing...
  24. ncbi Dihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists
    John Lloyd
    Bristol Myers Squibb, Pharmaceutical Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 19:5469-73. 2009
    ..5 block of 0.030muM without significant block of other cardiac ion channels. This compound also showed good bioavailability in rats and robust pharmacodynamic effects in a rabbit model...
  25. ncbi Cost-effectiveness analysis of entecavir versus lamivudine in the first-line treatment of Australian patients with chronic hepatitis B
    Elizabeth Arnold
    Bristol Myers Squibb Australia, Melbourne, Victoria, Australia
    Appl Health Econ Health Policy 6:231-46. 2008
    ..The recent introduction of entecavir in Australia for the treatment of CHB patients in the naive treatment setting has triggered significant optimism with regards to improved clinical outcomes for CHB patients...
  26. ncbi New approaches for inhibiting HIV integrase: a journey beyond the active site
    Michael A Walker
    Bristol Myers Squibb, Virology Chemistry, Wallingford, CT 06492, USA
    Curr Opin Investig Drugs 10:129-36. 2009
    ..The second site was identified by the selective covalent trapping of pyridoxal phosphate to the C-terminal domain of the enzyme. The targeting of these sites as a potential novel approach for inhibiting HIV IN is reviewed...
  27. ncbi Enhancement of oral bioavailability of an HIV-attachment inhibitor by nanosizing and amorphous formulation approaches
    Michael G Fakes
    Biopharmaceutics R and D, Bristol Myers Squibb, 1 Squibb Drive, P O Box 191, New Brunswick, NJ 08903 0191, USA
    Int J Pharm 370:167-74. 2009
    ....
  28. ncbi TEMPOL, a membrane-permeable radical scavenger, attenuates gastric mucosal damage induced by ischemia/reperfusion: a key role for superoxide anion
    Dalaal M Abdallah
    Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Cairo, Egypt
    Eur J Pharmacol 603:93-7. 2009
    ..Therefore, specific SOD mimetics could be beneficial as complementary agents in the management of gastric ulceration...
  29. ncbi Pulmonary delivery of a GLP-1 receptor agonist, BMS-686117
    Feng Qian
    Biopharmaceutics Research and Development, Bristol Myers Squibb Company, New Brunswick, NJ 08903, USA
    Int J Pharm 366:218-20. 2009
    ..This study demonstrated that pulmonary delivery is a promising, non-invasive route for the administration of BMS-686117...
  30. ncbi Raman spectroscopic and visible absorption investigation of LiCrSi2O6 pyroxene under pressure
    C J S Pommier
    Pharmaceutical Research Institute, Bristol Myers Squibb, PO Box 191, New Brunswick, New Jersey 08903 0191, USA
    Appl Spectrosc 62:766-72. 2008
    ..Comparison is made with the Raman spectra of LiAlSi2O6 and LiFeSi2O6 in the P21/c phase and the visible spectra of NaCrSi2O6 at high pressures...
  31. ncbi Modeling and active site refinement for G protein-coupled receptors: application to the beta-2 adrenergic receptor
    Stanley R Krystek
    Department of Molecular Biosciences, Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
    J Comput Aided Mol Des 20:463-70. 2006
    ..The modeling protocol enables an ensemble approach to binding mode prediction. The utility of models for beta-2 adrenergic receptor will be discussed...
  32. ncbi A comparative study of available software for high-accuracy homology modeling: from sequence alignments to structural models
    Akbar Nayeem
    Computer Assisted Drug Design, Pharmaceutical Research Institute, Bristol Myers Squibb, Princeton, New Jersey 08543, USA
    Protein Sci 15:808-24. 2006
    ..Additionally, we note that DSModeler and MOE, which generate reasonable models for sequence identities >25%, are significantly more functional and easier to use when compared with the other structure-building software...
  33. ncbi Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase
    Scott H Watterson
    Bristol Myers Squibb PRI, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:2879-82. 2002
    ..A series of novel amide-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described...
  34. ncbi Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities
    Kyoung Soon Kim
    Department of Oncology Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543 4000, USA
    J Med Chem 45:3905-27. 2002
    ....
  35. ncbi 99mTc-Labeling of a hydrazinonicotinamide-conjugated LTB(4) receptor antagonist useful for imaging infection and inflammation
    Shuang Liu
    Bristol Myers Squibb Medical Imaging, 331 Treble Cove Road, North Billerica, Massachusetts 01862, USA
    Bioconjug Chem 13:881-6. 2002
    ..The LC-MS data are completely consistent with the 1:1:1:1 composition for Tc:SG380:tricine:TPPTS...
  36. ncbi CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships
    Dean A Wacker
    Bristol Myers Squibb Company, Experimental Station, PO Box 80336, Wilmington, DE 19880 0336, USA
    Bioorg Med Chem Lett 12:1785-9. 2002
    ....
  37. ncbi Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides
    Natesan Murugesan
    Department of Chemistry, Cardiovascular Agents, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 12:517-20. 2002
    ..Among the analogues examined, the pyrimidine derivative 18 is the most potent (K(i)=0.9 nM) and selective for the ET(A) receptor, approximately equivalent to 1...
  38. ncbi The inhibition and selectivity of bacterial topoisomerases by BMS-284756 and its analogues
    L E Lawrence
    Bristol Myers Squibb Pharmaceutical Research Institute, Infectious Diseases, Department of Microbiology, 5 Research Parkway, Wallingford, CT 06492, USA
    J Antimicrob Chemother 48:195-201. 2001
    ..BMS-284756 demonstrated greater Gram-positive antibacterial activity and similar inhibition of targets compared with other fluoroquinolones, and more favourable selectivity compared with the other BMS-284756 analogues...
  39. ncbi Sensitivity and tolerance to ethanol in mouse lines selected for ethanol-induced hypothermia
    K E Browman
    Portland Alcohol Research Center, Department of Veterans Affairs Medical Center, 3710 Southwest US Veterans Hospital Road, Portland, OR 97201, USA
    Pharmacol Biochem Behav 67:821-9. 2000
    ..All three COLD lines developed significant tolerance, while the HOT lines did not. The HOT and COLD mice provide a genetic model to study mechanisms mediating acute EtOH-induced hypothermia as well as tolerance development...
  40. ncbi Antiviral efficacy of lobucavir (BMS-180194), a cyclobutyl-guanosine nucleoside analogue, in the woodchuck (Marmota monax) model of chronic hepatitis B virus (HBV) infection
    E V Genovesi
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut, CT 06492 7660, USA
    Antiviral Res 48:197-203. 2000
    ..These results indicated that the minimally effective antiviral daily per os dose of lobucavir in WHV-carrier woodchucks was approximately 5 mg/kg...
  41. ncbi Complex adaptive systems and human health: the influence of common genotypes of the apolipoprotein E (ApoE) gene polymorphism and age on the relational order within a field of lipid metabolism traits
    K E Zerba
    Bristol Myers Squibb, Pharmaceutical Research Institute, Non Clinical Biostatistics, Princeton, NJ 08543 5400, USA
    Hum Genet 107:466-75. 2000
    ..These dynamic actions emerge as the phenotypes that are measures of human health in the population at large...
  42. ncbi Clinical pharmacology of gatifloxacin, a new fluoroquinolone
    D M Grasela
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA
    Clin Infect Dis 31:S51-8. 2000
    ..Clinical studies show that gatifloxacin has limited potential to prolong the QT interval on the electrocardiogram and lacks the potential to cause photosensitivity reactions, to alter oral glucose tolerance, or to cause crystalluria...
  43. ncbi Stavudine resistance: an update on susceptibility following prolonged therapy
    P F Lin
    Bristol Myers Squibb, Wallingford, Conn, USA
    Antivir Ther 4:21-8. 1999
    ..This low incidence of stavudine resistance is in striking contrast to that observed with other nucleoside analogues and further supports the use of stavudine in first-line combination therapy for HIV patients...
  44. ncbi BR96 sFv-PE40 immunotoxin: nonclinical safety assessment
    H G Haggerty
    Department of Drug Safety Evaluation, Bristol Myers Squibb, Syracuse, New York 13221, USA
    Toxicol Pathol 27:87-94. 1999
    ..The immunogenicity of BR96 sFv-PE40 could be inhibited by combined treatment with an immunosuppressant in dogs, thus maintaining exposure to BR96 sFv-PE40...
  45. ncbi CD6-ligand interactions: a paradigm for SRCR domain function?
    A Aruffo
    Bristol Myers Squibb Pharmaceutical Research Institute, Seattle, WA 98121, USA
    Immunol Today 18:498-504. 1997
    ..Analysis of the CD6-ALCAM interaction may help to understand how other SRCR domains bind to their ligands...
  46. ncbi BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice
    James R Burke
    Department of Immunology, Inflammation and Pulmonary Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    J Biol Chem 278:1450-6. 2003
    ..Thus, the compound is effective against NF-kappa B activation in mice and represents an important tool for investigating the role of IKK in disease models...
  47. ncbi Differentiation of Hdm2-mediated p53 ubiquitination and Hdm2 autoubiquitination activity by small molecular weight inhibitors
    Zhihong Lai
    Department of Chemical Enzymology, Bristol Myers Squibb Company, Experimental Station, Wilmington, DE 19880, USA
    Proc Natl Acad Sci U S A 99:14734-9. 2002
    ..Selective inhibitors of hdm2 E3 ligase activity could provide a novel mechanism for the development of new chemotherapeutics for the treatment of human cancers...
  48. ncbi CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine
    Argyrios G Arvanitis
    Discovery Chemistry Wilmington, Bristol Myers Squibb Company, Experimental Station, Wilmington, DE 19880, USA
    Bioorg Med Chem Lett 13:289-91. 2003
    ..Individual analogues were synthesized from key intermediates obtained via palladium-catalyzed coupling of 3-pyridyl zinc or boronic acid organometallic intermediates with 2-benzyloxy-4-chloro-3-nitropyridine 12...
  49. ncbi Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors
    Mimi L Quan
    Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 16:1795-8. 2006
    ..This approach resulted in a series of potent, selective, and orally bioavailable factor Xa inhibitors...
  50. ncbi A 96-well single-pot protein precipitation, liquid chromatography/tandem mass spectrometry (LC/MS/MS) method for the determination of muraglitazar, a novel diabetes drug, in human plasma
    Y J Xue
    Pharmaceutical Candidate Optimization, Pharmaceutical Research Institute, Bristol Myers Squibb, New Brunswick, NJ 08903, USA
    J Chromatogr B Analyt Technol Biomed Life Sci 831:213-22. 2006
    ..The method has been successfully applied to analyze human plasma samples in support of a first-in-man study. This method has also been validated in monkey and mouse plasma for the determination of muraglitazar...
  51. ncbi Grading melanocytic dysplasia in paraffin wax embedded tissue by the nucleic acid index
    D M Berman
    Laboratory of Pathology, National Cancer Institute, Bldg 10 2N212, 10 Center Drive Bethesda, MD 20896, USA
    J Clin Pathol 58:1206-10. 2005
    ..However, light microscopy is subjective and crucial genomic changes do not always show as changes in histology...
  52. ncbi Analysis of cellular events using CellCard System in cell-based high-content multiplexed assays
    Taosheng Chen
    Bristol Myers Squibb Company, Lead Discovery and Profiling, 5 Research Parkway, Wallingford, CT 06492, USA
    Expert Rev Mol Diagn 5:817-29. 2005
    ..In this technology review, the authors discuss personal experience with assay validation, data analysis, results such as cell type-specific compound effects, and the potential application of the CellCard System in drug discovery...
  53. ncbi Effects of feeding an infant formula containing Lactobacillus GG on the colonization of the intestine: a dose-response study in healthy infants
    Bryon W Petschow
    Mead Johnson Nutritionals, Evansville, IN 47721, USA
    J Clin Gastroenterol 39:786-90. 2005
    ....
  54. ncbi Solid-phase synthesis of 5-substituted amino pyrazoles
    Dharmpal S Dodd
    Early Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 4000, Princeton, New Jersey 08543 4000, USA
    J Comb Chem 7:584-8. 2005
    ....
  55. ncbi Catalytic asymmetric diazoacetate cyclopropanation of 1-tosyl-3-vinylindoles. A route to conformationally restricted homotryptamines
    Lawrence R Marcin
    Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
    Org Lett 7:2651-4. 2005
    ..The resulting cycloadducts are demonstrated to be useful intermediates for the synthesis of conformationally restricted, homotryptamine-like analogues such as BMS-505130...
  56. ncbi Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor
    Mimi L Quan
    Discovery Chemistry, Pharmaceutical Research Institute, Bristol Myers Squibb Co, P O Box 5400, Princeton, New Jersey 08543 5400, USA
    J Med Chem 48:1729-44. 2005
    ....
  57. ncbi Cell culture-based models for intestinal permeability: a critique
    Praveen V Balimane
    Department of Metabolism and Pharmacokinetics, Bristol Myers Squibb, Princeton, NJ 08543, USA
    Drug Discov Today 10:335-43. 2005
    ..Here, in addition to an objective analysis of the utility of cell culture models for permeability screening, anticipated future trends in the field of cell culture models are discussed...
  58. ncbi Creation and comparison of MS/MS spectral libraries using quadrupole ion trap and triple-quadrupole mass spectrometers
    Jonathan L Josephs
    Bristol Myers Squibb, Pharmaceutical Research Institute, New Brunswick, NJ 08543 5400, USA
    Rapid Commun Mass Spectrom 18:743-59. 2004
    ..The ability to obtain library-searchable spectra at low concentrations is demonstrated for the analysis of a sample of progesterone spiked with hydroxyprogesterone impurities at 0.1 and 0.01%...
  59. ncbi Efficient asymmetric synthesis of the vasopeptidase inhibitor BMS-189921
    Janak Singh
    Process Research and Development, The Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 4000, Princeton, New Jersey 08543, USA
    Org Lett 5:3155-8. 2003
    ..Olefin 3 was converted to 6b via asymmetric hydrogenation. Alternatively, enyne 12 was converted to racemic alpha-aminoazepinone 15b, which was transformed to 6b by a practical dynamic resolution...
  60. ncbi (S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine
    Yong Jin Wu
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Med Chem 46:3197-200. 2003
    ..In a rat model of migraine, 2 demonstrated significant oral activity in reducing the total number of cortical spreading depressions induced by potassium chloride...
  61. ncbi Validation and application of a high-performance liquid chromatography/tandem mass spectrometry assay for sumatriptan in human plasma
    David W Boulton
    Clinical Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA
    Biomed Chromatogr 17:48-52. 2003
    ..The utility of the assay was demonstrated by following sumatriptan plasma concentrations in two healthy subjects for 8-12 h following a single 20 mg intranasal dose...
  62. ncbi Characterization of a hemagglutinin-specific inhibitor of influenza A virus
    G Luo
    Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
    Virology 226:66-76. 1996
    ..These experiments further illustrate that the hemagglutinin protein of influenza virus is a viable target for the discovery and development of small molecule inhibitors of virus growth...