Richard J Hazen

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV
    Richard Hazen
    Department of Virology, GlaxoSmithKline, 5 Moore Dr, P O Box 13398, Research Triangle Park, NC 27709, USA
    Antimicrob Agents Chemother 51:3147-54. 2007
  2. ncbi Anti-human immunodeficiency virus type 1 activity of the nonnucleoside reverse transcriptase inhibitor GW678248 in combination with other antiretrovirals against clinical isolate viruses and in vitro selection for resistance
    Richard J Hazen
    Department of Virology, Metabolic and Viral Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Dr, P O Box 13398, Research Triangle Park, North Carolina 27709, USA
    Antimicrob Agents Chemother 49:4465-73. 2005
  3. ncbi Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor
    Karen R Romines
    GlaxoSmithKline Inc, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 49:727-39. 2006
  4. ncbi Antiviral activity of GW678248, a novel benzophenone nonnucleoside reverse transcriptase inhibitor
    Robert G Ferris
    Department of Virology, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Antimicrob Agents Chemother 49:4046-51. 2005
  5. ncbi Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2
    George A Freeman
    GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 47:5923-36. 2004
  6. ncbi Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors
    Ronald G Sherrill
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 15:3560-4. 2005
  7. ncbi Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 15:3496-500. 2005
  8. ncbi Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 16:1788-94. 2006
  9. ncbi Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitors
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 52:2754-61. 2009
  10. ncbi Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1
    Joseph H Chan
    GlaxoSmithKline Inc, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 47:1175-82. 2004

Detail Information

Publications20

  1. ncbi In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV
    Richard Hazen
    Department of Virology, GlaxoSmithKline, 5 Moore Dr, P O Box 13398, Research Triangle Park, NC 27709, USA
    Antimicrob Agents Chemother 51:3147-54. 2007
    ..Brecanavir is by a substantial margin the most potent and broadly active antiviral agent among the PIs tested in vitro...
  2. ncbi Anti-human immunodeficiency virus type 1 activity of the nonnucleoside reverse transcriptase inhibitor GW678248 in combination with other antiretrovirals against clinical isolate viruses and in vitro selection for resistance
    Richard J Hazen
    Department of Virology, Metabolic and Viral Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Dr, P O Box 13398, Research Triangle Park, North Carolina 27709, USA
    Antimicrob Agents Chemother 49:4465-73. 2005
    ....
  3. ncbi Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor
    Karen R Romines
    GlaxoSmithKline Inc, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 49:727-39. 2006
    ..Compound 70h has also demonstrated relatively low clearance in intravenous pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clinical studies...
  4. ncbi Antiviral activity of GW678248, a novel benzophenone nonnucleoside reverse transcriptase inhibitor
    Robert G Ferris
    Department of Virology, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Antimicrob Agents Chemother 49:4046-51. 2005
    ..This compound exhibits excellent preclinical antiviral properties and, as a prodrug designated GW695634, is being developed as a new generation of NNRTI for the treatment of HIV-1 in combination with other antiretroviral agents...
  5. ncbi Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2
    George A Freeman
    GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 47:5923-36. 2004
    ..Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors...
  6. ncbi Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors
    Ronald G Sherrill
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 15:3560-4. 2005
    ..A series of novel N-alkoxy-arylsulfonamide HIV protease inhibitors with low picomolar enzyme activity and single digit nanomolar antiviral activity is disclosed...
  7. ncbi Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 15:3496-500. 2005
    ..In addition, a number of compounds in this series were more potent against the drug-resistant mutant viruses than they were against wild-type virus...
  8. ncbi Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 16:1788-94. 2006
    ..Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385...
  9. ncbi Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitors
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 52:2754-61. 2009
    ..Pharmacokinetic data in rats for one carboxamide analogue demonstrated oral bioavailability and reasonable in vivo clearance...
  10. ncbi Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1
    Joseph H Chan
    GlaxoSmithKline Inc, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 47:1175-82. 2004
    ..The antiviral data together with the favorable pharmacokinetic data of GW4511 suggested that these benzophenones possess attributes of a new NNRTI drug candidate...
  11. ncbi The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral
    Edward P Garvey
    Department of Virology, RC2 3983, GlaxoSmithKline, 5 Moore Dr, Research Triangle Park, NC 27709 3398, USA
    Antimicrob Agents Chemother 52:901-8. 2008
    ..Thus, based on all the data, GSK364735 exerted potent antiviral activity through the inhibition of viral DNA integration by interacting at the two-metal binding site within the catalytic center of HIV integrase...
  12. ncbi Relative anti-HIV-1 efficacy of lamivudine and emtricitabine in vitro is dependent on cell type
    Richard Hazen
    Department of Virology, GlaxoSmithKline, Research Triange Park, North Carolina 27709, USA
    J Acquir Immune Defic Syndr 32:255-8. 2003
    ....
  13. ncbi Phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine and related nucleosides with potent activity against HIV and HBV
    Kristjan S Gudmundsson
    Division of Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA
    Nucleosides Nucleotides Nucleic Acids 22:1953-61. 2003
    ..Especially marked was the improvement in potency of phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine against both HIV and HBV...
  14. ncbi Phosphoramidate protides of carbocyclic 2',3'-dideoxy-2',3'-didehydro-7-deazaadenosine with potent activity against HIV and HBV
    Kristjan S Gudmundsson
    Division of Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina, USA
    Nucleosides Nucleotides Nucleic Acids 23:1929-37. 2004
    ..Several of these protides showed significantly improved antiviral potency over the parent nucleosides against both HIV and HBV...
  15. ncbi Lack of antagonism between abacavir, lamivudine, and tenofovir against wild-type and drug-resistant HIV-1
    E Randall Lanier
    GlaxoSmithKline, Research Triangle Park, NC 27705, USA
    J Acquir Immune Defic Syndr 39:519-22. 2005
    ..Antagonistic interactions were not detected for any combination. If the systems examined accurately reflect the in vivo situation, antagonism does not substantially contribute to the poor efficacy of this triple combination...
  16. ncbi Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 14:959-63. 2004
    ..In addition, significant improvements in antiviral potencies against wild type and the two mutant viruses were also realized...
  17. ncbi Optimization of pyrrolidinone based HIV protease inhibitors
    Ronald G Sherrill
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 15:81-4. 2005
    ..Optimization of P1-substituted pyrrolidinone based HIV protease inhibitors has yielded analogs with very potent antiviral activity...
  18. ncbi Small molecule modulators of HIV Rev/Rev response element interaction identified by random screening
    Richard L Chapman
    Department of Molecular Screening, GlaxoSmithKline, PO Box 1-3398, Research Triangle Park, NC 27709-3398, USA
    Antiviral Res 54:149-62. 2002
    ..Thus, small molecules can modulate this macromolecular protein-RNA interaction in vitro. However, no compound demonstrated HIV antiviral activity in a relevant cell-based assay...
  19. ncbi Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1
    Andrew L Hopkins
    Division of Structural Biology, The Wellcome Trust Centre for Human Genetics, University of Oxford, Roosevelt Drive, Oxford, OX3 7BN, UK
    J Med Chem 47:5912-22. 2004
    ..Members of this quinolone series retain high activity against the important resistance mutations in RT at Tyr181Cys and Leu100Ile...
  20. ncbi Synthesis of potential anti-HIV GP120 inhibitors using a lysine template
    Valerie E Doyl
    J Enzyme Inhib Med Chem 17:175-82. 2002
    ..Compounds were assayed against HIV-infected C8166 cells and some showed weak anti-HIV activity...