Glenn Noronha

Summary

Affiliation: TargeGen Inc
Country: USA

Publications

  1. ncbi request reprint Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors
    Glenn Noronha
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:5546-50. 2006
  2. ncbi request reprint Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays
    Glenn Noronha
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:602-8. 2007
  3. ncbi request reprint Inhibitors of ABL and the ABL-T315I mutation
    Glenn Noronha
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Curr Top Med Chem 8:905-21. 2008
  4. doi request reprint Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degener
    Moorthy S S Palanki
    TargeGen Inc, 9890 Judicial Drive, San Diego, CA 92121, USA
    J Med Chem 51:1546-59. 2008
  5. ncbi request reprint The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes
    Jianguo Cao
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:5812-8. 2007
  6. ncbi request reprint Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease
    John Doukas
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 328:758-65. 2009
  7. ncbi request reprint Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction
    Moorthy S S Palanki
    TargeGen Inc, 9380 Judicial Drive, San Diego California 92121, USA
    J Med Chem 50:4279-94. 2007
  8. pmc Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema
    John Doukas
    TargeGen, Inc, San Diego, California
    J Cell Physiol 216:29-37. 2008
  9. ncbi request reprint Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methy
    Steven X Hu
    TargeGen, Inc, San Diego, CA 92121, USA
    Drug Metab Dispos 35:929-36. 2007
  10. doi request reprint Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors
    Ifat Geron
    Department of Medicine, University of California, San Diego, La Jolla, CA 92093, USA
    Cancer Cell 13:321-30. 2008

Collaborators

Detail Information

Publications13

  1. ncbi request reprint Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors
    Glenn Noronha
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:5546-50. 2006
    ..To the best of our knowledge, benzotriazine template based compounds have not been reported as kinase inhibitors. The 3-(2-(1-pyrrolidinyl)ethoxy)phenyl analogue (43) was identified as one of the most potent inhibitors of Src kinase...
  2. ncbi request reprint Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays
    Glenn Noronha
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:602-8. 2007
    ....
  3. ncbi request reprint Inhibitors of ABL and the ABL-T315I mutation
    Glenn Noronha
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Curr Top Med Chem 8:905-21. 2008
    ..The success of these inhibitors has greater implication not only in CML, but also in other diseases driven by kinases where the mutated gatekeeper residue plays a major role...
  4. doi request reprint Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degener
    Moorthy S S Palanki
    TargeGen Inc, 9890 Judicial Drive, San Diego, CA 92121, USA
    J Med Chem 51:1546-59. 2008
    ..On the basis of its superior profile, compound 12 was advanced. It is currently in a clinical trial as a first in class, VEGFr2 targeting, topically applied compound for the treatment of AMD...
  5. ncbi request reprint The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes
    Jianguo Cao
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:5812-8. 2007
    ..This designed interaction provides an advantage in overcoming the challenges arising from the T315I mutation of Abl and transforms poor (ca. 10 microM) inhibitors into those with low nM potency...
  6. ncbi request reprint Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease
    John Doukas
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 328:758-65. 2009
    ..Furthermore, these studies support the hypothesis that PI3K delta and gamma are suitable molecular targets for these diseases...
  7. ncbi request reprint Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction
    Moorthy S S Palanki
    TargeGen Inc, 9380 Judicial Drive, San Diego California 92121, USA
    J Med Chem 50:4279-94. 2007
    ..The structure-activity relationship studies of various analogues of diaminopteridine-diphenol-based on biochemical assays resulted in potent inhibitors of PI3K...
  8. pmc Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema
    John Doukas
    TargeGen, Inc, San Diego, California
    J Cell Physiol 216:29-37. 2008
    ..These data suggest that TG100801 may provide a new topically applied treatment approach for ocular neovascularization and retinal edema...
  9. ncbi request reprint Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methy
    Steven X Hu
    TargeGen, Inc, San Diego, CA 92121, USA
    Drug Metab Dispos 35:929-36. 2007
    ....
  10. doi request reprint Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors
    Ifat Geron
    Department of Medicine, University of California, San Diego, La Jolla, CA 92093, USA
    Cancer Cell 13:321-30. 2008
    ..Thus, TG101348 may be an effective inhibitor of JAK2V617F+ MPDs in clinical trials...
  11. pmc Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury
    John Doukas
    TargeGen, Inc, 9380 Judicial Drive, San Diego, CA 92121, USA
    Proc Natl Acad Sci U S A 103:19866-71. 2006
    ..In conclusion, by targeting pathologic events occurring relatively late in myocardial damage, we have identified a potential means of addressing an elusive clinical goal: meaningful cardioprotection in the postreperfusion time period...
  12. ncbi request reprint Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera
    Gerlinde Wernig
    Division of Hematology, Department of Medicine, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
    Cancer Cell 13:311-20. 2008
    ....
  13. pmc Retinal vascular permeability suppression by topical application of a novel VEGFR2/Src kinase inhibitor in mice and rabbits
    Lea Scheppke
    Department of Cell Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    J Clin Invest 118:2337-46. 2008
    ....