YIFENG XIONG

Summary

Affiliation: Arena Pharmaceuticals
Country: USA

Publications

  1. ncbi Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia
    YIFENG XIONG
    Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 22:1870-3. 2012
  2. ncbi Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis
    YIFENG XIONG
    Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
    J Med Chem 53:4412-21. 2010
  3. ncbi Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia
    YIFENG XIONG
    Arena Pharmaceuticals, San Diego, California 92121, USA
    J Med Chem 53:5696-706. 2010
  4. ncbi Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control
    Graeme Semple
    Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:3134-41. 2011
  5. ncbi APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology
    John W Adams
    Arena Pharmaceuticals, Inc, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 331:96-103. 2009
  6. ncbi Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents
    Peter I Dosa
    Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, United States
    Bioorg Med Chem Lett 19:5486-9. 2009
  7. ncbi 5-HT(2A) inverse-agonists for the treatment of insomnia
    Bradley R Teegarden
    Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Curr Top Med Chem 8:969-76. 2008
  8. ncbi Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
    Graeme Semple
    Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
    J Med Chem 51:5172-5. 2008

Detail Information

Publications8

  1. ncbi Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia
    YIFENG XIONG
    Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 22:1870-3. 2012
    ..Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation...
  2. ncbi Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis
    YIFENG XIONG
    Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
    J Med Chem 53:4412-21. 2010
    ..10k was orally bioavailable in rats, dogs, and monkeys and had an acceptable safety profile. As a result, 10k was selected further evaluation and advanced into clinical development as a potential treatment for arterial thrombosis...
  3. ncbi Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia
    YIFENG XIONG
    Arena Pharmaceuticals, San Diego, California 92121, USA
    J Med Chem 53:5696-706. 2010
    ..In vivo, these two compounds showed dose-dependent, statistically significant improvements on deep sleep (delta power) and sleep consolidation at doses as low as 0.1 mg/kg...
  4. ncbi Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control
    Graeme Semple
    Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:3134-41. 2011
    ..As a result of these and other data described here, 3k (APD668, JNJ-28630368) was the first compound with this mechanism of action to be progressed into clinical development for the treatment of diabetes...
  5. ncbi APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology
    John W Adams
    Arena Pharmaceuticals, Inc, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 331:96-103. 2009
    ..These results demonstrate that APD791 is an orally available, high-affinity 5-HT(2A) receptor antagonist with potent activity on platelets and vascular smooth muscle...
  6. ncbi Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents
    Peter I Dosa
    Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, United States
    Bioorg Med Chem Lett 19:5486-9. 2009
    ..Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation...
  7. ncbi 5-HT(2A) inverse-agonists for the treatment of insomnia
    Bradley R Teegarden
    Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Curr Top Med Chem 8:969-76. 2008
    ....
  8. ncbi Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
    Graeme Semple
    Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
    J Med Chem 51:5172-5. 2008
    ..Compound 8g showed in vivo activity in rodents and was active in an oral glucose tolerance test in mice following oral administration...