Jianming Bao

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Novel fragmentation reaction of correolide
    Jianming Bao
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
    Org Lett 4:1871-3. 2002
  2. ncbi request reprint Benzamide derivatives as blockers of Kv1.3 ion channel
    Shouwu Miao
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 13:1161-4. 2003
  3. ncbi request reprint Potent Kv1.3 inhibitors from correolide-modification of the C18 position
    Jianming Bao
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:447-51. 2005
  4. ncbi request reprint p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones
    Jianming Bao
    Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:64-8. 2006
  5. doi request reprint Tetrahydroindolizinone NK1 antagonists
    Jianming Bao
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:2354-8. 2010
  6. ncbi request reprint Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties
    William A Schmalhofer
    Department of Ion Channels, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Biochemistry 41:7781-94. 2002
  7. doi request reprint 2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways
    Andrew J Kassick
    Discovery Chemistry, In Vitro Pharmacology, Drug Metabolism, and Laboratory Animal Resources, Merck Research Laboratories, Merck and Co, Rahway, New Jersey 07065, United States
    J Med Chem 56:5940-8. 2013

Collaborators

Detail Information

Publications7

  1. ncbi request reprint Novel fragmentation reaction of correolide
    Jianming Bao
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
    Org Lett 4:1871-3. 2002
    ..A mechanism involving a retroaldol reaction, a nucleophilic opening of the epoxide, and a subsequent acetoxy elimination reaction was proposed...
  2. ncbi request reprint Benzamide derivatives as blockers of Kv1.3 ion channel
    Shouwu Miao
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 13:1161-4. 2003
    ..In in vitro assays, trans isomers display moderate selectivity for binding to Kv1.3 over other Kv1.x channels present in human brain...
  3. ncbi request reprint Potent Kv1.3 inhibitors from correolide-modification of the C18 position
    Jianming Bao
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:447-51. 2005
    ..The most potent analog 43 is 15-fold more potent than correolide as inhibitor of human T cell proliferation...
  4. ncbi request reprint p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones
    Jianming Bao
    Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:64-8. 2006
    ..They also displayed excellent PK profiles across three animal species. Quinolinone at 10 mpk showed comparable oral efficacy to that of dexamethasone at 1 mpk in a murine collagen-induced arthritis model...
  5. doi request reprint Tetrahydroindolizinone NK1 antagonists
    Jianming Bao
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:2354-8. 2010
    ..Compound 40 has high NK(1) binding affinity, good selectivity for other NK receptors and promising in vivo properties. It also has clean P(450) inhibition and hPXR induction profiles...
  6. ncbi request reprint Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties
    William A Schmalhofer
    Department of Ion Channels, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Biochemistry 41:7781-94. 2002
    ..3 channel inhibitors useful for the safe treatment of autoimmune diseases...
  7. doi request reprint 2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways
    Andrew J Kassick
    Discovery Chemistry, In Vitro Pharmacology, Drug Metabolism, and Laboratory Animal Resources, Merck Research Laboratories, Merck and Co, Rahway, New Jersey 07065, United States
    J Med Chem 56:5940-8. 2013
    ..In preclinical species, compound 3 has demonstrated potency, brain penetration, and a safety profile similar to 2, as well as excellent pharmacokinetics. ..