Anne B Eldrup

Summary

Affiliation: Boehringer Ingelheim

Publications

  1. doi request reprint Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase
    Anne B Eldrup
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Ridgefield, Connecticut 06877, USA
    J Med Chem 52:5880-95. 2009
  2. doi request reprint Optimization of piperidyl-ureas as inhibitors of soluble epoxide hydrolase
    Anne B Eldrup
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Ridgefield, CT 06877, United States
    Bioorg Med Chem Lett 20:571-5. 2010
  3. doi request reprint Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase
    Steven J Taylor
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, 900 Ridgebury Rd PO Box 368, Ridgefield, CT 06877 036, USA
    Bioorg Med Chem Lett 19:5864-8. 2009
  4. ncbi request reprint Synthesis and evaluation of S-acyl-2-thioethyl esters of modified nucleoside 5'-monophosphates as inhibitors of hepatitis C virus RNA replication
    Thazha P Prakash
    Department of Medicinal Chemistry, Isis Pharmaceuticals, 2292 Faraday Avenue, Carlsbad, California 92008, USA
    J Med Chem 48:1199-210. 2005
  5. doi request reprint Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method
    Jennifer A Kowalski
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, CT 06877, USA
    Bioorg Med Chem Lett 20:3703-7. 2010
  6. doi request reprint Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists
    Steven J Taylor
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, 900 Ridgebury Rd, PO Box 368, Ridgefield, CT 06877 036, USA
    Bioorg Med Chem Lett 23:2177-80. 2013
  7. ncbi request reprint Synthesis and biological evaluation of 5R- and 5S-methyl substituted D- and L-configuration 1,3-dioxolane nucleoside analogs
    Sanjib Bera
    Department of Medicinal Chemistry, Isis Pharmaceuticals, Carlsbad, CA 92008, USA
    Bioorg Med Chem 12:6237-47. 2004
  8. ncbi request reprint Structure-activity relationship study on a simple cationic peptide motif for cellular delivery of antisense peptide nucleic acid
    Klaus Albertshofer
    Department of Medicinal Chemistry, Isis Pharmaceuticals, Inc, 1891 Rutherford Road, Carlsbad, CA 92008, USA
    J Med Chem 48:6741-9. 2005
  9. doi request reprint Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat
    John D Huber
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Ridgefield, Connecticut 06877, United States
    J Med Chem 55:7114-40. 2012
  10. ncbi request reprint Structure-activity relationship of heterobase-modified 2'-C-methyl ribonucleosides as inhibitors of hepatitis C virus RNA replication
    Anne B Eldrup
    Department of Medicinal Chemistry, Isis Pharmaceuticals, 2280 Faraday Avenue, Carlsbad, CA 92008, USA
    J Med Chem 47:5284-97. 2004

Collaborators

Detail Information

Publications10

  1. doi request reprint Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase
    Anne B Eldrup
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Ridgefield, Connecticut 06877, USA
    J Med Chem 52:5880-95. 2009
    ..An inhibitor from this class displayed an attractive in vitro metabolic profile and high and sustained plasma exposure in the rat after oral administration...
  2. doi request reprint Optimization of piperidyl-ureas as inhibitors of soluble epoxide hydrolase
    Anne B Eldrup
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Ridgefield, CT 06877, United States
    Bioorg Med Chem Lett 20:571-5. 2010
    ....
  3. doi request reprint Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase
    Steven J Taylor
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, 900 Ridgebury Rd PO Box 368, Ridgefield, CT 06877 036, USA
    Bioorg Med Chem Lett 19:5864-8. 2009
    ..Structure-guided optimization of these analogs gave rise to nanomolar inhibitors of human sEH that had acceptable plasma exposure to qualify them as probes to determine the in vivo phenotypic consequences of sEH inhibition...
  4. ncbi request reprint Synthesis and evaluation of S-acyl-2-thioethyl esters of modified nucleoside 5'-monophosphates as inhibitors of hepatitis C virus RNA replication
    Thazha P Prakash
    Department of Medicinal Chemistry, Isis Pharmaceuticals, 2292 Faraday Avenue, Carlsbad, California 92008, USA
    J Med Chem 48:1199-210. 2005
    ..Additionally, chromosomal aberration studies with the SATE prodrug in cells showed no statistically relevant increase in aberrations compared to the concurrent controls...
  5. doi request reprint Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method
    Jennifer A Kowalski
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, CT 06877, USA
    Bioorg Med Chem Lett 20:3703-7. 2010
    ....
  6. doi request reprint Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists
    Steven J Taylor
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, 900 Ridgebury Rd, PO Box 368, Ridgefield, CT 06877 036, USA
    Bioorg Med Chem Lett 23:2177-80. 2013
    ..The series of benzylamine and benzylsulfone antagonists herein reported display a combination of nanomolar molecular and cellular potency as well as acceptable in vitro permeability and metabolic stability...
  7. ncbi request reprint Synthesis and biological evaluation of 5R- and 5S-methyl substituted D- and L-configuration 1,3-dioxolane nucleoside analogs
    Sanjib Bera
    Department of Medicinal Chemistry, Isis Pharmaceuticals, Carlsbad, CA 92008, USA
    Bioorg Med Chem 12:6237-47. 2004
    ..In addition, activity against vaccinia and HIV was evaluated in cell-based assays. The 2-hydroxymethyl-5-methyl-1,3-dioxolanes were found to be inactive...
  8. ncbi request reprint Structure-activity relationship study on a simple cationic peptide motif for cellular delivery of antisense peptide nucleic acid
    Klaus Albertshofer
    Department of Medicinal Chemistry, Isis Pharmaceuticals, Inc, 1891 Rutherford Road, Carlsbad, CA 92008, USA
    J Med Chem 48:6741-9. 2005
    ..In a preliminary PK/tissue distribution study in healthy mice, the parent conjugate exhibited relatively broad tissue distribution and only modest elimination via excretion within the time frame of the study...
  9. doi request reprint Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat
    John D Huber
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Ridgefield, Connecticut 06877, United States
    J Med Chem 55:7114-40. 2012
    ..Pharmacological evaluation of 60 revealed a remarkable ability to prevent ischemic damage in an ex vivo model of ischemia reperfusion injury in isolated rat hearts...
  10. ncbi request reprint Structure-activity relationship of heterobase-modified 2'-C-methyl ribonucleosides as inhibitors of hepatitis C virus RNA replication
    Anne B Eldrup
    Department of Medicinal Chemistry, Isis Pharmaceuticals, 2280 Faraday Avenue, Carlsbad, CA 92008, USA
    J Med Chem 47:5284-97. 2004
    ....