C Boss

Summary

Affiliation: Actelion Pharmaceuticals Ltd
Country: Switzerland

Publications

  1. doi request reprint Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action
    Christoph Boss
    Actelion Pharmaceuticals Ltd, Drug Discovery and Preclinical Development, Hegenheimermattweg 91, 4123, Allschwil, Switzerland
    ChemMedChem 11:1995-2014. 2016
  2. doi request reprint From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective
    Christoph Boss
    Drug Discovery and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland Electronic address
    Bioorg Med Chem Lett 26:3381-94. 2016
  3. doi request reprint Recent trends in orexin research--2010 to 2015
    Christoph Boss
    Drug Discovery Chemistry, Actelion Pharmaceuticals Ltd, Hegenheimermattweg 91, CH 4123 Allschwil, Switzerland Electronic address
    Bioorg Med Chem Lett 25:2875-87. 2015
  4. doi request reprint Orexin receptor antagonists--a patent review (2010 to August 2014)
    Christoph Boss
    Drug Discovery and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Expert Opin Ther Pat 24:1367-81. 2014
  5. doi request reprint Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist
    Christoph Boss
    Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd Gewerbestrasse 16, 4123 Allschwil BL Switzerland
    ChemMedChem 9:2486-96. 2014
  6. ncbi request reprint Endothelin receptor antagonists: structures, synthesis, selectivity and therapeutic applications
    C Boss
    Department of Medicinal Chemistry, Actelion Pharmaceuticals Ltd, Allschwil BL, Switzerland
    Curr Med Chem 9:349-83. 2002
  7. ncbi request reprint Inhibitors of the Plasmodium falciparum parasite aspartic protease plasmepsin II as potential antimalarial agents
    C Boss
    Drug Discovery Chemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Curr Med Chem 10:883-907. 2003
  8. ncbi request reprint Bis-sulfonamides as endothelin receptor antagonists
    Christoph Boss
    Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Bioorg Med Chem Lett 13:951-4. 2003
  9. ncbi request reprint X-ray structure of plasmepsin II complexed with a potent achiral inhibitor
    Lars Prade
    Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
    J Biol Chem 280:23837-43. 2005
  10. ncbi request reprint Achiral, cheap, and potent inhibitors of Plasmepsins I, II, and IV
    Christoph Boss
    Drug Discovery, Chemistry and Biology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland
    ChemMedChem 1:1341-5. 2006

Detail Information

Publications13

  1. doi request reprint Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action
    Christoph Boss
    Actelion Pharmaceuticals Ltd, Drug Discovery and Preclinical Development, Hegenheimermattweg 91, 4123, Allschwil, Switzerland
    ChemMedChem 11:1995-2014. 2016
    ..Herein we describe our optimization efforts from the screening hit to the potential drug candidate with respect to antiparasitic activity, drug metabolism and pharmacokinetics (DMPK) properties, and in vivo pharmacological efficacy. ..
  2. doi request reprint From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective
    Christoph Boss
    Drug Discovery and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland Electronic address
    Bioorg Med Chem Lett 26:3381-94. 2016
    ..A condensed overview of the competitive landscape in the field of ERAs puts the different strategies and tactics applied by the medicinal chemists involved in this endeavor into perspective. ..
  3. doi request reprint Recent trends in orexin research--2010 to 2015
    Christoph Boss
    Drug Discovery Chemistry, Actelion Pharmaceuticals Ltd, Hegenheimermattweg 91, CH 4123 Allschwil, Switzerland Electronic address
    Bioorg Med Chem Lett 25:2875-87. 2015
    ..The review reflects on the most recent activities in the field of orexin research. ..
  4. doi request reprint Orexin receptor antagonists--a patent review (2010 to August 2014)
    Christoph Boss
    Drug Discovery and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Expert Opin Ther Pat 24:1367-81. 2014
    ..Clinical proof of concept was obtained with dual orexin receptor antagonists in primary insomnia. Merck's suvorexant got FDA approval on 13 August 2014 for the treatment of insomnia...
  5. doi request reprint Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist
    Christoph Boss
    Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd Gewerbestrasse 16, 4123 Allschwil BL Switzerland
    ChemMedChem 9:2486-96. 2014
    ..ACT-462206 shows anxiolytic-like properties in rats without affecting cognition and motor function. It is therefore a potential candidate for the treatment of insomnia...
  6. ncbi request reprint Endothelin receptor antagonists: structures, synthesis, selectivity and therapeutic applications
    C Boss
    Department of Medicinal Chemistry, Actelion Pharmaceuticals Ltd, Allschwil BL, Switzerland
    Curr Med Chem 9:349-83. 2002
    ....
  7. ncbi request reprint Inhibitors of the Plasmodium falciparum parasite aspartic protease plasmepsin II as potential antimalarial agents
    C Boss
    Drug Discovery Chemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Curr Med Chem 10:883-907. 2003
    ..We review the drug discovery efforts that were published in the literature on this enzyme, and we present the compounds synthesized at Actelion Pharmaceuticals Ltd...
  8. ncbi request reprint Bis-sulfonamides as endothelin receptor antagonists
    Christoph Boss
    Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Bioorg Med Chem Lett 13:951-4. 2003
    ..This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the pharmacological consequences of selective ET(B) receptor blockade...
  9. ncbi request reprint X-ray structure of plasmepsin II complexed with a potent achiral inhibitor
    Lars Prade
    Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
    J Biol Chem 280:23837-43. 2005
    ..These newly obtained structural insights will further guide our attempts to improve compound properties eventually leading to the identification of molecules suitable as antimalarial drugs...
  10. ncbi request reprint Achiral, cheap, and potent inhibitors of Plasmepsins I, II, and IV
    Christoph Boss
    Drug Discovery, Chemistry and Biology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland
    ChemMedChem 1:1341-5. 2006
  11. ncbi request reprint Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists
    Martin H Bolli
    Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
    J Med Chem 47:2776-95. 2004
    ..In this animal model, the efficacy of the benzo[e][1,4]diazepin-2-one derivative rac-39au was superior to that of racemic ambrisentan, rac-2...
  12. ncbi request reprint The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists
    Martin H Bolli
    Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
    Bioorg Med Chem Lett 13:955-9. 2003
    ..g., 70 and 75). The propargyl derivative 26 significantly reduced blood pressure in in vivo model studies with hypertensive salt-sensitive Dahl rats...
  13. ncbi request reprint Inhibitors of Plasmepsin II-potential antimalarial agents
    Olivier Corminboeuf
    Drug Discovery Chemistry and Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland
    Bioorg Med Chem Lett 16:6194-9. 2006
    ..The results show that the new structural class is not only inhibiting PMII in vitro but is also active in a P. falciparum infected human red blood cell assay...