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Chemmedchem|July 9, 2016
Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping ApproachBibia Heidmann, John Gatfield, Catherine Roch, et al.Bioorganic & Medicinal Chemistry Letters|April 4, 2015
Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2Thierry Sifferlen, Amandine Boller, Audrey Chardonneau, et al.The Journal of Pharmacology and Experimental Therapeutics|September 11, 2008
Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonistMarc Iglarz, Christoph Binkert, Keith Morrison, et al.Journal of Medicinal Chemistry|August 7, 2012
The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonistMartin H Bolli, Christoph Boss, Christoph Binkert, et al.Journal of Medicinal Chemistry|May 14, 2004
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonistsMartin H Bolli, Judith Marfurt, Corinna Grisostomi, et al.Bioorganic & Medicinal Chemistry Letters|January 23, 2014
Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1Thierry Sifferlen, Amandine Boller, Audrey Chardonneau, et al.Chemmedchem|August 23, 2014
Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonistChristoph Boss, Catherine Roch-Brisbare, Michel A Steiner, et al.Chemmedchem|April 7, 2025
Discovery of Novel Aminopyrimidines as Selective EP2 Receptor AntagonistsIsabelle Lyothier, Stefan Diethelm, Julien Pothier, et al.Bioorganic & Medicinal Chemistry Letters|October 27, 2009
New classes of potent and bioavailable human renin inhibitorsL'ubos Remen, Olivier Bezençon, Sylvia Richard-Bildstein, et al.Chemmedchem|April 7, 2025
Discovery of ACT-1002-4271 as a Dual Prostaglandin E2 Receptor 2/Prostaglandin E2 Receptor 4 Antagonist with In Vivo Anti-Tumor EfficacyIsabelle Lyothier, Stefan Diethelm, Julien Pothier, et al.Pageof 5