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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 1.
Sifferlen T, Boller A, Chardonneau A, Cottreel E, Hoecker J, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Gatfield J, Treiber A, Brisbare-Roch C, Jenck F, Boss C. Sifferlen T, et al. Among authors: williams jt. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1201-8. doi: 10.1016/j.bmcl.2013.12.092. Epub 2013 Dec 30. Bioorg Med Chem Lett. 2014. PMID: 24447850
Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.
Boss C, Roch-Brisbare C, Steiner MA, Treiber A, Dietrich H, Jenck F, von Raumer M, Sifferlen T, Brotschi C, Heidmann B, Williams JT, Aissaoui H, Siegrist R, Gatfield J. Boss C, et al. Among authors: williams jt. ChemMedChem. 2014 Nov;9(11):2486-96. doi: 10.1002/cmdc.201402258. Epub 2014 Aug 21. ChemMedChem. 2014. PMID: 25147058
Discovery of a Novel Orally Active, Selective LPA Receptor Type 1 Antagonist, 4-(4-(2-Isopropylphenyl)-4-((2-methoxy-4-methylphenyl)carbamoyl)piperidin-1-yl)-4-oxobutanoic Acid, with a Distinct Molecular Scaffold.
Lescop C, Brotschi C, Williams JT, Sager CP, Birker M, Morrison K, Froidevaux S, Delahaye S, Nayler O, Bolli MH. Lescop C, et al. Among authors: williams jt. J Med Chem. 2024 Feb 22;67(4):2379-2396. doi: 10.1021/acs.jmedchem.3c01826. Epub 2024 Feb 13. J Med Chem. 2024. PMID: 38349223
509 results