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Page 1
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.
Bezençon O, Bur D, Weller T, Richard-Bildstein S, Remen L, Sifferlen T, Corminboeuf O, Grisostomi C, Boss C, Prade L, Delahaye S, Treiber A, Strickner P, Binkert C, Hess P, Steiner B, Fischli W. Bezençon O, et al. Among authors: weller t. J Med Chem. 2009 Jun 25;52(12):3689-702. doi: 10.1021/jm900022f. J Med Chem. 2009. PMID: 19358611
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Bolli MH, Marfurt J, Grisostomi C, Boss C, Binkert C, Hess P, Treiber A, Thorin E, Morrison K, Buchmann S, Bur D, Ramuz H, Clozel M, Fischli W, Weller T. Bolli MH, et al. Among authors: weller t. J Med Chem. 2004 May 20;47(11):2776-95. doi: 10.1021/jm031115r. J Med Chem. 2004. PMID: 15139756
Achiral, cheap, and potent inhibitors of Plasmepsins I, II, and IV.
Boss C, Corminboeuf O, Grisostomi C, Meyer S, Jones AF, Prade L, Binkert C, Fischli W, Weller T, Bur D. Boss C, et al. Among authors: weller t. ChemMedChem. 2006 Dec;1(12):1341-5. doi: 10.1002/cmdc.200600223. ChemMedChem. 2006. PMID: 17091526 No abstract available.
New classes of potent and bioavailable human renin inhibitors.
Remen L, Bezençon O, Richard-Bildstein S, Bur D, Prade L, Corminboeuf O, Boss C, Grisostomi C, Sifferlen T, Strickner P, Hess P, Delahaye S, Treiber A, Weller T, Binkert C, Steiner B, Fischli W. Remen L, et al. Among authors: weller t. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6762-5. doi: 10.1016/j.bmcl.2009.09.104. Epub 2009 Oct 1. Bioorg Med Chem Lett. 2009. PMID: 19853442
Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.
Sifferlen T, Boss C, Cottreel E, Koberstein R, Gude M, Aissaoui H, Weller T, Gatfield J, Brisbare-Roch C, Jenck F. Sifferlen T, et al. Among authors: weller t. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1539-42. doi: 10.1016/j.bmcl.2010.01.070. Epub 2010 Jan 22. Bioorg Med Chem Lett. 2010. PMID: 20144866
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Bolli MH, Abele S, Binkert C, Bravo R, Buchmann S, Bur D, Gatfield J, Hess P, Kohl C, Mangold C, Mathys B, Menyhart K, Müller C, Nayler O, Scherz M, Schmidt G, Sippel V, Steiner B, Strasser D, Treiber A, Weller T. Bolli MH, et al. Among authors: weller t. J Med Chem. 2010 May 27;53(10):4198-211. doi: 10.1021/jm100181s. J Med Chem. 2010. PMID: 20446681
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 antagonist.
Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T. Bolli MH, et al. Among authors: weller t. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16. J Med Chem. 2012. PMID: 22862294
Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.
Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C. Sifferlen T, et al. Among authors: weller t. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2212-6. doi: 10.1016/j.bmcl.2013.01.088. Epub 2013 Jan 29. Bioorg Med Chem Lett. 2013. PMID: 23434414
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.
Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C. Sifferlen T, et al. Among authors: weller t. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3857-63. doi: 10.1016/j.bmcl.2013.04.071. Epub 2013 May 8. Bioorg Med Chem Lett. 2013. PMID: 23719231
219 results