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Items: 1 to 50 of 58

1.

From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs.

Brotschi C, Bolli MH, Gatfield J, Heidmann B, Jenck F, Roch C, Sifferlen T, Treiber A, Williams JT, Boss C.

ChemMedChem. 2020 Jan 16. doi: 10.1002/cmdc.201900618. [Epub ahead of print]

PMID:
31945272
2.

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure-Activity Relationships, and Sleep-Promoting Properties in Rats.

Brotschi C, Roch C, Gatfield J, Treiber A, Williams JT, Sifferlen T, Heidmann B, Jenck F, Bolli MH, Boss C.

ChemMedChem. 2019 Jul 3;14(13):1257-1270. doi: 10.1002/cmdc.201900242. Epub 2019 Jun 5.

PMID:
31066976
3.

Cross-species comparison of the metabolism and excretion of selexipag.

Ichikawa T, Yamada T, Treiber A, Gnerre C, Segrestaa J, Seeland S, Nonaka K.

Xenobiotica. 2019 Mar;49(3):284-301. doi: 10.1080/00498254.2018.1444814. Epub 2018 Mar 21.

PMID:
29468921
4.

The metabolism and drug-drug interaction potential of the selective prostacyclin receptor agonist selexipag.

Gnerre C, Segrestaa J, Seeland S, Äänismaa P, Pfeifer T, Delahaye S, de Kanter R, Ichikawa T, Yamada T, Treiber A.

Xenobiotica. 2018 Jul;48(7):704-719. doi: 10.1080/00498254.2017.1357088. Epub 2017 Aug 30.

PMID:
28737453
5.

The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.

Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, Schindelholz B, Muehlan C, van Gerven J, Jenck F.

J Pharmacol Exp Ther. 2017 Sep;362(3):489-503. doi: 10.1124/jpet.117.241596. Epub 2017 Jun 29.

PMID:
28663311
6.

Pharmacokinetics of the selective prostacyclin receptor agonist selexipag in rats, dogs and monkeys.

Ichikawa T, Yamada T, Treiber A, Gnerre C, Nonaka K.

Xenobiotica. 2018 Feb;48(2):186-196. doi: 10.1080/00498254.2017.1294277. Epub 2017 Mar 2.

PMID:
28277164
7.

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach.

Heidmann B, Gatfield J, Roch C, Treiber A, Tortoioli S, Brotschi C, Williams JT, Bolli MH, Abele S, Sifferlen T, Jenck F, Boss C.

ChemMedChem. 2016 Oct 6;11(19):2132-2146. doi: 10.1002/cmdc.201600175. Epub 2016 Jul 8.

PMID:
27390287
8.

4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic Acid Butyl Ester (ACT-246475) and Its Prodrug (ACT-281959), a Novel P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel.

Caroff E, Hubler F, Meyer E, Renneberg D, Gnerre C, Treiber A, Rey M, Hess P, Steiner B, Hilpert K, Riederer MA.

J Med Chem. 2015 Dec 10;58(23):9133-53. doi: 10.1021/acs.jmedchem.5b00933. Epub 2015 Nov 18.

PMID:
26550844
9.

Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug-Drug Interactions.

de Kanter R, Sidharta PN, Delahaye S, Gnerre C, Segrestaa J, Buchmann S, Kohl C, Treiber A.

Clin Pharmacokinet. 2016 Mar;55(3):369-80. doi: 10.1007/s40262-015-0322-y.

PMID:
26385839
10.

The metabolism of the dual endothelin receptor antagonist macitentan in rat and dog.

Treiber A, Miraval T, Bolli MH, Funel JA, Segrestaa J, Seeland S.

Xenobiotica. 2016;46(3):253-67. doi: 10.3109/00498254.2015.1070302. Epub 2015 Sep 4.

PMID:
26337830
11.

ATP-induced cellular stress and mitochondrial toxicity in cells expressing purinergic P2X7 receptor.

Seeland S, Kettiger H, Murphy M, Treiber A, Giller J, Kiss A, Sube R, Krähenbühl S, Hafner M, Huwyler J.

Pharmacol Res Perspect. 2015 Mar;3(2):e00123. doi: 10.1002/prp2.123. Epub 2015 Mar 12.

12.

Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan.

Sidharta PN, Treiber A, Dingemanse J.

Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. Review.

13.

Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Gatfield J, Treiber A, Roch C, Jenck F, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Boss C.

Bioorg Med Chem Lett. 2015 May 1;25(9):1884-91. doi: 10.1016/j.bmcl.2015.03.035. Epub 2015 Mar 21.

PMID:
25838147
14.

Pharmacokinetic interactions between simvastatin and setipiprant, a CRTH2 antagonist.

Gehin M, Sidharta PN, Gnerre C, Treiber A, Halabi A, Dingemanse J.

Eur J Clin Pharmacol. 2015 Jan;71(1):15-23. doi: 10.1007/s00228-014-1767-x. Epub 2014 Oct 18.

PMID:
25323804
15.

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.

ChemMedChem. 2014 Nov;9(11):2486-96. doi: 10.1002/cmdc.201402258. Epub 2014 Aug 21.

PMID:
25147058
16.

Optimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y(12) antagonists for inhibition of platelet aggregation.

Caroff E, Meyer E, Treiber A, Hilpert K, Riederer MA.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4323-31. doi: 10.1016/j.bmcl.2014.06.070. Epub 2014 Jul 1.

PMID:
25113932
17.

Macitentan does not interfere with hepatic bile salt transport.

Treiber A, Äänismaa P, de Kanter R, Delahaye S, Treher M, Hess P, Sidharta P.

J Pharmacol Exp Ther. 2014 Jul;350(1):130-43. doi: 10.1124/jpet.114.214106. Epub 2014 Apr 25.

PMID:
24769543
18.

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.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1201-8. doi: 10.1016/j.bmcl.2013.12.092. Epub 2013 Dec 30.

PMID:
24447850
19.

Novel S1P1 receptor agonists--part 1: From pyrazoles to thiophenes.

Bolli MH, Müller C, Mathys B, Abele S, Birker M, Bravo R, Bur D, Hess P, Kohl C, Lehmann D, Nayler O, Rey M, Meyer S, Scherz M, Schmidt G, Steiner B, Treiber A, Velker J, Weller T.

J Med Chem. 2013 Dec 12;56(23):9737-55. doi: 10.1021/jm4014373. Epub 2013 Nov 22.

PMID:
24266709
20.

Time course of cerebrovascular autoregulation during extreme Trendelenburg position for robotic-assisted prostatic surgery.

Schramm P, Treiber AH, Berres M, Pestel G, Engelhard K, Werner C, Closhen D.

Anaesthesia. 2014 Jan;69(1):58-63. doi: 10.1111/anae.12477. Epub 2013 Nov 20.

21.

Robotic assisted prostatic surgery in the Trendelenburg position does not impair cerebral oxygenation measured using two different monitors: A clinical observational study.

Closhen D, Treiber AH, Berres M, Sebastiani A, Werner C, Engelhard K, Schramm P.

Eur J Anaesthesiol. 2014 Feb;31(2):104-9. doi: 10.1097/EJA.0000000000000000.

PMID:
24225725
22.

Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.

Steiner MA, Gatfield J, Brisbare-Roch C, Dietrich H, Treiber A, Jenck F, Boss C.

ChemMedChem. 2013 Jun;8(6):898-903. doi: 10.1002/cmdc.201300003. Epub 2013 Apr 15.

PMID:
23589487
23.

Elucidation of the metabolic pathways and the resulting multiple metabolites of almorexant, a dual orexin receptor antagonist, in humans.

Dingemanse J, Hoever P, Hoch M, Treiber A, Wagner-Redeker W, Miraval T, Hopfgartner G, Shakeri-Nejad K.

Drug Metab Dispos. 2013 May;41(5):1046-59. doi: 10.1124/dmd.112.050120. Epub 2013 Feb 21.

PMID:
23431113
24.

A cell-based, multiparametric sensor approach characterises drug-induced cytotoxicity in human liver HepG2 cells.

Seeland S, Török M, Kettiger H, Treiber A, Hafner M, Huwyler J.

Toxicol In Vitro. 2013 Apr;27(3):1109-20. doi: 10.1016/j.tiv.2013.02.001. Epub 2013 Feb 14.

PMID:
23416262
25.

Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line.

Fahrmayr C, König J, Auge D, Mieth M, Münch K, Segrestaa J, Pfeifer T, Treiber A, Fromm M.

Br J Pharmacol. 2013 May;169(1):21-33. doi: 10.1111/bph.12126.

26.

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.

J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16.

PMID:
22862294
27.

Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans.

Bruderer S, Hopfgartner G, Seiberling M, Wank J, Sidharta PN, Treiber A, Dingemanse J.

Xenobiotica. 2012 Sep;42(9):901-10. doi: 10.3109/00498254.2012.664665. Epub 2012 Mar 30.

PMID:
22458347
28.

Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist.

Bruderer S, Aänismaa P, Homery MC, Häusler S, Landskroner K, Sidharta PN, Treiber A, Dingemanse J.

AAPS J. 2012 Mar;14(1):68-78. doi: 10.1208/s12248-011-9316-3. Epub 2011 Dec 22.

29.

Improvement of rotary encoders in human-machine-interfaces through optimized acoustic feedback.

Treiber AS, Gruhler G, Rozinaj G.

J Acoust Soc Am. 2011 Aug;130(2):EL57-61. doi: 10.1121/1.3601925.

PMID:
21877771
30.

Surgical and pharmacological animal models used in drug metabolism and pharmacokinetics.

Landskroner KA, Hess P, Treiber A.

Xenobiotica. 2011 Aug;41(8):687-700. doi: 10.3109/00498254.2011.569772. Epub 2011 Apr 13. Review.

PMID:
21486193
31.

On-line identification of P-glycoprotein substrates by monitoring of extracellular acidification and respiration rates in living cells.

Seeland S, Treiber A, Hafner M, Huwyler J.

Biochim Biophys Acta. 2011 Jul;1808(7):1827-31. doi: 10.1016/j.bbamem.2011.03.003. Epub 2011 Mar 22.

32.

Piperidine-based renin inhibitors: upper chain optimization.

Corminboeuf O, Bezençon O, Remeň L, Grisostomi C, Richard-Bildstein S, Bur D, Prade L, Strickner P, Hess P, Fischli W, Steiner B, Treiber A.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6291-6. doi: 10.1016/j.bmcl.2010.08.087. Epub 2010 Aug 22.

PMID:
20843690
33.

Design and optimization of new piperidines as renin inhibitors.

Corminboeuf O, Bezençon O, Grisostomi C, Remeň L, Richard-Bildstein S, Bur D, Prade L, Hess P, Strickner P, Fischli W, Steiner B, Treiber A.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6286-90. doi: 10.1016/j.bmcl.2010.08.086. Epub 2010 Aug 22.

PMID:
20843686
34.

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.

J Med Chem. 2010 May 27;53(10):4198-211. doi: 10.1021/jm100181s.

PMID:
20446681
35.

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.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6762-5. doi: 10.1016/j.bmcl.2009.09.104. Epub 2009 Oct 1.

PMID:
19853442
36.

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.

J Med Chem. 2009 Jun 25;52(12):3689-702. doi: 10.1021/jm900022f.

PMID:
19358611
37.

In vitro and in vivo pharmacokinetic characteristics of clazosentan, an intravenous endothelin receptor antagonist, in humans.

van Giersbergen PL, Treiber A, Dingemanse J.

Int J Clin Pharmacol Ther. 2009 Mar;47(3):169-77.

PMID:
19281726
38.

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Aissaoui H, Koberstein R, Zumbrunn C, Gatfield J, Brisbare-Roch C, Jenck F, Treiber A, Boss C.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5729-33. doi: 10.1016/j.bmcl.2008.09.079. Epub 2008 Sep 26.

PMID:
18845436
39.

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist.

Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, Weller T, Bolli MH, Boss C, Buchmann S, Capeleto B, Hess P, Qiu C, Clozel M.

J Pharmacol Exp Ther. 2008 Dec;327(3):736-45. doi: 10.1124/jpet.108.142976. Epub 2008 Sep 9.

PMID:
18780830
40.
41.
42.

Inhibitory and inductive effects of rifampin on the pharmacokinetics of bosentan in healthy subjects.

van Giersbergen PL, Treiber A, Schneiter R, Dietrich H, Dingemanse J.

Clin Pharmacol Ther. 2007 Mar;81(3):414-9. Epub 2007 Jan 24. Erratum in: Clin Pharmacol Ther. 2007 Mar;81(3):460.

PMID:
17251982
43.

Temporal characteristics of feeding behavior in the Munich miniature pig.

Musial F, Kowalski A, Treiber A, Enck P.

Physiol Behav. 2006 Jan 30;87(1):206-18. Epub 2005 Oct 25.

PMID:
16253295
44.

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.

J Med Chem. 2004 May 20;47(11):2776-95.

PMID:
15139756
45.
46.

In vivo and in vitro disposition profile of tezosentan, an intravenous dual endothelin receptor antagonist, in humans.

Treiber A, Van Giersbergen PL, Dingemanse J.

Xenobiotica. 2003 Apr;33(4):399-414.

PMID:
12745875
47.

No influence of the endothelin receptor antagonist bosentan on basal and indomethacin-induced reduction of cerebral blood flow in pigs.

Rasmussen M, Poulsen PH, Treiber A, Delahaye S, Tankisi A, Cold GE, Therkelsen K, Gjedde A, Astrup J.

Acta Anaesthesiol Scand. 2003 Feb;47(2):200-7.

PMID:
12631050
48.

Mechanism of the aromatic hydroxylation of thiophene by acid-catalyzed peracid oxidation.

Treiber A, Dansette PM, Mansuy D.

J Org Chem. 2002 Oct 18;67(21):7261-6.

PMID:
12375952
49.

Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptor.

van Giersbergen PL, Gnerre C, Treiber A, Dingemanse J, Meyer UA.

Eur J Pharmacol. 2002 Aug 23;450(2):115-21.

PMID:
12206849
50.

In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide.

van Giersbergen PL, Treiber A, Clozel M, Bodin F, Dingemanse J.

Clin Pharmacol Ther. 2002 Apr;71(4):253-62.

PMID:
11956508

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