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Page 1
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.
Fader LD, Bailey M, Beaulieu E, Bilodeau F, Bonneau P, Bousquet Y, Carson RJ, Chabot C, Coulombe R, Duan J, Fenwick C, Garneau M, Halmos T, Jakalian A, James C, Kawai SH, Landry S, LaPlante SR, Mason SW, Morin S, Rioux N, Simoneau B, Surprenant S, Thavonekham B, Thibeault C, Trinh T, Tsantrizos Y, Tsoung J, Yoakim C, Wernic D. Fader LD, et al. Among authors: thibeault c. ACS Med Chem Lett. 2016 Jun 9;7(8):797-801. doi: 10.1021/acsmedchemlett.6b00194. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563405 Free PMC article.
Discovery of Potent, Orally Bioavailable Inhibitors of Human Cytomegalovirus.
Fader L, Brault M, Desjardins J, Dansereau N, Lamorte L, Tremblay S, Bilodeau F, Bordeleau J, Duplessis M, Gorys V, Gillard J, Gleason JL, James C, Joly MA, Kuhn C, Llinas-Brunet M, Luo L, Morency L, Morin S, Parisien M, Poirier M, Thibeault C, Trinh T, Sturino C, Srivastava S, Yoakim C, Franti M. Fader L, et al. Among authors: thibeault c. ACS Med Chem Lett. 2016 Mar 1;7(5):525-30. doi: 10.1021/acsmedchemlett.6b00064. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190604 Free PMC article.
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Ruel R, Thibeault C, L'Heureux A, Martel A, Cai ZW, Wei D, Qian L, Barrish JC, Mathur A, D'Arienzo C, Hunt JT, Kamath A, Marathe P, Zhang Y, Derbin G, Wautlet B, Mortillo S, Jeyaseelan R Sr, Henley B, Tejwani R, Bhide RS, Trainor GL, Fargnoli J, Lombardo LJ. Ruel R, et al. Among authors: thibeault c. Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. doi: 10.1016/j.bmcl.2008.03.057. Epub 2008 Mar 22. Bioorg Med Chem Lett. 2008. PMID: 18395443
Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Qiao JX, Wang TC, Ruel R, Thibeault C, L'Heureux A, Schumacher WA, Spronk SA, Hiebert S, Bouthillier G, Lloyd J, Pi Z, Schnur DM, Abell LM, Hua J, Price LA, Liu E, Wu Q, Steinbacher TE, Bostwick JS, Chang M, Zheng J, Gao Q, Ma B, McDonnell PA, Huang CS, Rehfuss R, Wexler RR, Lam PY. Qiao JX, et al. Among authors: thibeault c. J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12. J Med Chem. 2013. PMID: 24164581
Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.
Ruel R, L'Heureux A, Thibeault C, Lapointe P, Martel A, Qiao JX, Hua J, Price LA, Wu Q, Chang M, Zheng J, Huang CS, Wexler RR, Rehfuss R, Lam PY. Ruel R, et al. Among authors: thibeault c. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6825-8. doi: 10.1016/j.bmcl.2013.10.009. Epub 2013 Oct 11. Bioorg Med Chem Lett. 2013. PMID: 24269480
New azole antagonists with high affinity for the P2Y(1) receptor.
Ruel R, L'Heureux A, Thibeault C, Daris JP, Martel A, Price LA, Wu Q, Hua J, Wexler RR, Rehfuss R, Lam PY. Ruel R, et al. Among authors: thibeault c. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3519-22. doi: 10.1016/j.bmcl.2013.04.041. Epub 2013 Apr 25. Bioorg Med Chem Lett. 2013. PMID: 23668989
Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.
Jeon YT, Yang W, Qiao JX, Li L, Ruel R, Thibeault C, Hiebert S, Wang TC, Wang Y, Liu Y, Clark CG, Wong HS, Zhu J, Wu DR, Sun D, Chen BC, Mathur A, Chacko SA, Malley M, Chen XQ, Shen H, Huang CS, Schumacher WA, Bostwick JS, Stewart AB, Price LA, Hua J, Li D, Levesque PC, Seiffert DA, Rehfuss R, Wexler RR, Lam PY. Jeon YT, et al. Among authors: thibeault c. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1294-8. doi: 10.1016/j.bmcl.2014.01.066. Epub 2014 Jan 31. Bioorg Med Chem Lett. 2014. PMID: 24513044
Soluble ACE2 correlates with severe COVID-19 and can impair antibody responses.
Lebedin M, Ratswohl C, Garg A, Schips M, García CV, Spatt L, Thibeault C, Obermayer B, Weiner J, Velásquez IM, Gerhard C, Stubbemann P, Hanitsch LG, Pischon T, Witzenrath M, Sander LE, Kurth F, Meyer-Hermann M, de la Rosa K. Lebedin M, et al. Among authors: thibeault c. iScience. 2024 Feb 24;27(3):109330. doi: 10.1016/j.isci.2024.109330. eCollection 2024 Mar 15. iScience. 2024. PMID: 38496296 Free PMC article.
Endoscopic Features of Post-COVID-19 Cholangiopathy and Its Management Using ERCP.
Leonhardt S, Grajecki D, Geisel D, Fehrenbach U, Adler A, Leonhardt J, Horst D, Kurth F, Thibeault C, Janssen HJ, Kaul T, Faiss S, Tacke F, Jürgensen C. Leonhardt S, et al. Among authors: thibeault c. Am J Gastroenterol. 2024 Apr 1;119(4):748-759. doi: 10.14309/ajg.0000000000002562. Epub 2023 Oct 16. Am J Gastroenterol. 2024. PMID: 37843039 Free PMC article.
95 results