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Page 1
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.
Chen HY, Plummer CW, Xiao D, Chobanian HR, DeMong D, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Di Salvo J, Thomas-Fowlkes B, Souza S, Tatosian DA, Chen Q, Hafey MJ, Houle R, Nolting AF, Orr R, Ehrhart J, Weinglass AB, Tschirret-Guth R, Howard AD, Colletti SL. Chen HY, et al. Among authors: tschirret guth r. ACS Med Chem Lett. 2018 Jun 14;9(7):685-690. doi: 10.1021/acsmedchemlett.8b00149. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034601 Free PMC article.
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
Plummer CW, Clements MJ, Chen H, Rajagopalan M, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Nolting AF, Orr R, Christensen M, Campeau LC, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Nargund R, Howard AD, Colletti SL. Plummer CW, et al. Among authors: tschirret guth r. ACS Med Chem Lett. 2017 Jan 23;8(2):221-226. doi: 10.1021/acsmedchemlett.6b00443. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197316 Free PMC article.
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
Pio B, Chobanian HR, Guo Y, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Ashley E, Orr R, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Samuel K, Chen Q, Shang J, Lamca J, Ehrhart J, Nargund R, Howard AD, Colletti SL. Pio B, et al. Among authors: tschirret guth r. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1842-1848. doi: 10.1016/j.bmcl.2019.04.050. Epub 2019 May 2. Bioorg Med Chem Lett. 2019. PMID: 31109791
Development of a novel class of potent and selective FIXa inhibitors.
Zhang T, Andre P, Bateman TJ, Chen YH, Desai K, Ellsworth K, Geissler WM, Guo L, Hruza A, Jian T, Meng D, Parker DL Jr, Qian X, Reichert P, Sherer EC, Shu M, Smith CJ, Sonatore LM, Tschirret-Guth R, Nolting AF, Orr R, Campeau LC, Araki K, Nishimura T, Sakurada I, Wood HB. Zhang T, et al. Among authors: tschirret guth r. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4945-4949. doi: 10.1016/j.bmcl.2015.04.057. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25978966
Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Meng D, Andre P, Bateman TJ, Berger R, Chen YH, Desai K, Dewnani S, Ellsworth K, Feng D, Geissler WM, Guo L, Hruza A, Jian T, Li H, Metzger J, Parker DL, Reichert P, Sherer EC, Smith CJ, Sonatore LM, Tschirret-Guth R, Wu J, Xu J, Zhang T, Campeau LC, Orr R, Poirier M, McCabe-Dunn J, Araki K, Nishimura T, Sakurada I, Hirabayashi T, Wood HB. Meng D, et al. Among authors: tschirret guth r. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5437-43. doi: 10.1016/j.bmcl.2015.07.078. Epub 2015 Jul 31. Bioorg Med Chem Lett. 2015. PMID: 26318999
Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents.
Lévesque JF, Bleasby K, Chefson A, Chen A, Dubé D, Ducharme Y, Fournier PA, Gagné S, Gallant M, Grimm E, Hafey M, Han Y, Houle R, Lacombe P, Laliberté S, MacDonald D, Mackay B, Papp R, Tschirret-Guth R. Lévesque JF, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5547-51. doi: 10.1016/j.bmcl.2011.06.095. Epub 2011 Jun 28. Bioorg Med Chem Lett. 2011. PMID: 21784634
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Kassick AJ, Jiang J, Bunda J, Wilson D, Bao J, Lu H, Lin P, Ball RG, Doss GA, Tong X, Tsao KL, Wang H, Chicchi G, Karanam B, Tschirret-Guth R, Samuel K, Hora DF, Kumar S, Madeira M, Eng W, Hargreaves R, Purcell M, Gantert L, Cook J, DeVita RJ, Mills SG. Kassick AJ, et al. Among authors: tschirret guth r. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
Selective PPARgamma modulators with improved pharmacological profiles.
Liu K, Black RM, Acton JJ 3rd, Mosley R, Debenham S, Abola R, Yang M, Tschirret-Guth R, Colwell L, Liu C, Wu M, Wang CF, MacNaul KL, McCann ME, Moller DE, Berger JP, Meinke PT, Jones AB, Wood HB. Liu K, et al. Bioorg Med Chem Lett. 2005 May 16;15(10):2437-40. doi: 10.1016/j.bmcl.2005.03.092. Bioorg Med Chem Lett. 2005. PMID: 15863293
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Jiang J, Bunda JL, Doss GA, Chicchi GG, Kurtz MM, Tsao KL, Tong X, Zheng S, Upthagrove A, Samuel K, Tschirret-Guth R, Kumar S, Wheeldon A, Carlson EJ, Hargreaves R, Burns D, Hamill T, Ryan C, Krause SM, Eng W, DeVita RJ, Mills SG. Jiang J, et al. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
35 results