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Page 1
Thiazole-based IL-17 inhibitors discovered by scaffold morphing.
Velcicky J, Ngo E, Bauer MR, Meyer A, Schlapbach A, Racine S, Orain D, Pflieger D, Teixeira-Fouchard S, Dubois C, Goetz A, Steiner R, Palmieri M, Bussenault A, Stringer R, Larger P, Riek S, Schmutz P, Lehmann S, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: larger p. ChemMedChem. 2024 Dec 23:e202400851. doi: 10.1002/cmdc.202400851. Online ahead of print. ChemMedChem. 2024. PMID: 39715021
Identification of TAK-756, A Potent TAK1 Inhibitor for the Treatment of Osteoarthritis through Intra-Articular Administration.
Langlois JB, Brenneisen S, Rodde S, Vangrevelinghe E, Rose G, Lerch P, Sorge M, Ullrich T, Patora-Komisarska K, Quancard J, Larger P, Gianola L, Textor C, Chenal G, Rubic-Schneider T, Simkova K, Masmanidou O, Scheufler C, Lammens A, Bouzan A, Demirci S, Flotte L, Rivet H, Hartmann L, Guezel D, Flueckiger M, Schilb A, Schuepbach E, Kettle R, Jacobi C, Pearson D, Richards PJ, Minetti GC. Langlois JB, et al. Among authors: larger p. J Med Chem. 2024 Dec 12;67(23):21163-21185. doi: 10.1021/acs.jmedchem.4c01938. Epub 2024 Nov 22. J Med Chem. 2024. PMID: 39576936
Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors.
Velcicky J, Bauer MR, Schlapbach A, Lapointe G, Meyer A, Vögtle M, Blum E, Ngo E, Rolando C, Nimsgern P, Teixeira-Fouchard S, Lehmann H, Furet P, Berst F, Schümann J, Stringer R, Larger P, Schmid C, Prendergast CT, Riek S, Schmutz P, Lehmann S, Berghausen J, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: larger p. J Med Chem. 2024 Sep 26;67(18):16692-16711. doi: 10.1021/acs.jmedchem.4c01520. Epub 2024 Sep 14. J Med Chem. 2024. PMID: 39276085
Phase 1/2a trial of intravenous BAL101553, a novel controller of the spindle assembly checkpoint, in advanced solid tumours.
Kristeleit R, Evans J, Molife LR, Tunariu N, Shaw H, Slater S, Haris NRM, Brown NF, Forster MD, Diamantis N, Rulach R, Greystoke A, Asghar U, Rata M, Anderson S, Bachmann F, Hannah A, Kaindl T, Lane HA, Larger PJ, Schmitt-Hoffmann A, Engelhardt M, Tzankov A, Plummer R, Lopez J. Kristeleit R, et al. Among authors: larger pj. Br J Cancer. 2020 Oct;123(9):1360-1369. doi: 10.1038/s41416-020-1010-8. Epub 2020 Aug 3. Br J Cancer. 2020. PMID: 32741975 Free PMC article. Clinical Trial.
A Phase 1 study of BAL101553, a novel tumor checkpoint controller targeting microtubules, administered as 48-h infusion in adult patients with advanced solid tumors.
Joerger M, Stathis A, Metaxas Y, Hess D, Mantiero M, Mark M, Volden M, Kaindl T, Engelhardt M, Larger P, Lane H, Hafner P, Levy N, Stuedeli S, Sessa C, von Moos R. Joerger M, et al. Among authors: larger p. Invest New Drugs. 2020 Aug;38(4):1067-1076. doi: 10.1007/s10637-019-00850-z. Epub 2019 Aug 30. Invest New Drugs. 2020. PMID: 31471863 Free PMC article. Clinical Trial.
Discovery, synthesis, selectivity modulation and DMPK characterization of 5-azaspiro[2.4]heptanes as potent orexin receptor antagonists.
Stasi LP, Artusi R, Bovino C, Buzzi B, Canciani L, Caselli G, Colace F, Garofalo P, Giambuzzi S, Larger P, Letari O, Mandelli S, Perugini L, Pucci S, Salvi M, Toro P. Stasi LP, et al. Among authors: larger p. Bioorg Med Chem Lett. 2013 May 1;23(9):2653-8. doi: 10.1016/j.bmcl.2013.02.093. Epub 2013 Mar 1. Bioorg Med Chem Lett. 2013. PMID: 23535328
12 results