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Page 1
Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.
Mammoliti O, Jansen K, El Bkassiny S, Palisse A, Triballeau N, Bucher D, Allart B, Jaunet A, Tricarico G, De Wachter M, Menet C, Blanc J, Letfus V, Rupčić R, Šmehil M, Poljak T, Coornaert B, Sonck K, Duys I, Waeckel L, Lecru L, Marsais F, Jagerschmidt C, Auberval M, Pujuguet P, Oste L, Borgonovi M, Wakselman E, Christophe T, Houvenaghel N, Jans M, Heckmann B, Sanière L, Brys R. Mammoliti O, et al. Among authors: triballeau n. J Med Chem. 2021 Oct 14;64(19):14557-14586. doi: 10.1021/acs.jmedchem.1c01066. Epub 2021 Sep 28. J Med Chem. 2021. PMID: 34581584
Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis.
Desroy N, Housseman C, Bock X, Joncour A, Bienvenu N, Cherel L, Labeguere V, Rondet E, Peixoto C, Grassot JM, Picolet O, Annoot D, Triballeau N, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Blanque R, Cottereaux C, Vandervoort N, Christophe T, Mollat P, Lamers M, Auberval M, Hrvacic B, Ralic J, Oste L, van der Aar E, Brys R, Heckmann B. Desroy N, et al. Among authors: triballeau n. J Med Chem. 2017 May 11;60(9):3580-3590. doi: 10.1021/acs.jmedchem.7b00032. Epub 2017 May 1. J Med Chem. 2017. PMID: 28414242
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
Pizzonero M, Dupont S, Babel M, Beaumont S, Bienvenu N, Blanqué R, Cherel L, Christophe T, Crescenzi B, De Lemos E, Delerive P, Deprez P, De Vos S, Djata F, Fletcher S, Kopiejewski S, L'Ebraly C, Lefrançois JM, Lavazais S, Manioc M, Nelles L, Oste L, Polancec D, Quénéhen V, Soulas F, Triballeau N, van der Aar EM, Vandeghinste N, Wakselman E, Brys R, Saniere L. Pizzonero M, et al. Among authors: triballeau n. J Med Chem. 2014 Dec 11;57(23):10044-57. doi: 10.1021/jm5012885. Epub 2014 Dec 1. J Med Chem. 2014. PMID: 25380412
Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B. Joncour A, et al. Among authors: triballeau n. J Med Chem. 2017 Sep 14;60(17):7371-7392. doi: 10.1021/acs.jmedchem.7b00647. Epub 2017 Aug 18. J Med Chem. 2017. PMID: 28731719
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Brebion F, Gosmini R, Deprez P, Varin M, Peixoto C, Alvey L, Jary H, Bienvenu N, Triballeau N, Blanque R, Cottereaux C, Christophe T, Vandervoort N, Mollat P, Touitou R, Leonard P, De Ceuninck F, Botez I, Monjardet A, van der Aar E, Amantini D. Brebion F, et al. Among authors: triballeau n. J Med Chem. 2021 Mar 25;64(6):2937-2952. doi: 10.1021/acs.jmedchem.0c02008. Epub 2021 Mar 15. J Med Chem. 2021. PMID: 33719441 Free article.
Correction to Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2- a]pyridine Series of Autotaxin Inhibitors.
Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B. Joncour A, et al. Among authors: triballeau n. J Med Chem. 2018 May 10;61(9):4270. doi: 10.1021/acs.jmedchem.8b00579. Epub 2018 Apr 19. J Med Chem. 2018. PMID: 29672037 No abstract available.
Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator.
Nique F, Hebbe S, Triballeau N, Peixoto C, Lefrançois JM, Jary H, Alvey L, Manioc M, Housseman C, Klaassen H, Van Beeck K, Guédin D, Namour F, Minet D, Van der Aar E, Feyen J, Fletcher S, Blanqué R, Robin-Jagerschmidt C, Deprez P. Nique F, et al. Among authors: triballeau n. J Med Chem. 2012 Oct 11;55(19):8236-47. doi: 10.1021/jm300281x. Epub 2012 Sep 25. J Med Chem. 2012. PMID: 22957947
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
Schann S, Menet C, Arvault P, Mercier G, Frauli M, Mayer S, Hubert N, Triballeau N, Bertrand HO, Acher F, Neuville P. Schann S, et al. Among authors: triballeau n. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4856-60. doi: 10.1016/j.bmcl.2006.06.062. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16828551
Discovery of diarylhydantoins as new selective androgen receptor modulators.
Nique F, Hebbe S, Peixoto C, Annoot D, Lefrançois JM, Duval E, Michoux L, Triballeau N, Lemoullec JM, Mollat P, Thauvin M, Prangé T, Minet D, Clément-Lacroix P, Robin-Jagerschmidt C, Fleury D, Guédin D, Deprez P. Nique F, et al. Among authors: triballeau n. J Med Chem. 2012 Oct 11;55(19):8225-35. doi: 10.1021/jm300249m. Epub 2012 Sep 25. J Med Chem. 2012. PMID: 22897611
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