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Page 1
Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
Labéguère F, Dupont S, Alvey L, Soulas F, Newsome G, Tirera A, Quenehen V, Mai TTT, Deprez P, Blanqué R, Oste L, Le Tallec S, De Vos S, Hagers A, Vandevelde A, Nelles L, Vandervoort N, Conrath K, Christophe T, van der Aar E, Wakselman E, Merciris D, Cottereaux C, da Costa C, Saniere L, Clement-Lacroix P, Jenkins L, Milligan G, Fletcher S, Brys R, Gosmini R. Labéguère F, et al. Among authors: oste l. J Med Chem. 2020 Nov 25;63(22):13526-13545. doi: 10.1021/acs.jmedchem.0c00272. Epub 2020 Sep 23. J Med Chem. 2020. PMID: 32902984 Free article. Clinical Trial.
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: l ebraly c, oste l. 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 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: oste l. 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 of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
Mammoliti O, Palisse A, Joannesse C, El Bkassiny S, Allart B, Jaunet A, Menet C, Coornaert B, Sonck K, Duys I, Clément-Lacroix 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: oste l. J Med Chem. 2021 May 13;64(9):6037-6058. doi: 10.1021/acs.jmedchem.1c00138. Epub 2021 May 3. J Med Chem. 2021. PMID: 33939425
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: oste l. 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
IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases.
Lavazais S, Jargosch M, Dupont S, Labéguère F, Menet C, Jagerschmidt C, Ohm F, Kupcsik L, Parent I, Cottereaux C, Marsais F, Oste L, Van de Water A, Christophe T, De Vos S, Fallon P, Lauffer F, Clément-Lacroix P, Eyerich K, Brys R. Lavazais S, et al. Among authors: oste l. Sci Transl Med. 2023 Feb 15;15(683):eabj3289. doi: 10.1126/scitranslmed.abj3289. Epub 2023 Feb 15. Sci Transl Med. 2023. PMID: 36791209
Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.
Mammoliti O, Martina S, Claes P, Coti G, Blanque R, Jagerschmidt C, Shoji K, Borgonovi M, De Vos S, Marsais F, Oste L, Quinton E, López-Ramos M, Amantini D, Brys R, Jimenez JM, Galien R, van der Plas S. Mammoliti O, et al. Among authors: oste l. J Med Chem. 2024 Jun 13;67(11):8545-8568. doi: 10.1021/acs.jmedchem.4c00769. Epub 2024 May 28. J Med Chem. 2024. PMID: 38805213 Free PMC article. Clinical Trial.
A multiparameter approach to monitor disease activity in collagen-induced arthritis.
Seeuws S, Jacques P, Van Praet J, Drennan M, Coudenys J, Decruy T, Deschepper E, Lepescheux L, Pujuguet P, Oste L, Vandeghinste N, Brys R, Verbruggen G, Elewaut D. Seeuws S, et al. Among authors: oste l. Arthritis Res Ther. 2010;12(4):R160. doi: 10.1186/ar3119. Epub 2010 Aug 23. Arthritis Res Ther. 2010. PMID: 20731827 Free PMC article.
24 results