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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. 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 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. 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
Progress toward JAK1-selective inhibitors.
Menet CJ, Mammoliti O, López-Ramos M. Menet CJ, et al. Among authors: mammoliti o. Future Med Chem. 2015;7(2):203-35. doi: 10.4155/fmc.14.149. Future Med Chem. 2015. PMID: 25686006 Review.
Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis.
Van der Plas SE, Kelgtermans H, Mammoliti O, Menet C, Tricarico G, De Blieck A, Joannesse C, De Munck T, Lambin D, Cowart M, Dropsit S, Martina SLX, Gees M, Wesse AS, Conrath K, Andrews M. Van der Plas SE, et al. Among authors: mammoliti o. J Med Chem. 2021 Jan 14;64(1):343-353. doi: 10.1021/acs.jmedchem.0c01796. Epub 2021 Jan 5. J Med Chem. 2021. PMID: 33399458
Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.
Van der Plas SE, Kelgtermans H, De Munck T, Martina SLX, Dropsit S, Quinton E, De Blieck A, Joannesse C, Tomaskovic L, Jans M, Christophe T, van der Aar E, Borgonovi M, Nelles L, Gees M, Stouten P, Van Der Schueren J, Mammoliti O, Conrath K, Andrews M. Van der Plas SE, et al. Among authors: mammoliti o. J Med Chem. 2018 Feb 22;61(4):1425-1435. doi: 10.1021/acs.jmedchem.7b01288. Epub 2018 Jan 10. J Med Chem. 2018. PMID: 29148763
Correction to "Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis".
Van der Plas SE, Kelgtermans H, Mammoliti O, Menet C, Tricarico G, De Blieck A, Joannesse C, De Munck T, Lambin D, Cowart M, Dropsit S, Martina SLX, Gees M, Wesse AS, Conrath K, Andrews M. Van der Plas SE, et al. Among authors: mammoliti o. J Med Chem. 2021 Sep 23;64(18):13933. doi: 10.1021/acs.jmedchem.1c01537. Epub 2021 Sep 14. J Med Chem. 2021. PMID: 34520202 No abstract available.
Identification and Characterization of Novel CFTR Potentiators.
Gees M, Musch S, Van der Plas S, Wesse AS, Vandevelde A, Verdonck K, Mammoliti O, Hwang TC, Sonck K, Stouten P, Swensen AM, Jans M, Van der Schueren J, Nelles L, Andrews M, Conrath K. Gees M, et al. Among authors: mammoliti o. Front Pharmacol. 2018 Oct 26;9:1221. doi: 10.3389/fphar.2018.01221. eCollection 2018. Front Pharmacol. 2018. PMID: 30416447 Free PMC article.
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
Pizzonero M, Akkari R, Bock X, Gosmini R, De Lemos E, Duthion B, Newsome G, Mai TT, Roques V, Jary H, Lefrancois JM, Cherel L, Quenehen V, Babel M, Merayo N, Bienvenu N, Mammoliti O, Coti G, Palisse A, Cowart M, Shrestha A, Greszler S, Van Der Plas S, Jansen K, Claes P, Jans M, Gees M, Borgonovi M, De Wilde G, Conrath K. Pizzonero M, et al. Among authors: mammoliti o. J Med Chem. 2024 Apr 11;67(7):5216-5232. doi: 10.1021/acs.jmedchem.3c01790. Epub 2024 Mar 25. J Med Chem. 2024. PMID: 38527911 Free PMC article.