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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: conrath k. 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, 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: conrath k. 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 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: conrath k. 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
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N, Vayssiere B, De Vos S, Fletcher S, Brys R, van 't Klooster G, Feyen JH, Menet C. Van Rompaey L, et al. Among authors: conrath k. J Immunol. 2013 Oct 1;191(7):3568-77. doi: 10.4049/jimmunol.1201348. Epub 2013 Sep 4. J Immunol. 2013. PMID: 24006460
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: conrath k. 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 GLPG/ABBV-2737, a Novel Class of Corrector, Which Exerts Functional Synergy With Other CFTR Modulators.
de Wilde G, Gees M, Musch S, Verdonck K, Jans M, Wesse AS, Singh AK, Hwang TC, Christophe T, Pizzonero M, Van der Plas S, Desroy N, Cowart M, Stouten P, Nelles L, Conrath K. de Wilde G, et al. Among authors: conrath k. Front Pharmacol. 2019 May 9;10:514. doi: 10.3389/fphar.2019.00514. eCollection 2019. Front Pharmacol. 2019. PMID: 31143125 Free PMC article.
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: conrath k. 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 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: conrath k. 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
Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222.
Singh AK, Fan Y, Balut C, Alani S, Manelli AM, Swensen AM, Jia Y, Neelands TR, Vortherms TA, Liu B, Searle XB, Wang X, Gao W, Hwang TC, Ren HY, Cyr D, Kym PR, Conrath K, Tse C. Singh AK, et al. Among authors: conrath k. J Pharmacol Exp Ther. 2020 Jan;372(1):107-118. doi: 10.1124/jpet.119.261800. Epub 2019 Nov 15. J Pharmacol Exp Ther. 2020. PMID: 31732698 Free PMC article.
60 results