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Page 1
Evaluation of a novel CFTR potentiator in COPD ferrets with acquired CFTR dysfunction.
Kaza N, Lin VY, Stanford D, Hussain SS, Falk Libby E, Kim H, Borgonovi M, Conrath K, Mutyam V, Byzek SA, Tang LP, Trombley JE, Rasmussen L, Schoeb T, Leung HM, Tearney GJ, Raju SV, Rowe SM. Kaza N, et al. Among authors: borgonovi m. Eur Respir J. 2022 Jul 13;60(1):2101581. doi: 10.1183/13993003.01581-2021. Print 2022 Jul. Eur Respir J. 2022. PMID: 34916262 Free PMC article.
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: borgonovi m. 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
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: borgonovi m. 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.
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: borgonovi m. 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. Among authors: borgonovi m. 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 of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
Peixoto C, Joncour A, Temal-Laib T, Tirera A, Dos Santos A, Jary H, Bucher D, Laenen W, Pereira Fernandes A, Lavazais S, Delachaume C, Merciris D, Saccomani C, Drennan M, López-Ramos M, Wakselman E, Dupont S, Borgonovi M, Roca Magadan C, Monjardet A, Brys R, De Vos S, Andrews M, Jimenez JM, Amantini D, Desroy N. Peixoto C, et al. Among authors: borgonovi m. J Med Chem. 2024 Apr 11;67(7):5233-5258. doi: 10.1021/acs.jmedchem.3c02246. Epub 2024 Mar 29. J Med Chem. 2024. PMID: 38552030 Free PMC article.
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Temal-Laib T, Peixoto C, Desroy N, De Lemos E, Bonnaterre F, Bienvenu N, Picolet O, Sartori E, Bucher D, López-Ramos M, Roca Magadán C, Laenen W, Flower T, Mollat P, Bugaud O, Touitou R, Pereira Fernandes A, Lavazais S, Monjardet A, Borgonovi M, Gosmini R, Brys R, Amantini D, De Vos S, Andrews M. Temal-Laib T, et al. Among authors: borgonovi m. J Med Chem. 2024 Jan 11;67(1):380-401. doi: 10.1021/acs.jmedchem.3c01428. Epub 2023 Dec 26. J Med Chem. 2024. PMID: 38147525 Free PMC article.
18 results