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Page 1
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: saniere 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 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: saniere 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 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: saniere 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: saniere 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
The Medium-Chain Fatty Acid Receptor GPR84 Mediates Myeloid Cell Infiltration Promoting Steatohepatitis and Fibrosis.
Puengel T, De Vos S, Hundertmark J, Kohlhepp M, Guldiken N, Pujuguet P, Auberval M, Marsais F, Shoji KF, Saniere L, Trautwein C, Luedde T, Strnad P, Brys R, Clément-Lacroix P, Tacke F. Puengel T, et al. Among authors: saniere l. J Clin Med. 2020 Apr 16;9(4):1140. doi: 10.3390/jcm9041140. J Clin Med. 2020. PMID: 32316235 Free PMC article.
Reinvestigation of the Branimycin Stereochemistry at Position 17-C.
Čikoš A, Triballeau N, Hubbard PA, Žiher D, Stouten PF, Doyon JG, Deschrijver T, Wouters J, Lépine RH, Saniere L. Čikoš A, et al. Among authors: saniere l. Org Lett. 2016 Feb 19;18(4):780-3. doi: 10.1021/acs.orglett.6b00044. Epub 2016 Feb 5. Org Lett. 2016. PMID: 26849068
The Small Molecule Ephrin Receptor Inhibitor, GLPG1790, Reduces Renewal Capabilities of Cancer Stem Cells, Showing Anti-Tumour Efficacy on Preclinical Glioblastoma Models.
Gravina GL, Mancini A, Colapietro A, Delle Monache S, Sferra R, Vitale F, Cristiano L, Martellucci S, Marampon F, Mattei V, Beirinckx F, Pujuguet P, Saniere L, Lorenzon G, van der Aar E, Festuccia C. Gravina GL, et al. Among authors: saniere l. Cancers (Basel). 2019 Mar 13;11(3):359. doi: 10.3390/cancers11030359. Cancers (Basel). 2019. PMID: 30871240 Free PMC article.
Antitumorigenic Effects of Inhibiting Ephrin Receptor Kinase Signaling by GLPG1790 against Colorectal Cancer Cell Lines In Vitro and In Vivo.
Colapietro A, Gravina GL, Petragnano F, Fasciani I, Scicchitano BM, Beirinckx F, Pujuguet P, Saniere L, Van der Aar E, Musio D, De Felice F, Mattei V, Martellucci S, Maggio R, Tombolini V, Festuccia C, Marampon F. Colapietro A, et al. Among authors: saniere l. J Oncol. 2020 Feb 27;2020:9342732. doi: 10.1155/2020/9342732. eCollection 2020. J Oncol. 2020. PMID: 32184826 Free PMC article.
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Hamilton E, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Scullion P, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Bruin J, Hamilton W, Uitdehaag J, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Rankovic Z, et al. Among authors: saniere l. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. doi: 10.1016/j.bmcl.2010.01.100. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20149657
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Finlay W, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Arbuckle W, Anderson M, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Jones P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Rankovic Z, et al. Among authors: saniere l. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6237-41. doi: 10.1016/j.bmcl.2010.08.101. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20843687
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