Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.

Autor: Mammoliti O; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Jansen K; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., El Bkassiny S; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Palisse A; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Triballeau N; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Bucher D; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Allart B; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Jaunet A; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Tricarico G; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., De Wachter M; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Menet C; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Blanc J; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Letfus V; Fidelta Ltd., Prilaz Baruna Filipovića 29, ZagrebHR-10000, Croatia., Rupčić R; Fidelta Ltd., Prilaz Baruna Filipovića 29, ZagrebHR-10000, Croatia., Šmehil M; Fidelta Ltd., Prilaz Baruna Filipovića 29, ZagrebHR-10000, Croatia., Poljak T; Fidelta Ltd., Prilaz Baruna Filipovića 29, ZagrebHR-10000, Croatia., Coornaert B; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Sonck K; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Duys I; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Waeckel L; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Lecru L; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Marsais F; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Jagerschmidt C; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Auberval M; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Pujuguet P; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Oste L; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Borgonovi M; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Wakselman E; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Christophe T; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Houvenaghel N; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Jans M; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Heckmann B; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Sanière L; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Brys R; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Oct 14; Vol. 64 (19), pp. 14557-14586. Date of Electronic Publication: 2021 Sep 28.

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.

Autor: Mammoliti O; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Palisse A; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Joannesse C; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., El Bkassiny S; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Allart B; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Jaunet A; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Menet C; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Coornaert B; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Sonck K; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Duys I; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Clément-Lacroix P; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Oste L; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Borgonovi M; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Wakselman E; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Christophe T; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Houvenaghel N; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Jans M; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium., Heckmann B; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Sanière L; Galapagos SASU, 102 avenue Gaston Roussel, 93230 Romainville, France., Brys R; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 6037-6058. Date of Electronic Publication: 2021 May 03.

Properties of Oligonucleotides with Six Membered Carbohydrate Mimics and a 1,4-Relationship Between the Base Moiety and the Hydroxymethyl Group.

Autor: Herdewijn, P., Allart, B., Bouvere, B. De, Winter, H. De, Hendrix, C., Hossain, N., Schepers, G., Verheggen, I., Wroblowski, B., Aerschot, A. Van

Publikováno v: Nucleosides & Nucleotides; Jun1999, Vol. 18 Issue 6/7, p1371-1376, 6p

Technical assistance: Two method for tracking of a wheelchair.

Autor: Allart, B., Marhic, B., Delahoche, L., Remy-Neris, O., Jolly-Desodt, A.M.

Publikováno v: 2008 IEEE International Conference on Multisensor Fusion & Integration for Intelligent Systems; 2008, p252-257, 6p

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