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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, Frédéric; Dupont, Sonia; Alvey, Luke; Soulas, Florilène; Newsome, Gregory; Tirera, Amynata; Quenehen, Vanessa; Mai, Thi Thu Trang; Deprez, Pierre; Blanqué, Roland; Oste, Line; Le Tallec, Sandrine; De Vos, Steve; Hagers, Annick; Vandevelde, Ann; Nelles, Luc; Vandervoort, Nele; Conrath, Katja; Christophe, Thierry; van der Aar, Ellen; Wakselman, Emanuelle; Merciris, Didier; Cottereaux, Céline; da Costa, Cécile; Saniere, Laurent; Clement-Lacroix, Philippe; Jenkins, Laura; Milligan, Graeme; Fletcher, Stephen; Brys, Reginald; Gosmini, Romain.
Afiliação
  • Labéguère F; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Dupont S; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Alvey L; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Soulas F; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Newsome G; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Tirera A; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Quenehen V; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Mai TTT; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Deprez P; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Blanqué R; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Oste L; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Le Tallec S; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • De Vos S; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Hagers A; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Vandevelde A; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Nelles L; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Vandervoort N; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Conrath K; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Christophe T; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • van der Aar E; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Wakselman E; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Merciris D; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Cottereaux C; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • da Costa C; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Saniere L; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Clement-Lacroix P; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
  • Jenkins L; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, United Kingdom.
  • Milligan G; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, United Kingdom.
  • Fletcher S; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Brys R; Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium.
  • Gosmini R; Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
J Med Chem ; 63(22): 13526-13545, 2020 11 25.
Article em En | MEDLINE | ID: mdl-32902984
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores Acoplados a Proteínas G / Descoberta de Drogas Tipo de estudo: Clinical_trials / Prognostic_studies Limite: Animals / Female / Humans / Male Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores Acoplados a Proteínas G / Descoberta de Drogas Tipo de estudo: Clinical_trials / Prognostic_studies Limite: Animals / Female / Humans / Male Idioma: En Ano de publicação: 2020 Tipo de documento: Article