Galapagos BE0003818359

GLPG2938

1. Pokerface 16 juni 2016 16:18

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   • Pokerface

     Lid sinds: 27 mrt 2001

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   GLPG2938
   Ziekte 1: Idiopatische Longfibrose (IPF)
   Ziekte 2: NASH ???
   Start fase 1: H2 2017
2. Pokerface 24 februari 2017 14:40

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   • Pokerface

     Lid sinds: 27 mrt 2001

     Laatste bezoek: 19 apr 2024

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   Het ligt nog steeds in de planning om in 2017 een Fase 1 studie te starten met GLPG2938. Verder nog weinig bekend over dit molecuul.
3. Lama Daila 21 juni 2021 07:30

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   • Lama Daila

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   drughunter.com/small-molecules-of-the...
   
   The Galapagos S1PR2 antagonist GLPG2938 is a preclinical candidate intended for the treatment of idiopathic pulmonary fibrosis (IPF). Though several S1PR1 modulators have been approved, no selective S1PR2 antagonist has entered clinical development yet. The Galapagos team attempted to find a new starting point with two consecutive HTS campaigns, but did not find any advanceable starting points, but were able to develop a literature starting point to a candidate. A hydrazine motif in the starting point was replaced with a benzylic amine in a surprisingly large property change for a central motif. Improving lipophilic efficiency was key to reducing CYP inhibition. GLPG2938 does not appear to have entered development yet, but should be a useful tool to understand S1PR2 biology.
   
   pubs.acs.org/doi/10.1021/acs.jmedchem...
   
   Publication Date:May 3, 2021
   
   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