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-Reference-Cited by-同舟云学术

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

Published:2020-09-09 Issue:22 Volume:63 Page:13526-13545
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Labéguère Frédéric¹,Dupont Sonia¹,Alvey Luke¹,Soulas Florilène¹,Newsome Gregory¹,Tirera Amynata¹,Quenehen Vanessa¹,Mai Thi Thu Trang¹,Deprez Pierre¹,Blanqué Roland¹,Oste Line²,Le Tallec Sandrine¹,De Vos Steve²,Hagers Annick²,Vandevelde Ann²,Nelles Luc²,Vandervoort Nele²,Conrath Katja²,Christophe Thierry²,van der Aar Ellen²,Wakselman Emanuelle¹,Merciris Didier¹,Cottereaux Céline¹,da Costa Cécile¹,Saniere Laurent¹,Clement-Lacroix Philippe¹,Jenkins Laura³,Milligan Graeme³^ORCID,Fletcher Stephen²,Brys Reginald²,Gosmini Romain¹

Affiliation:

1. Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France

2. Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium

3. 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

Funder

Galapagos

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

http://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c00272

Reference32 articles.

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2. International Union of Basic and Clinical Pharmacology. LXXXVIII. G Protein-Coupled Receptor List: Recommendations for New Pairings with Cognate Ligands

3. Medium-chain Fatty Acid-sensing Receptor, GPR84, Is a Proinflammatory Receptor