未登录 IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases IRAK4抑制抑制驱动炎症性皮肤病的致病过程 Lavazais, Stephanie; Jargosch, Manja; Dupont, Sonia; Labeguere, Frederic; Menet, Christel; Jagerschmidt, Catherine; Ohm, Frenz; Kupcsik, Laszlo; Parent, Isabelle; Cottereaux, Celine; Marsais, Florence; Oste, Line; Van de Water, An; Christophe, Thierry; De Vos, Steve; Fallon, Padraic; Lauffer, Felix; Clement-Lacroix, Philippe; Eyerich, Kilian; Brys, Reginald 分享 收藏
Pharmacological characterization of GLPG1972/S201086, a potent and selective small-molecule inhibitor of ADAMTS5 Clement-Lacroix, P.; Little, C. B.; Smith, M. M.; Cottereaux, C.; Merciris, D.; Meurisse, S.; Mollat, P.; Touitou, R.; Brebion, F.; Gosmini, R.; De Ceuninck, F.; Botez, I; Lepescheux, L.; van der Aar, E.; Christophe, T.; Vandervoort, N.; Blanque, R.; Comas, D.; Deprez, P.; Amantini, D. 分享 收藏
Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases Mammoliti, Oscar; Jansen, Koen; El Bkassiny, Sandy; Palisse, Adeline; Triballeau, Nicolas; Bucher, Denis; Allart, Brigitte; Jaunet, Alex; Tricarico, Giovanni; De Wachter, Maxim; Menet, Christel; Blanc, Javier; Letfus, Vatroslav; Rupcic, Renata; Smehil, Mario; Poljak, Tanja; Coornaert, Beatrice; Sonck, Kathleen; Duys, Inge; Waeckel, Ludovic; Lecru, Lola; Marsais, Florence; Jagerschmidt, Catherine; Auberval, Marielle; Pujuguet, Philippe; Oste, Line; Borgonovi, Monica; Wakselman, Emanuelle; Christophe, Thierry; Houvenaghel, Nicolas; Jans, Mia; Heckmann, Bertrand; Saniere, Laurent; Brys, Reginald 分享 收藏
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, Oscar; Palisse, Adeline; Joannesse, Caroline; El Bkassiny, Sandy; Allart, Brigitte; Jaunet, Alex; Menet, Christel; Coornaert, Beatrice; Sonck, Kathleen; Duys, Inge; Clement-Lacroix, Philippe; Oste, Line; Borgonovi, Monica; Wakselman, Emanuelle; Christophe, Thierry; Houvenaghel, Nicolas; Jans, Mia; Heckmann, Bertrand; Saniere, Laurent; Brys, Reginald 分享 收藏
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis Brebion, Franck; Gosmini, Romain; Deprez, Pierre; Varin, Marie; Peixoto, Christophe; Alvey, Luke; Jary, Helene; Bienvenu, Natacha; Triballeau, Nicolas; Blanque, Roland; Cottereaux, Celine; Christophe, Thierry; Vandervoort, Nele; Mollat, Patrick; Touitou, Robert; Leonard, Philip; De Ceuninck, Frederic; Botez, Iuliana; Monjardet, Alain; van der Aar, Ellen; Amantini, David 分享 收藏
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 Labeguere, Frederic; Dupont, Sonia; Alvey, Luke; Soulas, Florilene; Newsome, Gregory; Tirera, Amynata; Quenehen, Vanessa; Thi Thu Trang Mai; Deprez, Pierre; Blanque, 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, Celine; da Costa, Cecile; Saniere, Laurent; Clement-Lacroix, Philippe; Jenkins, Laura; Milligan, Graeme; Fletcher, Stephen; Brys, Reginald; Gosmini, Romain 分享 收藏
Discovery, Structure Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors (vol 60, pg 7371, 2017) Joncour, Agnes; Desroy, Nicolas; Housseman, Christopher; Bock, Xavier; Bienvenu, Natacha; Cherel, Laetitia; Labeguere, Virginie; Peixoto, Christophe; Annoot, Denis; Lepissier, Luce; Heiermann, Jorg; Hengeveld, Willem Jan; Pilzak, Gregor; Monjardet, Alain; Wakselman, Emanuelle; Roncoroni, Veronique; Le Tallec, Sandrine; Galien, Rene; David, Christelle; Vandervoort, Nele; Christophe, Thierry; Conrath, Katja; Jans, Mia; Wohlkonig, Alexandre; Soror, Sameh; Steyaert, Jan; Touitou, Robert; Fleury, Damien; Vercheval, Lionel; Mollat, Patrick; Triballeau, Nicolas; van der Aar, Ellen; Brys, Reginald; Heckmann, Bertrand 分享 收藏
ADAMTS-5 INHIBITION WITH THE POTENT AND HIGHLY SELECTIVE INHIBITOR GLPG1972 RESULTS IN STRONG DISEASE-MODIFYING OA DRUG EFFECTS IN THE RAT MENISCECTOMY MODEL Clement-Lacroix, P.; Meurisse, S.; Lepescheux, L.; Merciris, D.; Borgonovi, M.; Cottereaux, C.; Mollat, P.; Brebion, F.; Gosmini, R.; De Ceuninck, F.; Botez, I.; Christophe, T.; van der Aar, E. E.; Vandervoort, N.; Blanque, R.; Comas, D.; Deprez, P.; Amantini, D. 分享 收藏
Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent Van der Plas, Steven E.; Kelgtermans, Hans; De Munck, Tom; Martina, Sebastien L. X.; Dropsit, Sebastien; Quinton, Evelyne; De Blieck, Ann; Joannesse, Caroline; Tomaskovic, Linda; Jans, Mia; Christophe, Thierry; van der Aar, Ellen; Borgonovi, Monica; Nelles, Luc; Gees, Maarten; Stouten, Pieter; Van Der Schueren, Jan; Mammoliti, Oscar; Conrath, Katja; Andrews, Martin 分享 收藏
Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors Joncour, Agnes; Desroy, Nicolas; Housseman, Christopher; Bock, Xavier; Bienvenu, Natacha; Cherel, Laetitia; Labeguere, Virginie; Peixoto, Christophe; Annoot, Denis; Lepissier, Luce; Heiermann, Jorg; Hengeveld, Willem Jan; Pilzak, Gregor; Monjardet, Alain; Wakselman, Emanuelle; Roncoroni, Veronique; Le Tallec, Sandrine; Gallen, Rene; David, Christelle; Vandervoort, Nele; Christophe, Thierry; Conrath, Katja; Jans, Mia; Wohlkonig, Alexandre; Soror, Sameh; Steyaert, Jan; Touitou, Robert; Fleury, Damien; Vercheval, Lionel; Mollat, Patrick; Triballeau, Nicolas; van der Aar, Ellen; Brys, Reginald; Heckmann, Bertrand 分享 收藏
Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis Desroy, Nicolas; Housseman, Christopher; Bock, Xavier; Joncour, Agnes; Bienvenu, Natacha; Cherel, Laetitia; Labeguere, Virginie; Rondet, Emilie; Peixoto, Christophe; Grassot, Jean-Marie; Picolet, Olivier; Annoott, Denis; Triballeau, Nicolas; Monjardet, Alain; Wakselman, Emanuelle; Roncoroni, Veronique; Le Tallec, Sandrine; Blanque, Roland; Cottereaux, Celine; Vandervoort, Nele; Christophe, Thierry; Mollat, Patrick; Lamers, Marieke; Auberval, Marielle; Hrvacic, Boska; Ralic, Jovica; Oste, Line; van der Aar, Ellen; Brys, Reginald; Heckmann, Bertrand 分享 收藏
GLPG1972: A POTENT, SELECTIVE, ORALLY AVAILABLE ADAMTS-5 INHIBITOR FOR THE TREATMENT OF OA Clement-Lacroix, P.; Little, C.; Meurisse, S.; Blanque, R.; Mollat, P.; Brebion, F.; Gosmini, R.; De Ceuninck, F.; Botez, I.; Lepescheux, L.; van der Aar, E.; Christophe, T.; Vandervoort, N.; Cottereaux, C.; Comas, D.; Deprez, P.; Amantini, D. 分享 收藏
Discovery and Optimization of an Azetidine Chemical Series As a Free Fatty Acid Receptor 2 (FFA2) Antagonist: From Hit to Clinic Pizzonero, Mathieu; Dupont, Sonia; Babel, Marielle; Beaumont, Stephane; Bienvenu, Natacha; Blanque, Roland; Cherel, Laetitia; Christophe, Thierry; Crescenzi, Benedetta; De Lemos, Elsa; Delerive, Philippe; Deprez, Pierre; De Vos, Steve; Djata, Fatoumata; Fletcher, Stephen; Kopiejewski, Sabrina; L'Ebraly, Christelle; Lefrancois, Jean-Michel; Lavazais, Stephanie; Manioc, Murielle; Nelles, Luc; Oste, Line; Polancec, Denis; Quenehen, Vanessa; Soulas, Florilene; Triballeau, Nicolas; van der Aar, Ellen M.; Vandeghinste, Nick; Wakselman, Emanuelle; Brys, Reginald; Saniere, Laurent 分享 收藏
Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634 Menet, Christel J.; Fletcher, Stephen R.; Van Lommen, Guy; Geney, Raphael; Blanc, Javier; Smits, Koen; Jouannigot, Nolwenn; Deprez, Pierre; van der Aar, Ellen M.; Clement-Lacroix, Philippe; Lepescheux, Lien; Galien, Rene; Vayssiere, Beatrice; Nelles, Luc; Christophe, Thierry; Brys, Reginald; Uhring, Muriel; Ciesieski, Fabrice; Van Rompaey, Luc 分享 收藏
GLPG0634M1, A MAJOR METABOLITE OF THE JAK1-SELECTIVE INHIBITOR GLPG0634, IS ALSO JAK1-SELECTIVE AND EFFICIENT IN THE RAT CIA MODEL Belleville-Da-Costa, C.; Merciris, D.; Vayssiere, B.; Houvenaghel, N.; Monjardet, A.; Lepescheux, L.; Dupont, S.; Christophe, T.; Borgonovi, M.; Clement-Lacroix, P.; Menet, C.; Van Rompaey, L.; Brys, R.; Galien, R. 分享 收藏
Preclinical Characterization of GLPG0634, a Selective Inhibitor of JAK1, for the Treatment of Inflammatory Diseases Van Rompaey, Luc; Galien, Rene; van der Aar, Ellen M.; Clement-Lacroix, Philippe; Nelles, Luc; Smets, Bart; Lepescheux, Lien; Christophe, Thierry; Conrath, Katja; Vandeghinste, Nick; Vayssiere, Beatrice; De Vos, Steve; Fletcher, Stephen; Brys, Reginald; van 't Klooster, Gerben; Feyen, Jean H. M.; Menet, Christel 分享 收藏
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis Pethe, Kevin; Bifani, Pablo; Jang, Jichan; Kang, Sunhee; Park, Seijin; Ahn, Sujin; Jiricek, Jan; Jung, Juyoung; Jeon, Hee Kyoung; Cechetto, Jonathan; Christophe, Thierry; Lee, Honggun; Kempf, Marie; Jackson, Mary; Lenaerts, Anne J.; Ha Pham; Jones, Victoria; Seo, Min Jung; Kim, Young Mi; Seo, Mooyoung; Seo, Jeong Jea; Park, Dongsik; Ko, Yoonae; Choi, Inhee; Kim, Ryangyeo; Kim, Se Yeon; Lim, SeungBin; Yim, Seung-Ae; Nam, Jiyoun; Kang, Hwankyu; Kwon, Haejin; Oh, Chun-Taek; Cho, Yoojin; Jang, Yunhee; Kim, Junghwan; Chua, Adeline; Tan, Bee Huat; Nanjundappa, Mahesh B.; Rao, Srinivasa P. S.; Barnes, Whitney S.; Wintjens, Rene; Walker, John R.; Alonso, Sylvie; Lee, Saeyeon; Kim, Jungjun; Oh, Soohyun; Oh, Taegwon; Nehrbass, Ulf; Han, Sung-Jun; No, Zaesung; Lee, Jinhwa; Brodin, Priscille; Cho, Sang-Nae; Nam, Kiyean; Kim, Jaeseung 分享 收藏
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis Flipo, Marion; Willand, Nicolas; Lecat-Guillet, Nathalie; Hounsou, Candide; Desroses, Matthieu; Leroux, Florence; Lens, Zoe; Villeret, Vincent; Wohlkonig, Alexandre; Wintjens, Rene; Christophe, Thierry; Jeon, Hee Kyoung; Locht, Camille; Brodin, Priscille; Baulard, Alain R.; Deprez, Benoit 分享 收藏
New taxonomy and old collections: integrating DNA barcoding into the collection curation process Puillandre, N.; Bouchet, P.; Boisselier-Dubayle, M. -C.; Brisset, J.; Buge, B.; Castelin, M.; Chagnoux, S.; Christophe, T.; Corbari, L.; Lambourdiere, J.; Lozouet, P.; Marani, G.; Rivasseau, A.; Silva, N.; Terryn, Y.; Tillier, S.; Utge, J.; Samadi, S. 分享 收藏
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors Flipo, Marion; Desroses, Matthieu; Lecat-Guillet, Nathalie; Villemagne, Baptiste; Blondiaux, Nicolas; Leroux, Florence; Piveteau, Catherine; Mathys, Vanessa; Flament, Marie-Pierre; Siepmann, Juergen; Villeret, Vincent; Wohlkonig, Alexandre; Wintjens, Rene; Soror, Sameh H.; Christophe, Thierry; Jeon, Hee Kyoung; Locht, Camille; Brodin, Priscille; Deprez, Benoit; Baulard, Alain R.; Willand, Nicolas 分享 收藏
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