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Page 1
Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors.
Velcicky J, Janser P, Gommermann N, Brenneisen S, Ilic S, Vangrevelinghe E, Stiefl N, Boettcher A, Arnold C, Malinverni C, Dawson J, Murgasova R, Desrayaud S, Beltz K, Hinniger A, Dekker C, Farady CJ, Mackay A. Velcicky J, et al. Among authors: vangrevelinghe e. J Med Chem. 2024 Jan 25;67(2):1544-1562. doi: 10.1021/acs.jmedchem.3c02098. Epub 2024 Jan 4. J Med Chem. 2024. PMID: 38175811
Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.
Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM. Weigert O, et al. Among authors: vangrevelinghe e. J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23. J Exp Med. 2012. PMID: 22271575 Free PMC article.
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P. Gerspacher M, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138510
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Pissot-Soldermann C, Gerspacher M, Furet P, Gaul C, Holzer P, McCarthy C, Radimerski T, Regnier CH, Baffert F, Drueckes P, Tavares GA, Vangrevelinghe E, Blasco F, Ottaviani G, Ossola F, Scesa J, Reetz J. Pissot-Soldermann C, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2609-13. doi: 10.1016/j.bmcl.2010.02.056. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20231096
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.
van Eis MJ, Evenou JP, Floersheim P, Gaul C, Cowan-Jacob SW, Monovich L, Rummel G, Schuler W, Stark W, Strauss A, von Matt A, Vangrevelinghe E, Wagner J, Soldermann N. van Eis MJ, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7367-72. doi: 10.1016/j.bmcl.2011.10.025. Epub 2011 Oct 21. Bioorg Med Chem Lett. 2011. PMID: 22078216
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK. Ostermann N, et al. Among authors: vangrevelinghe e. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
Syk inhibitors with high potency in presence of blood.
Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H. Thoma G, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. doi: 10.1016/j.bmcl.2014.03.075. Epub 2014 Apr 3. Bioorg Med Chem Lett. 2014. PMID: 24726806
Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.
Shaw D, Hollingworth G, Soldermann N, Sprague E, Schuler W, Vangrevelinghe E, Duggan N, Thomas M, Kosaka T, Waters N, van Eis MJ. Shaw D, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4812-7. doi: 10.1016/j.bmcl.2014.09.002. Epub 2014 Sep 6. Bioorg Med Chem Lett. 2014. PMID: 25248678
31 results