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Page 1
Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.
Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Yan W, Merton KP, Schoetens F, Ma JY, Skaptason J, Gao J, Tran DT, Venkatesan H, Rosen MD, Shankley NP, Rabinowitz MH. Barrett TD, et al. Among authors: schoetens f. Br J Pharmacol. 2015 Aug;172(16):4078-88. doi: 10.1111/bph.13188. Epub 2015 Jun 26. Br J Pharmacol. 2015. PMID: 25988595 Free PMC article.
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA. Swanson DM, et al. Among authors: schoetens f. J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8. J Med Chem. 2016. PMID: 27548392
Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534.
Xue X, De Leon-Tabaldo A, Luna-Roman R, Castro G, Albers M, Schoetens F, DePrimo S, Devineni D, Wilde T, Goldberg S, Kinzel O, Hoffmann T, Fourie AM, Thurmond RL. Xue X, et al. Among authors: schoetens f. Sci Rep. 2021 May 26;11(1):11066. doi: 10.1038/s41598-021-90497-9. Sci Rep. 2021. PMID: 34040108 Free PMC article. Clinical Trial.
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A. Letavic MA, et al. Among authors: schoetens f. J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25. J Med Chem. 2017. PMID: 28493698
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Chrovian CC, Soyode-Johnson A, Peterson AA, Gelin CF, Deng X, Dvorak CA, Carruthers NI, Lord B, Fraser I, Aluisio L, Coe KJ, Scott B, Koudriakova T, Schoetens F, Sepassi K, Gallacher DJ, Bhattacharya A, Letavic MA. Chrovian CC, et al. Among authors: schoetens f. J Med Chem. 2018 Jan 11;61(1):207-223. doi: 10.1021/acs.jmedchem.7b01279. Epub 2017 Dec 20. J Med Chem. 2018. PMID: 29211470
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Chrovian CC, Soyode-Johnson A, Stenne B, Pippel DJ, Schoellerman J, Lord B, Needham AS, Xia C, Coe KJ, Sepassi K, Schoetens F, Scott B, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: schoetens f. J Med Chem. 2020 Sep 10;63(17):9181-9196. doi: 10.1021/acs.jmedchem.9b02113. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32787105