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Page 1
Thiazole-based IL-17 inhibitors discovered by scaffold morphing.
Velcicky J, Ngo E, Bauer MR, Meyer A, Schlapbach A, Racine S, Orain D, Pflieger D, Teixeira-Fouchard S, Dubois C, Goetz A, Steiner R, Palmieri M, Bussenault A, Stringer R, Larger P, Riek S, Schmutz P, Lehmann S, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: gommermann n. ChemMedChem. 2024 Dec 23:e202400851. doi: 10.1002/cmdc.202400851. Online ahead of print. ChemMedChem. 2024. PMID: 39715021
Discovery of NP3-253, a Potent Brain Penetrant Inhibitor of the NLRP3 Inflammasome.
Mackay A, Velcicky J, Gommermann N, Mattes H, Janser P, Wright M, Dubois C, Brenneisen S, Ilic S, Vangrevelinghe E, Stiefl N, Boettcher A, Schoenboerner M, Vogelsanger M, Muller-Bentz S, Kamke M, Rubert J, Kauffmann M, Desrayaud S, Trunzer M, Srinivas H, Hinniger A, von Burg N, Beltz K, Dekker C, Farady CJ. Mackay A, et al. Among authors: gommermann n. J Med Chem. 2024 Dec 12;67(23):20780-20798. doi: 10.1021/acs.jmedchem.4c02350. Epub 2024 Nov 22. J Med Chem. 2024. PMID: 39574318
Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors.
Velcicky J, Bauer MR, Schlapbach A, Lapointe G, Meyer A, Vögtle M, Blum E, Ngo E, Rolando C, Nimsgern P, Teixeira-Fouchard S, Lehmann H, Furet P, Berst F, Schümann J, Stringer R, Larger P, Schmid C, Prendergast CT, Riek S, Schmutz P, Lehmann S, Berghausen J, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: gommermann n. J Med Chem. 2024 Sep 26;67(18):16692-16711. doi: 10.1021/acs.jmedchem.4c01520. Epub 2024 Sep 14. J Med Chem. 2024. PMID: 39276085
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: gommermann n. 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
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: gommermann n. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
Structural basis of species-selective antagonist binding to the succinate receptor.
Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP. Haffke M, et al. Among authors: gommermann n. Nature. 2019 Oct;574(7779):581-585. doi: 10.1038/s41586-019-1663-8. Epub 2019 Oct 23. Nature. 2019. PMID: 31645725
GPR91 senses extracellular succinate released from inflammatory macrophages and exacerbates rheumatoid arthritis.
Littlewood-Evans A, Sarret S, Apfel V, Loesle P, Dawson J, Zhang J, Muller A, Tigani B, Kneuer R, Patel S, Valeaux S, Gommermann N, Rubic-Schneider T, Junt T, Carballido JM. Littlewood-Evans A, et al. Among authors: gommermann n. J Exp Med. 2016 Aug 22;213(9):1655-62. doi: 10.1084/jem.20160061. Epub 2016 Aug 1. J Exp Med. 2016. PMID: 27481132 Free PMC article.
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Gommermann N, Buehlmayer P, von Matt A, Breitenstein W, Masuya K, Pirard B, Furet P, Cowan-Jacob SW, Weckbecker G. Gommermann N, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3628-31. doi: 10.1016/j.bmcl.2010.04.112. Epub 2010 Apr 29. Bioorg Med Chem Lett. 2010. PMID: 20483608
15 results