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Structure-Based and Property-Driven Optimization of N-Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors.
Hoegenauer K, Kallen J, Jiménez-Núñez E, Strang R, Ertl P, Cooke NG, Hintermann S, Voegtle M, Betschart C, McKay DJJ, Wagner J, Ottl J, Beerli C, Billich A, Dawson J, Kaupmann K, Streiff M, Gobeau N, Harlfinger S, Stringer R, Guntermann C. Hoegenauer K, et al. J Med Chem. 2019 Dec 12;62(23):10816-10832. doi: 10.1021/acs.jmedchem.9b01291. Epub 2019 Dec 3. J Med Chem. 2019. PMID: 31729873
Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.
Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S. Carcache DA, et al. Among authors: hoegenauer k. J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24. J Med Chem. 2018. PMID: 29990434
Retinoic-acid-orphan-receptor-C inhibition suppresses Th17 cells and induces thymic aberrations.
Guntermann C, Piaia A, Hamel ML, Theil D, Rubic-Schneider T, Del Rio-Espinola A, Dong L, Billich A, Kaupmann K, Dawson J, Hoegenauer K, Orain D, Hintermann S, Stringer R, Patel DD, Doelemeyer A, Deurinck M, Schümann J. Guntermann C, et al. Among authors: hoegenauer k. JCI Insight. 2017 Mar 9;2(5):e91127. doi: 10.1172/jci.insight.91127. JCI Insight. 2017. PMID: 28289717 Free PMC article.
The 2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry.
Ciulli A, Hamann L, Jahnke W, Kalgutkar AS, Magauer T, Ritter T, Steadman V, Williams SD, Winter G, Hoegenauer K, Krawinkler KH, Stepan AF. Ciulli A, et al. Among authors: hoegenauer k. ChemMedChem. 2021 Aug 5;16(15):2417-2423. doi: 10.1002/cmdc.202100372. Epub 2021 Jun 10. ChemMedChem. 2021. PMID: 34114371
Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.
Argikar U, Blatter M, Bednarczyk D, Chen Z, Cho YS, Doré M, Dumouchel JL, Ho S, Hoegenauer K, Kawanami T, Mathieu S, Meredith E, Möbitz H, Murphy SK, Parthasarathy S, Soldermann CP, Santos J, Silver S, Skolnik S, Stojanovic A. Argikar U, et al. Among authors: hoegenauer k. J Med Chem. 2022 Sep 22;65(18):12386-12402. doi: 10.1021/acs.jmedchem.2c01068. Epub 2022 Sep 7. J Med Chem. 2022. PMID: 36069672
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C. Hoegenauer K, et al. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14. ACS Med Chem Lett. 2017. PMID: 28947947 Free PMC article.
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Stauffer F, Furet P, Graveleau N, Smith AB, Hebach C, Hollingworth GJ, Lewis I, Gutmann S, Rummel G, Knapp M, Wolf RM, Blanz J, Feifel R, Burkhart C, Zécri F. Hoegenauer K, et al. ACS Med Chem Lett. 2016 Jun 2;7(8):762-7. doi: 10.1021/acsmedchemlett.6b00119. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563400 Free PMC article.
23 results