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Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.
Narjes F, Xue Y, von Berg S, Malmberg J, Llinas A, Olsson RI, Jirholt J, Grindebacke H, Leffler A, Hossain N, Lepistö M, Thunberg L, Leek H, Aagaard A, McPheat J, Hansson EL, Bäck E, Tångefjord S, Chen R, Xiong Y, Hongbin G, Hansson TG. Narjes F, et al. Among authors: lepisto m. J Med Chem. 2018 Sep 13;61(17):7796-7813. doi: 10.1021/acs.jmedchem.8b00783. Epub 2018 Aug 27. J Med Chem. 2018. PMID: 30095900
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.
Evenäs J, Edfeldt F, Lepistö M, Svitacheva N, Synnergren A, Lundquist B, Gränse M, Rönnholm A, Varga M, Wright J, Wei M, Yue S, Wang J, Li C, Li X, Chen G, Liao Y, Lv G, Tjörnebo A, Narjes F. Evenäs J, et al. Among authors: lepisto m. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1315-21. doi: 10.1016/j.bmcl.2014.01.050. Epub 2014 Jan 28. Bioorg Med Chem Lett. 2014. PMID: 24508129
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Edman K, Ahlgren R, Bengtsson M, Bladh H, Bäckström S, Dahmén J, Henriksson K, Hillertz P, Hulikal V, Jerre A, Kinchin L, Kåse C, Lepistö M, Mile I, Nilsson S, Smailagic A, Taylor J, Tjörnebo A, Wissler L, Hansson T. Edman K, et al. Among authors: lepisto m. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2571-7. doi: 10.1016/j.bmcl.2014.03.070. Epub 2014 Apr 2. Bioorg Med Chem Lett. 2014. PMID: 24755427
Saccharin Aza Bioisosteres-Synthesis and Preclinical Property Comparisons.
Chen Y, Aurell CJ, Pettersen A, Lewis RJ, Hayes MA, Lepistö M, Jonson AC, Leek H, Thunberg L. Chen Y, et al. Among authors: lepisto m. ACS Med Chem Lett. 2017 May 1;8(6):672-677. doi: 10.1021/acsmedchemlett.7b00137. eCollection 2017 Jun 8. ACS Med Chem Lett. 2017. PMID: 28626531 Free PMC article.
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Hemmerling M, Nilsson S, Edman K, Eirefelt S, Russell W, Hendrickx R, Johnsson E, Kärrman Mårdh C, Berger M, Rehwinkel H, Abrahamsson A, Dahmén J, Eriksson AR, Gabos B, Henriksson K, Hossain N, Ivanova S, Jansson AH, Jensen TJ, Jerre A, Johansson H, Klingstedt T, Lepistö M, Lindsjö M, Mile I, Nikitidis G, Steele J, Tehler U, Wissler L, Hansson T. Hemmerling M, et al. Among authors: lepisto m. J Med Chem. 2017 Oct 26;60(20):8591-8605. doi: 10.1021/acs.jmedchem.7b01215. Epub 2017 Oct 12. J Med Chem. 2017. PMID: 28937774
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Ripa L, Edman K, Dearman M, Edenro G, Hendrickx R, Ullah V, Chang HF, Lepistö M, Chapman D, Geschwindner S, Wissler L, Svanberg P, Lawitz K, Malmberg J, Nikitidis A, Olsson RI, Bird J, Llinas A, Hegelund-Myrbäck T, Berger M, Thorne P, Harrison R, Köhler C, Drmota T. Ripa L, et al. Among authors: lepisto m. J Med Chem. 2018 Mar 8;61(5):1785-1799. doi: 10.1021/acs.jmedchem.7b01690. Epub 2018 Feb 16. J Med Chem. 2018. PMID: 29424542
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.
von Berg S, Xue Y, Collins M, Llinas A, Olsson RI, Halvarsson T, Lindskog M, Malmberg J, Jirholt J, Krutrök N, Ramnegård M, Brännström M, Lundqvist A, Lepistö M, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG, Narjes F. von Berg S, et al. Among authors: lepisto m. ACS Med Chem Lett. 2019 May 29;10(6):972-977. doi: 10.1021/acsmedchemlett.9b00158. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223457 Free PMC article.
44 results