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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: llinas a. 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
Discovery of N-(1-adamantyl)-2-(4-alkylpiperazin-1-yl)acetamide derivatives as T-type calcium channel (Cav3.2) inhibitors.
Giordanetto F, Knerr L, Selmi N, Llinàs A, Lindqvist A, Wang QD, Ståhlberg P, Thorstensson F, Ullah V, Nilsson K, O'Mahony G, Högberg G, Lindhardt E, Strand A, Duker G. Giordanetto F, et al. Among authors: llinas a. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5557-61. doi: 10.1016/j.bmcl.2011.06.092. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782423
Oxadiazoles in medicinal chemistry.
Boström J, Hogner A, Llinàs A, Wellner E, Plowright AT. Boström J, et al. Among authors: llinas a. J Med Chem. 2012 Mar 8;55(5):1817-30. doi: 10.1021/jm2013248. Epub 2012 Jan 13. J Med Chem. 2012. PMID: 22185670
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor.
Giordanetto F, Wållberg A, Knerr L, Selmi N, Ullah V, Thorstensson F, Lindelöf Å, Karlsson S, Nikitidis G, Llinas A, Wang QD, Lindqvist A, Högberg G, Lindhardt E, Åstrand A, Duker G. Giordanetto F, et al. Among authors: llinas a. Bioorg Med Chem Lett. 2013 Jan 1;23(1):119-24. doi: 10.1016/j.bmcl.2012.10.140. Epub 2012 Nov 12. Bioorg Med Chem Lett. 2013. PMID: 23200256
Discovery of AZD6642, an inhibitor of 5-lipoxygenase activating protein (FLAP) for the treatment of inflammatory diseases.
Lemurell M, Ulander J, Winiwarter S, Dahlén A, Davidsson Ö, Emtenäs H, Broddefalk J, Swanson M, Hovdal D, Plowright AT, Pettersen A, Rydén-Landergren M, Barlind J, Llinas A, Herslöf M, Drmota T, Sigfridsson K, Moses S, Whatling C. Lemurell M, et al. Among authors: llinas a. J Med Chem. 2015 Jan 22;58(2):897-911. doi: 10.1021/jm501531v. Epub 2014 Dec 22. J Med Chem. 2015. PMID: 25478788
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.
Gardelli C, Wada H, Ray A, Caffrey M, Llinas A, Shamovsky I, Tholander J, Larsson J, Sivars U, Hultin L, Andersson U, Sanganee HJ, Stenvall K, Leidvik B, Gedda K, Jinton L, Rydén Landergren M, Karabelas K. Gardelli C, et al. Among authors: llinas a. J Med Chem. 2018 Jul 26;61(14):5974-5987. doi: 10.1021/acs.jmedchem.8b00322. Epub 2018 Jul 6. J Med Chem. 2018. PMID: 29909635
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: llinas a. 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.
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Cooper M, Llinas A, Hansen P, Caffrey M, Ray A, Sjödin S, Shamovsky I, Wada H, Jellesmark Jensen T, Sivars U, Hultin L, Andersson U, Lundqvist S, Gedda K, Jinton L, Krutrök N, Lewis R, Jansson P, Gardelli C. Cooper M, et al. Among authors: llinas a. J Med Chem. 2020 Sep 10;63(17):9705-9730. doi: 10.1021/acs.jmedchem.0c00828. Epub 2020 Aug 27. J Med Chem. 2020. PMID: 32787075
AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Narjes F, Llinas A, von Berg S, Jirholt J, Lever S, Pehrson R, Collins M, Malmberg A, Svanberg P, Xue Y, Olsson RI, Malmberg J, Hughes G, Hossain N, Grindebacke H, Leffler A, Krutrök N, Bäck E, Ramnegård M, Lepistö M, Thunberg L, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG. Narjes F, et al. Among authors: llinas a. J Med Chem. 2021 Sep 23;64(18):13807-13829. doi: 10.1021/acs.jmedchem.1c01197. Epub 2021 Aug 31. J Med Chem. 2021. PMID: 34464130
89 results