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Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
Horan JC, Kuzmich D, Liu P, DiSalvo D, Lord J, Mao C, Hopkins TD, Yu H, Harcken C, Betageri R, Hill-Drzewi M, Patenaude L, Patel M, Fletcher K, Terenzzio D, Linehan B, Xia H, Patel M, Studwell D, Miller C, Hickey E, Levin JI, Smith D, Kemper RA, Modis LK, Bannen LC, Chan DS, Mac MB, Ng S, Wang Y, Xu W, Lemieux RM. Horan JC, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):466-471. doi: 10.1016/j.bmcl.2015.11.090. Epub 2015 Nov 26. Bioorg Med Chem Lett. 2016. PMID: 26687487
Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357.
Harcken C, Csengery J, Turner M, Wu L, Liang S, Sibley R, Brunette S, Labadia M, Hoyt K, Wayne A, Wieckowski T, Davis G, Panzenbeck M, Souza D, Kugler S, Terenzio D, Collin D, Smith D, Fryer RM, Tseng YC, Hehn JP, Fletcher K, Hughes RO. Harcken C, et al. ACS Med Chem Lett. 2021 Jan 5;12(1):143-154. doi: 10.1021/acsmedchemlett.0c00575. eCollection 2021 Jan 14. ACS Med Chem Lett. 2021. PMID: 33488976 Free PMC article.
Identification of novel azaindazole CCR1 antagonist clinical candidates.
Harcken C, Kuzmich D, Cook B, Mao C, Disalvo D, Razavi H, Swinamer A, Liu P, Zhang Q, Kukulka A, Skow D, Patel M, Patel M, Fletcher K, Sherry T, Joseph D, Smith D, Canfield M, Souza D, Bogdanffy M, Berg K, Brown M. Harcken C, et al. Bioorg Med Chem Lett. 2019 Feb 1;29(3):441-448. doi: 10.1016/j.bmcl.2018.12.024. Epub 2018 Dec 13. Bioorg Med Chem Lett. 2019. PMID: 30595446
An RORγt Oral Inhibitor Modulates IL-17 Responses in Peripheral Blood and Intestinal Mucosa of Crohn's Disease Patients.
Bassolas-Molina H, Raymond E, Labadia M, Wahle J, Ferrer-Picón E, Panzenbeck M, Zheng J, Harcken C, Hughes R, Turner M, Smith D, Calderón-Gómez E, Esteller M, Carrasco A, Esteve M, Dotti I, Corraliza AM, Masamunt MC, Arajol C, Guardiola J, Ricart E, Nabozny G, Salas A. Bassolas-Molina H, et al. Front Immunol. 2018 Oct 22;9:2307. doi: 10.3389/fimmu.2018.02307. eCollection 2018. Front Immunol. 2018. PMID: 30405600 Free PMC article.
1,797 results