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Page 1
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Xiao Z, Yang MG, Liu C, Sherwood T, Gilmore JL, Lin J, Li P, Wu DR, Tokarski J, Li S, Cheng L, Xie C, Fan J, Dierks E, Strnad J, Cvijic ME, Khan J, Ruzanov M, Galella M, Khandelwal P, Dyckman AJ, Mathur A, Lombardo LJ, Macor JE, Carter PH, Aranibar N, Burke JR, Weinstein DS. Xiao Z, et al. Among authors: dyckman aj. Bioorg Med Chem Lett. 2023 Jul 15;91:129373. doi: 10.1016/j.bmcl.2023.129373. Epub 2023 Jun 12. Bioorg Med Chem Lett. 2023. PMID: 37315697
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).
Sreekantha RK, Mussari CP, Dodd DS, Pasunoori L, Hegde S, Posy SL, Critton D, Ruepp S, Subramanian M, Salter-Cid LM, Tagore DM, Sarodaya S, Dudhgaonkar S, Poss MA, Schieven GL, Carter PH, Macor JE, Dyckman AJ. Sreekantha RK, et al. Among authors: dyckman aj. ACS Med Chem Lett. 2022 Apr 25;13(5):812-818. doi: 10.1021/acsmedchemlett.2c00049. eCollection 2022 May 12. ACS Med Chem Lett. 2022. PMID: 35586440 Free PMC article.
Bicyclic Ligand-Biased Agonists of S1P1: Exploring Side Chain Modifications to Modulate the PK, PD, and Safety Profiles.
Gilmore JL, Xiao HY, Dhar TGM, Yang M, Xiao Z, Yang X, Taylor TL, McIntyre KW, Warrack BM, Shi H, Levesque PC, Marino AM, Cornelius G, Mathur A, Shen DR, Pang J, Cvijic ME, Lehman-McKeeman LD, Sun H, Xie J, Salter-Cid L, Carter PH, Dyckman AJ. Gilmore JL, et al. Among authors: dyckman aj. J Med Chem. 2021 Feb 11;64(3):1454-1480. doi: 10.1021/acs.jmedchem.0c01109. Epub 2021 Jan 25. J Med Chem. 2021. PMID: 33492963
Aryl Ether-Derived Sphingosine-1-Phosphate Receptor (S1P1) Modulators: Optimization of the PK, PD, and Safety Profiles.
Xiao Z, Yang MG, Dhar TGM, Xiao HY, Gilmore JL, Marcoux D, McIntyre KW, Taylor TL, Shi H, Levesque PC, Marino AM, Cornelius G, Mathur A, Shen DR, Cvijic ME, Lehman-McKeeman LD, Sun H, Xie JH, Carter PH, Dyckman AJ. Xiao Z, et al. Among authors: dyckman aj. ACS Med Chem Lett. 2020 Aug 11;11(9):1766-1772. doi: 10.1021/acsmedchemlett.0c00333. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32944145 Free PMC article.
Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9).
Mussari CP, Dodd DS, Sreekantha RK, Pasunoori L, Wan H, Posy SL, Critton D, Ruepp S, Subramanian M, Watson A, Davies P, Schieven GL, Salter-Cid LM, Srivastava R, Tagore DM, Dudhgaonkar S, Poss MA, Carter PH, Dyckman AJ. Mussari CP, et al. Among authors: dyckman aj. ACS Med Chem Lett. 2020 Jul 29;11(9):1751-1758. doi: 10.1021/acsmedchemlett.0c00264. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32944143 Free PMC article.
Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials.
Gilmore JL, Xiao HY, Dhar TGM, Yang MG, Xiao Z, Xie J, Lehman-McKeeman LD, Gong L, Sun H, Lecureux L, Chen C, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Borowski V, Warrack BM, Li Y, Shi H, Levesque PC, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Rampulla R, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Salter-Cid LM, Carter PH, Dyckman AJ. Gilmore JL, et al. Among authors: dyckman aj. J Med Chem. 2019 Mar 14;62(5):2265-2285. doi: 10.1021/acs.jmedchem.8b01695. Epub 2019 Mar 6. J Med Chem. 2019. PMID: 30785748
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.
Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ. Yang MG, et al. Among authors: dyckman aj. J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7. J Med Chem. 2016. PMID: 28002964
28 results