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Page 1
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: marcoux d. 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.
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: marcoux d. 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
Identification of potent tricyclic prodrug S1P1 receptor modulators.
Marcoux D, Xiao HY, Murali Dhar TG, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Shi H, Levesque PC, Sun H, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Gupta A, Pragalathan B, Rampulla R, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Lombardo LJ, Carter PH, Dyckman AJ. Marcoux D, et al. Among authors: d arienzo cj. Medchemcomm. 2016 Nov 25;8(4):725-729. doi: 10.1039/c6md00539j. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108791 Free PMC article.
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Cherney RJ, Cornelius LAM, Srivastava A, Weigelt CA, Marcoux D, Duan JJ, Shi Q, Batt DG, Liu Q, Yip S, Wu DR, Ruzanov M, Sack J, Khan J, Wang J, Yarde M, Cvijic ME, Mathur A, Li S, Shuster D, Khandelwal P, Borowski V, Xie J, Obermeier M, Fura A, Stefanski K, Cornelius G, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Cherney RJ, et al. Among authors: marcoux d. ACS Med Chem Lett. 2020 Mar 31;11(6):1221-1227. doi: 10.1021/acsmedchemlett.0c00063. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551004 Free PMC article.
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA. Liu Q, et al. Among authors: marcoux d. J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5. J Med Chem. 2017. PMID: 28541707
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Marcoux D, Duan JJ, Shi Q, Cherney RJ, Srivastava AS, Cornelius L, Batt DG, Liu Q, Beaudoin-Bertrand M, Weigelt CA, Khandelwal P, Vishwakrishnan S, Selvakumar K, Karmakar A, Gupta AK, Basha M, Ramlingam S, Manjunath N, Vanteru S, Karmakar S, Maddala N, Vetrichelvan M, Gupta A, Rampulla RA, Mathur A, Yip S, Li P, Wu DR, Khan J, Ruzanov M, Sack JS, Wang J, Yarde M, Cvijic ME, Li S, Shuster DJ, Borowski V, Xie JH, McIntyre KW, Obermeier MT, Fura A, Stefanski K, Cornelius G, Hynes J Jr, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Marcoux D, et al. J Med Chem. 2019 Nov 14;62(21):9931-9946. doi: 10.1021/acs.jmedchem.9b01369. Epub 2019 Oct 31. J Med Chem. 2019. PMID: 31638797
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Yang MG, Beaudoin-Bertrand M, Xiao Z, Marcoux D, Weigelt CA, Yip S, Wu DR, Ruzanov M, Sack JS, Wang J, Yarde M, Li S, Shuster DJ, Xie JH, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Khandelwal P, Karmakar A, Basha M, Babu V, Gupta AK, Mathur A, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Yang MG, et al. Among authors: marcoux d. J Med Chem. 2021 Mar 11;64(5):2714-2724. doi: 10.1021/acs.jmedchem.0c01992. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591748
Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (RORγ/RORc) inverse agonists.
Marcoux D, Bertrand MB, Weigelt CA, Yip S, Galella M, Park H, Wu DR, Wang J, Yarde M, Cvijic ME, Li S, Hynes J Jr, Tino JA, Zhao Q, Dhar TGM. Marcoux D, et al. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127466. doi: 10.1016/j.bmcl.2020.127466. Epub 2020 Aug 5. Bioorg Med Chem Lett. 2020. PMID: 32763309
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Shi Q, Xiao Z, Yang MG, Marcoux D, Cherney RJ, Yip S, Li P, Wu DR, Weigelt CA, Sack J, Khan J, Ruzanov M, Wang J, Yarde M, Ellen Cvijic M, Li S, Shuster DJ, Xie J, Sherry T, Obermeier M, Fura A, Stefanski K, Cornelius G, Chacko S, Shu YZ, Khandelwal P, Hynes J Jr, Tino JA, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Shi Q, et al. Among authors: marcoux d. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127521. doi: 10.1016/j.bmcl.2020.127521. Epub 2020 Aug 31. Bioorg Med Chem Lett. 2020. PMID: 32882417
114 results