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Page 1
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS. Wrobleski ST, et al. Among authors: ruzanov m. J Med Chem. 2019 Oct 24;62(20):8973-8995. doi: 10.1021/acs.jmedchem.9b00444. Epub 2019 Jul 18. J Med Chem. 2019. PMID: 31318208
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.
Duan JJ, Lu Z, Jiang B, Stachura S, Weigelt CA, Sack JS, Khan J, Ruzanov M, Galella MA, Wu DR, Yarde M, Shen DR, Shuster DJ, Borowski V, Xie JH, Zhang L, Vanteru S, Gupta AK, Mathur A, Zhao Q, Foster W, Salter-Cid LM, Carter PH, Dhar TGM. Duan JJ, et al. Among authors: ruzanov m. ACS Med Chem Lett. 2019 Feb 26;10(3):367-373. doi: 10.1021/acsmedchemlett.9b00010. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891142 Free PMC article.
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.
Lu Z, Duan JJ, Xiao H, Neels J, Wu DR, Weigelt CA, Sack JS, Khan J, Ruzanov M, An Y, Yarde M, Karmakar A, Vishwakrishnan S, Baratam V, Shankarappa H, Vanteru S, Babu V, Basha M, Kumar Gupta A, Kumaravel S, Mathur A, Zhao Q, Salter-Cid LM, Carter PH, Murali Dhar TG. Lu Z, et al. Among authors: ruzanov m. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2265-2269. doi: 10.1016/j.bmcl.2019.06.036. Epub 2019 Jun 20. Bioorg Med Chem Lett. 2019. PMID: 31257087
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. Among authors: ruzanov m. 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
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.
Harikrishnan LS, Gill P, Kamau MG, Qin LY, Ruan Z, O'Malley D, Huynh T, Stachura S, Cavallaro CL, Lu Z, J-W Duan J, Weigelt CA, Sack JS, Ruzanov M, Khan J, Gururajan M, Wong JJ, Huang Y, Yarde M, Li Z, Chen C, Sun H, Borowski V, Murtaza A, Fink BE. Harikrishnan LS, et al. Among authors: ruzanov m. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127204. doi: 10.1016/j.bmcl.2020.127204. Epub 2020 Apr 20. Bioorg Med Chem Lett. 2020. PMID: 32334911
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: ruzanov m. 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.
Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists.
Duan JJ, Jiang B, Lu Z, Stachura S, Weigelt CA, Sack JS, Khan J, Ruzanov M, Wu DR, Yarde M, Shen DR, Zhao Q, Salter-Cid LM, Carter PH, Murali Dhar TG. Duan JJ, et al. Among authors: ruzanov m. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127441. doi: 10.1016/j.bmcl.2020.127441. Epub 2020 Jul 29. Bioorg Med Chem Lett. 2020. PMID: 32736080
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: ruzanov m. 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
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Liu C, Lin J, Langevine C, Smith D, Li J, Tokarski JS, Khan J, Ruzanov M, Strnad J, Zupa-Fernandez A, Cheng L, Gillooly KM, Shuster D, Zhang Y, Thankappan A, McIntyre KW, Chaudhry C, Elzinga PA, Chiney M, Chimalakonda A, Lombardo LJ, Macor JE, Carter PH, Burke JR, Weinstein DS. Liu C, et al. Among authors: ruzanov m. J Med Chem. 2021 Jan 14;64(1):677-694. doi: 10.1021/acs.jmedchem.0c01698. Epub 2020 Dec 28. J Med Chem. 2021. PMID: 33370104
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists.
Ruan Z, Park PK, Wei D, Purandare A, Wan H, O'Malley D, Stachura S, Perez H, Cavallaro CL, Weigelt CA, Sack JS, Ruzanov M, Khan J, Gururajan M, Wong JJ, Huang Y, Yarde M, Li Z, Chen C, Sun H, Borowski V, Xie JH, Anthony M, Agler M, Fink BE, Harikrishnan LS. Ruan Z, et al. Among authors: ruzanov m. Bioorg Med Chem Lett. 2021 Mar 1;35:127778. doi: 10.1016/j.bmcl.2021.127778. Epub 2021 Jan 8. Bioorg Med Chem Lett. 2021. PMID: 33422603
25 results