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Page 1
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.
Nair S, Kumar SR, Paidi VR, Sistla R, Kantheti D, Polimera SR, Thangavel S, Mukherjee AJ, Das M, Bhide RS, Pitts WJ, Murugesan N, Dudhgoankar S, Nagar J, Subramani S, Mazumder D, Carman JA, Holloway DA, Li X, Fereshteh MP, Ruepp S, Palanisamy K, Mariappan TT, Maddi S, Saxena A, Elzinga P, Chimalakonda A, Ruan Q, Ghosh K, Bose S, Sack J, Yan C, Kiefer SE, Xie D, Newitt JA, Saravanakumar SP, Rampulla RA, Barrish JC, Carter PH, Hynes J Jr. Nair S, et al. Among authors: ruepp s. ACS Med Chem Lett. 2020 Jun 10;11(7):1402-1409. doi: 10.1021/acsmedchemlett.0c00082. eCollection 2020 Jul 9. ACS Med Chem Lett. 2020. PMID: 32676146 Free PMC article.
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.
Bhide RS, Neels J, Qin LY, Ruan Z, Stachura S, Weigelt C, Sack JS, Stefanski K, Gu X, Xie JH, Goldstine CB, Skala S, Pedicord DL, Ruepp S, Dhar TG, Carter PH, Salter-Cid LM, Poss MA, Davies P. Bhide RS, et al. Among authors: ruepp s. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4256-60. doi: 10.1016/j.bmcl.2016.07.047. Epub 2016 Jul 21. Bioorg Med Chem Lett. 2016. PMID: 27476421
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Qin LY, Ruan Z, Cherney RJ, Dhar TGM, Neels J, Weigelt CA, Sack JS, Srivastava AS, Cornelius LAM, Tino JA, Stefanski K, Gu X, Xie J, Susulic V, Yang X, Yarde-Chinn M, Skala S, Bosnius R, Goldstein C, Davies P, Ruepp S, Salter-Cid L, Bhide RS, Poss MA. Qin LY, et al. Among authors: ruepp s. Bioorg Med Chem Lett. 2017 Feb 15;27(4):855-861. doi: 10.1016/j.bmcl.2017.01.016. Epub 2017 Jan 10. Bioorg Med Chem Lett. 2017. PMID: 28108251
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: ruepp s. 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
Selective IRAK4 Inhibition Attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity.
Dudhgaonkar S, Ranade S, Nagar J, Subramani S, Prasad DS, Karunanithi P, Srivastava R, Venkatesh K, Selvam S, Krishnamurthy P, Mariappan TT, Saxena A, Fan L, Stetsko DK, Holloway DA, Li X, Zhu J, Yang WP, Ruepp S, Nair S, Santella J, Duncia J, Hynes J, McIntyre KW, Carman JA. Dudhgaonkar S, et al. Among authors: ruepp s. J Immunol. 2017 Feb 1;198(3):1308-1319. doi: 10.4049/jimmunol.1600583. Epub 2016 Dec 21. J Immunol. 2017. PMID: 28003376 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: ruepp s. 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 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: ruepp s. 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.
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV. Wan H, et al. Among authors: ruepp s. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288683 Free PMC article.
Assessing the risk of drug crystallization in vivo.
Ruepp S, Janovitz E, Brodie T, White R, Santella J, Hynes J, Carman J, Pan D, Wu Y, Hanumegowda U, Gemzik B, Megill J, DiPiero J, Drexler D, Su CC, Hageman M. Ruepp S, et al. J Pharmacol Toxicol Methods. 2019 Mar-Apr;96:1-8. doi: 10.1016/j.vascn.2018.12.003. Epub 2018 Dec 13. J Pharmacol Toxicol Methods. 2019. PMID: 30553974
Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.
Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV. Purandare AV, et al. Among authors: ruepp su. Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21. Leukemia. 2012. PMID: 22015772
24 results