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Page 1
Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents. Discovery of water-soluble 3,9-difluoro-12,13-dihydro-13-[6-amino-beta-D-glucopyranosyl]-5H,13H-benzo[b]- thienyl[2,3-a]pyrrolo[3,4-c]carbazole- 5,7(6H)-dione (BMS-251873) with curative antitumor activity against prostate carcinoma xenograft tumor model.
Balasubramanian BN, St Laurent DR, Saulnier MG, Long BH, Bachand C, Beaulieu F, Clarke W, Deshpande M, Eummer J, Fairchild CR, Frennesson DB, Kramer R, Lee FY, Mahler M, Martel A, Naidu BN, Rose WC, Russell J, Ruediger E, Solomon C, Stoffan KM, Wong H, Wright JJ, Zimmermann K, Vyas DM. Balasubramanian BN, et al. Among authors: ruediger e. J Med Chem. 2004 Mar 25;47(7):1609-12. doi: 10.1021/jm034197s. J Med Chem. 2004. PMID: 15027851
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
Saulnier MG, Balasubramanian BN, Long BH, Frennesson DB, Ruediger E, Zimmermann K, Eummer JT, St Laurent DR, Stoffan KM, Naidu BN, Mahler M, Beaulieu F, Bachand C, Lee FY, Fairchild CR, Stadnick LK, Rose WC, Solomon C, Wong H, Martel A, Wright JJ, Kramer R, Langley DR, Vyas DM. Saulnier MG, et al. Among authors: ruediger e. J Med Chem. 2005 Apr 7;48(7):2258-61. doi: 10.1021/jm049090z. J Med Chem. 2005. PMID: 15801816
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Dextraze P, Fink BE, Gavai A, Goyal B, Han WC, Johnson W, Langley D, Lee FY, Marathe P, Mathur A, Oppenheimer S, Ruediger E, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Among authors: ruediger e. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2036-42. doi: 10.1016/j.bmcl.2007.01.002. Epub 2007 Jan 12. Bioorg Med Chem Lett. 2007. PMID: 17270437
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.
Beaulieu F, Ouellet C, Ruediger EH, Belema M, Qiu Y, Yang X, Banville J, Burke JR, Gregor KR, MacMaster JF, Martel A, McIntyre KW, Pattoli MA, Zusi FC, Vyas D. Beaulieu F, et al. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1233-7. doi: 10.1016/j.bmcl.2006.12.017. Epub 2006 Dec 9. Bioorg Med Chem Lett. 2007. PMID: 17197177
Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.
Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG. Belema M, et al. Among authors: ruediger eh. J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12. J Med Chem. 2014. PMID: 24521299
beta-alanine dipeptides as MC4R agonists.
Ruel R, Herpin TF, Iben L, Luo G, Martel A, Mason H, Mattson G, Poirier B, Ruediger EH, Shi D, Thibault C, Yu G, Antal Zimanyi I, Poindexter GS, Macor JE. Ruel R, et al. Among authors: ruediger eh. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4341-4. doi: 10.1016/j.bmcl.2003.09.036. Bioorg Med Chem Lett. 2003. PMID: 14643322
Novel quinolizidine salicylamide influenza fusion inhibitors.
Yu KL, Ruediger E, Luo G, Cianci C, Danetz S, Tiley L, Trehan AK, Monkovic I, Pearce B, Martel A, Krystal M, Meanwell NA. Yu KL, et al. Among authors: ruediger e. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2177-80. doi: 10.1016/s0960-894x(99)00361-3. Bioorg Med Chem Lett. 1999. PMID: 10465540
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Miller MM, Banville J, Friends TJ, Gagnon M, Hangeland JJ, Lavallée JF, Martel A, O'Grady H, Rémillard R, Ruediger E, Tremblay F, Posy SL, Allegretto NJ, Guarino VR, Harden DG, Harper TW, Hartl K, Josephs J, Malmstrom S, Watson C, Yang Y, Zhang G, Wong P, Yang J, Bouvier M, Seiffert DA, Wexler RR, Lawrence RM, Priestley ES, Marinier A. Miller MM, et al. Among authors: ruediger e. J Med Chem. 2019 Aug 22;62(16):7400-7416. doi: 10.1021/acs.jmedchem.9b00186. Epub 2019 Aug 5. J Med Chem. 2019. PMID: 31246024
Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Priestley ES, Banville J, Deon D, Dubé L, Gagnon M, Guy J, Lapointe P, Lavallée JF, Martel A, Plamondon S, Rémillard R, Ruediger E, Tremblay F, Posy SL, Guarino VR, Richter JM, Li J, Gupta A, Vetrichelvan M, Balapragalathan TJ, Mathur A, Hua J, Callejo M, Guay J, Sum CS, Cvijic ME, Watson C, Wong P, Yang J, Bouvier M, Gordon DA, Wexler RR, Marinier A. Priestley ES, et al. Among authors: ruediger e. J Med Chem. 2022 Jul 14;65(13):8843-8854. doi: 10.1021/acs.jmedchem.2c00359. Epub 2022 Jun 21. J Med Chem. 2022. PMID: 35729784
23 results