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Page 1
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA. Shi J, et al. Among authors: rampulla ra. J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27. J Med Chem. 2018. PMID: 29316397
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G. Salvati ME, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1910-5. doi: 10.1016/j.bmcl.2008.02.006. Epub 2008 Feb 8. Bioorg Med Chem Lett. 2008. PMID: 18291644
BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.
Shan W, Balog A, Quesnelle C, Gill P, Han WC, Norris D, Mandal S, Thiruvenkadam R, Gona KB, Thiyagarajan K, Kandula S, McGlinchey K, Menard K, Wen ML, Rose A, White R, Guarino V, Shen DR, Cvijic ME, Ranasinghe A, Dai J, Zhang Y, Wu DR, Mathur A, Rampulla R, Trainor G, Hunt JT, Vite GD, Westhouse R, Lee FY, Gavai AV. Shan W, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1905-9. doi: 10.1016/j.bmcl.2015.03.038. Epub 2015 Mar 23. Bioorg Med Chem Lett. 2015. PMID: 25857941
Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors.
Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY. Gavai AV, et al. Among authors: rampulla r. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7. doi: 10.1021/acsmedchemlett.5b00001. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005526 Free PMC article.
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Balog A, Rampulla R, Martin GS, Krystek SR, Attar R, Dell-John J, DiMarco JD, Fairfax D, Gougoutas J, Holst CL, Nation A, Rizzo C, Rossiter LM, Schweizer L, Shan W, Spergel S, Spires T, Cornelius G, Gottardis M, Trainor G, Vite GD, Salvati ME. Balog A, et al. ACS Med Chem Lett. 2015 Jun 19;6(8):908-12. doi: 10.1021/acsmedchemlett.5b00173. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288692 Free PMC article.
Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).
Qiao JX, Wang TC, Adam LP, Chen AY, Taylor DS, Yang RZ, Zhuang S, Sleph PG, Li JP, Li D, Yin X, Chang M, Chen XQ, Shen H, Li J, Smith D, Wu DR, Leith L, Harikrishnan LS, Kamau MG, Miller MM, Bilder D, Rampulla R, Li YX, Xu C, Lawrence RM, Poss MA, Levesque P, Gordon DA, Huang CS, Finlay HJ, Wexler RR, Salvati ME. Qiao JX, et al. J Med Chem. 2015 Nov 25;58(22):9010-26. doi: 10.1021/acs.jmedchem.5b01363. Epub 2015 Nov 17. J Med Chem. 2015. PMID: 26524347
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA. De Lucca GV, et al. J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27531604
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.
Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM. Sun LQ, et al. J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27564532
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. J Med Chem. 2016 Oct 13;59(19):9173-9200. doi: 10.1021/acs.jmedchem.6b01088. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27583770
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA. Jurica EA, et al. Among authors: rampulla ra. J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9. J Med Chem. 2017. PMID: 28112924
38 results