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Page 1
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW. Harris PA, et al. Among authors: eidam pm. J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2. J Med Chem. 2019. PMID: 31013427
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.
Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L. Charnley AK, et al. Among authors: eidam pm. Bioorg Med Chem. 2015 Nov 1;23(21):7000-6. doi: 10.1016/j.bmc.2015.09.038. Epub 2015 Sep 25. Bioorg Med Chem. 2015. PMID: 26455654
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J. Harris PA, et al. Among authors: eidam pm. J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28151659
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU, Kang J, Kasparcova V, Leister LK, Mahajan MK, Miller G, Nagilla R, Ouellette MT, Reilly MA, Rendina AR, Rivera EJ, Sun HH, Thorpe JH, Totoritis RD, Wang W, Wu D, Zhang D, Bertin J, Marquis RW. Harris PA, et al. Among authors: eidam pm. ACS Med Chem Lett. 2019 May 9;10(6):857-862. doi: 10.1021/acsmedchemlett.9b00108. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223438 Free PMC article.
Identification of selective small molecule inhibitors of the nucleotide-binding oligomerization domain 1 (NOD1) signaling pathway.
Rickard DJ, Sehon CA, Kasparcova V, Kallal LA, Haile PA, Zeng X, Montoute MN, Poore DD, Li H, Wu Z, Eidam PM, Emery JG, Marquis RW, Gough PJ, Bertin J. Rickard DJ, et al. Among authors: eidam pm. PLoS One. 2014 May 7;9(5):e96737. doi: 10.1371/journal.pone.0096737. eCollection 2014. PLoS One. 2014. PMID: 24806487 Free PMC article.
Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway.
Rickard DJ, Sehon CA, Kasparcova V, Kallal LA, Zeng X, Montoute MN, Chordia T, Poore DD, Li H, Wu Z, Eidam PM, Haile PA, Yu J, Emery JG, Marquis RW, Gough PJ, Bertin J. Rickard DJ, et al. Among authors: eidam pm. PLoS One. 2013 Aug 1;8(8):e69619. doi: 10.1371/journal.pone.0069619. Print 2013. PLoS One. 2013. PMID: 23936340 Free PMC article.
Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.
Morales-Ramos ÁI, Li YH, Hilfiker M, Mecom JS, Eidam P, Shi D, Tseng PS, Brooks C, Zhang D, Wang N, Jaworski JP, Morrow D, Fries H, Edwards R, Jin J. Morales-Ramos ÁI, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2806-11. doi: 10.1016/j.bmcl.2011.03.107. Epub 2011 Apr 5. Bioorg Med Chem Lett. 2011. PMID: 21514150
Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.
Jin J, Morales-Ramos A, Eidam P, Mecom J, Li Y, Brooks C, Hilfiker M, Zhang D, Wang N, Shi D, Tseng PS, Wheless K, Budzik B, Evans K, Jaworski JP, Jugus J, Leon L, Wu C, Pullen M, Karamshi B, Rao P, Ward E, Laping N, Evans C, Leach C, Holt D, Su X, Morrow D, Fries H, Thorneloe K, Edwards R. Jin J, et al. ACS Med Chem Lett. 2010 May 14;1(7):316-20. doi: 10.1021/ml100077x. eCollection 2010 Oct 14. ACS Med Chem Lett. 2010. PMID: 24900213 Free PMC article.
A formal synthesis of the callipeltoside aglycone.
Marshall JA, Eidam PM. Marshall JA, et al. Among authors: eidam pm. Org Lett. 2008 Jan 3;10(1):93-6. doi: 10.1021/ol702024b. Epub 2007 Dec 5. Org Lett. 2008. PMID: 18052287
13 results