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Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.
Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: tran tp. ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005540 Free PMC article.
Novel γ-secretase modulators: a review of patents from 2008 to 2010.
Pettersson M, Kauffman GW, am Ende CW, Patel NC, Stiff C, Tran TP, Johnson DS. Pettersson M, et al. Among authors: tran tp. Expert Opin Ther Pat. 2011 Feb;21(2):205-26. doi: 10.1517/13543776.2011.547479. Epub 2011 Jan 14. Expert Opin Ther Pat. 2011. PMID: 21231889 Review.
Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators.
Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Lira R, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Vetelino BC, Xie L, Zhang L, Pustilnik LR, Wood KM, O'Donnell CJ. Pettersson M, et al. Among authors: tran tp. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2906-11. doi: 10.1016/j.bmcl.2012.02.059. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22429469
Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione γ-secretase modulators.
Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Xie L, Zhang L, Pustilnik LR, Vetelino BC, Wood KM, Pozdnyakov N, Verhoest PR, O'Donnell CJ. Pettersson M, et al. Among authors: tran tp. J Med Chem. 2014 Feb 13;57(3):1046-62. doi: 10.1021/jm401782h. Epub 2014 Jan 28. J Med Chem. 2014. PMID: 24428186
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.
Stepan AF, Tran TP, Helal CJ, Brown MS, Chang C, O'Connor RE, De Vivo M, Doran SD, Fisher EL, Jenkinson S, Karanian D, Kormos BL, Sharma R, Walker GS, Wright AS, Yang EX, Brodney MA, Wager TT, Verhoest PR, Obach RS. Stepan AF, et al. Among authors: tran tp. ACS Med Chem Lett. 2018 Jan 4;9(2):68-72. doi: 10.1021/acsmedchemlett.7b00343. eCollection 2018 Feb 8. ACS Med Chem Lett. 2018. PMID: 29456790 Free PMC article.
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Butler TW, Dorff PH, Efremov IV, Evrard E, Green ME, Helal CJ, Kauffman GW, Mullins PB, Navaratnam T, O'Donnell CJ, O'Sullivan TJ, Patel NC, Stepan AF, Stiff CM, Subramanyam C, Trapa P, Tran TP, Vetelino BC, Yang E, Xie L, Pustilnik LR, Steyn SJ, Wood KM, Bales KR, Hajos-Korcsok E, Verhoest PR. Pettersson M, et al. Among authors: tran tp. J Med Chem. 2024 Jun 7. doi: 10.1021/acs.jmedchem.4c00580. Online ahead of print. J Med Chem. 2024. PMID: 38848667
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA, Meade MA, Roberts BJ, Fry DW, Gonzales AJ, Harvey PJ, Nelson JM, Sherwood V, Han HK, Pace G, Smaill JB, Denny WA, Showalter HD. Klutchko SR, et al. Among authors: tran tp. J Med Chem. 2006 Feb 23;49(4):1475-85. doi: 10.1021/jm050936o. J Med Chem. 2006. PMID: 16480284
141 results