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Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrrolidin-1-yl)-ethoxy]-phenyl}-amine).
Hu SX, Soll R, Yee S, Lohse DL, Kousba A, Zeng B, Yu X, McPherson A, Renick J, Cao J, Tabak A, Hood J, Doukas J, Noronha G, Martin M. Hu SX, et al. Among authors: martin m. Drug Metab Dispos. 2007 Jun;35(6):929-36. doi: 10.1124/dmd.106.014290. Epub 2007 Mar 19. Drug Metab Dispos. 2007. PMID: 17371799
Cyclic conversion of the novel Src kinase inhibitor [7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine (TG100435) and Its N-oxide metabolite by flavin-containing monoxygenases and cytochrome P450 reductase.
Kousba A, Soll R, Yee S, Martin M. Kousba A, et al. Among authors: martin m. Drug Metab Dispos. 2007 Dec;35(12):2242-51. doi: 10.1124/dmd.107.017384. Epub 2007 Sep 19. Drug Metab Dispos. 2007. PMID: 17881660
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration.
Palanki MS, Akiyama H, Campochiaro P, Cao J, Chow CP, Dellamary L, Doukas J, Fine R, Gritzen C, Hood JD, Hu S, Kachi S, Kang X, Klebansky B, Kousba A, Lohse D, Mak CC, Martin M, McPherson A, Pathak VP, Renick J, Soll R, Umeda N, Yee S, Yokoi K, Zeng B, Zhu H, Noronha G. Palanki MS, et al. Among authors: martin m. J Med Chem. 2008 Mar 27;51(6):1546-59. doi: 10.1021/jm7011276. Epub 2008 Feb 27. J Med Chem. 2008. PMID: 18311895
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.
Palanki MS, Dneprovskaia E, Doukas J, Fine RM, Hood J, Kang X, Lohse D, Martin M, Noronha G, Soll RM, Wrasidlo W, Yee S, Zhu H. Palanki MS, et al. Among authors: martin m. J Med Chem. 2007 Sep 6;50(18):4279-94. doi: 10.1021/jm051056c. Epub 2007 Aug 9. J Med Chem. 2007. PMID: 17685602
Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease.
Doukas J, Eide L, Stebbins K, Racanelli-Layton A, Dellamary L, Martin M, Dneprovskaia E, Noronha G, Soll R, Wrasidlo W, Acevedo LM, Cheresh DA. Doukas J, et al. Among authors: martin m. J Pharmacol Exp Ther. 2009 Mar;328(3):758-65. doi: 10.1124/jpet.108.144311. Epub 2008 Dec 4. J Pharmacol Exp Ther. 2009. PMID: 19056934
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.
Wernig G, Kharas MG, Okabe R, Moore SA, Leeman DS, Cullen DE, Gozo M, McDowell EP, Levine RL, Doukas J, Mak CC, Noronha G, Martin M, Ko YD, Lee BH, Soll RM, Tefferi A, Hood JD, Gilliland DG. Wernig G, et al. Among authors: martin m. Cancer Cell. 2008 Apr;13(4):311-20. doi: 10.1016/j.ccr.2008.02.009. Cancer Cell. 2008. PMID: 18394554 Free article.
Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization.
Thomsen WJ, Grottick AJ, Menzaghi F, Reyes-Saldana H, Espitia S, Yuskin D, Whelan K, Martin M, Morgan M, Chen W, Al-Shamma H, Smith B, Chalmers D, Behan D. Thomsen WJ, et al. Among authors: martin m. J Pharmacol Exp Ther. 2008 May;325(2):577-87. doi: 10.1124/jpet.107.133348. Epub 2008 Feb 5. J Pharmacol Exp Ther. 2008. PMID: 18252809
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