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190 related items for PubMed ID: 17371799

  • 1. 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.
    Drug Metab Dispos; 2007 Jun; 35(6):929-36. PubMed ID: 17371799
    [Abstract] [Full Text] [Related]

  • 2. 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.
    Drug Metab Dispos; 2007 Dec; 35(12):2242-51. PubMed ID: 17881660
    [Abstract] [Full Text] [Related]

  • 3. Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes.
    Kalgutkar AS, Hatch HL, Kosea F, Nguyen HT, Choo EF, McClure KF, Taylor TJ, Henne KR, Kuperman AV, Dombroski MA, Letavic MA.
    Biopharm Drug Dispos; 2006 Nov; 27(8):371-86. PubMed ID: 16944451
    [Abstract] [Full Text] [Related]

  • 4. Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
    Noronha G, Barrett K, Boccia A, Brodhag T, Cao J, Chow CP, Dneprovskaia E, Doukas J, Fine R, Gong X, Gritzen C, Gu H, Hanna E, Hood JD, Hu S, Kang X, Key J, Klebansky B, Kousba A, Li G, Lohse D, Mak CC, McPherson A, Palanki MS, Pathak VP, Renick J, Shi F, Soll R, Splittgerber U, Stoughton S, Tang S, Yee S, Zeng B, Zhao N, Zhu H.
    Bioorg Med Chem Lett; 2007 Feb 01; 17(3):602-8. PubMed ID: 17113292
    [Abstract] [Full Text] [Related]

  • 5. 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.
    J Med Chem; 2008 Mar 27; 51(6):1546-59. PubMed ID: 18311895
    [Abstract] [Full Text] [Related]

  • 6. Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey.
    Johnson BM, Kamath AV, Leet JE, Liu X, Bhide RS, Tejwani RW, Zhang Y, Qian L, Wei DD, Lombardo LJ, Shu YZ.
    Drug Metab Dispos; 2008 Dec 27; 36(12):2475-83. PubMed ID: 18787055
    [Abstract] [Full Text] [Related]

  • 7. Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor.
    Kammerer B, Scheible H, Albrecht W, Gleiter CH, Laufer S.
    Drug Metab Dispos; 2007 Jun 27; 35(6):875-83. PubMed ID: 17344341
    [Abstract] [Full Text] [Related]

  • 8. Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.
    Kamath AV, Wang J, Lee FY, Marathe PH.
    Cancer Chemother Pharmacol; 2008 Mar 27; 61(3):365-76. PubMed ID: 17429625
    [Abstract] [Full Text] [Related]

  • 9. An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.
    Tonn GR, Wong SG, Wong SC, Johnson MG, Ma J, Cho R, Floren LC, Kersey K, Berry K, Marcus AP, Wang X, Van Lengerich B, Medina JC, Pearson PG, Wong BK.
    Drug Metab Dispos; 2009 Mar 27; 37(3):502-13. PubMed ID: 19088267
    [Abstract] [Full Text] [Related]

  • 10. Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.
    Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC.
    Xenobiotica; 2009 Nov 27; 39(11):850-61. PubMed ID: 19845436
    [Abstract] [Full Text] [Related]

  • 11. Impact of hydrolysis-mediated clearance on the pharmacokinetics of novel anaplastic lymphoma kinase inhibitors.
    Teffera Y, Berry LM, Brake RL, Lewis RT, Saffran DC, Moore E, Liu J, Zhao Z.
    Drug Metab Dispos; 2013 Jan 27; 41(1):238-47. PubMed ID: 23118327
    [Abstract] [Full Text] [Related]

  • 12. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs.
    Beconi MG, Reed JR, Teffera Y, Xia YQ, Kochansky CJ, Liu DQ, Xu S, Elmore CS, Ciccotto S, Hora DF, Stearns RA, Vincent SH.
    Drug Metab Dispos; 2007 Apr 27; 35(4):525-32. PubMed ID: 17220241
    [Abstract] [Full Text] [Related]

  • 13. (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
    Ammirati MJ, Andrews KM, Boyer DD, Brodeur AM, Danley DE, Doran SD, Hulin B, Liu S, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soglia CB, Treadway JL, VanVolkenburg MA, Wilder DC, Piotrowski DW.
    Bioorg Med Chem Lett; 2009 Apr 01; 19(7):1991-5. PubMed ID: 19275964
    [Abstract] [Full Text] [Related]

  • 14. Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
    Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG.
    J Med Chem; 2008 Mar 27; 51(6):1637-48. PubMed ID: 18278858
    [Abstract] [Full Text] [Related]

  • 15. Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human.
    Sharma R, Sun H, Piotrowski DW, Ryder TF, Doran SD, Dai H, Prakash C.
    Drug Metab Dispos; 2012 Nov 27; 40(11):2143-61. PubMed ID: 22896728
    [Abstract] [Full Text] [Related]

  • 16. Prediction of oral pharmacokinetics of cMet kinase inhibitors in humans: physiologically based pharmacokinetic model versus traditional one-compartment model.
    Yamazaki S, Skaptason J, Romero D, Vekich S, Jones HM, Tan W, Wilner KD, Koudriakova T.
    Drug Metab Dispos; 2011 Mar 27; 39(3):383-93. PubMed ID: 21098644
    [Abstract] [Full Text] [Related]

  • 17. Species differential stereoselective oxidation of a methylsulfide metabolite of MK-0767 [(+/-)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl)phenyl]methyl]benzamide], a peroxisome proliferator-activated receptor dual agonist.
    Karanam BV, Welch CJ, Reddy VG, Chilenski J, Biba M, Vincent S.
    Drug Metab Dispos; 2004 Oct 27; 32(10):1061-8. PubMed ID: 15229170
    [Abstract] [Full Text] [Related]

  • 18. Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor.
    Liu L, Halladay JS, Shin Y, Wong S, Coraggio M, La H, Baumgardner M, Le H, Gopaul S, Boggs J, Kuebler P, Davis JC, Liao XC, Lubach JW, Deese A, Sowell CG, Currie KS, Young WB, Khojasteh SC, Hop CE, Wong H.
    Drug Metab Dispos; 2011 Oct 27; 39(10):1840-9. PubMed ID: 21742900
    [Abstract] [Full Text] [Related]

  • 19. Biotransformation of lovastatin. V. Species differences in in vivo metabolite profiles of mouse, rat, dog, and human.
    Halpin RA, Ulm EH, Till AE, Kari PH, Vyas KP, Hunninghake DB, Duggan DE.
    Drug Metab Dispos; 1993 Oct 27; 21(6):1003-11. PubMed ID: 7905377
    [Abstract] [Full Text] [Related]

  • 20. Metabolites of [(14)C]-5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3, 6-tetrahydropyridine in mice, rats, dogs, and humans.
    Christensen EB, Andersen JB, Pedersen H, Jensen KG, Dalgaard L.
    Drug Metab Dispos; 1999 Nov 27; 27(11):1341-9. PubMed ID: 10534320
    [Abstract] [Full Text] [Related]

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