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Items: 1 to 50 of 135

1.

Pharmacokinetic de-risking tools for selection of monoclonal antibody lead candidates.

Dostalek M, Prueksaritanont T, Kelley RF.

MAbs. 2017 Jul;9(5):756-766. doi: 10.1080/19420862.2017.1323160. Epub 2017 May 2. Review.

2.

Validation of a microdose probe drug cocktail for clinical drug interaction assessments for drug transporters and CYP3A.

Prueksaritanont T, Tatosian DA, Chu X, Railkar R, Evers R, Chavez-Eng C, Lutz R, Zeng W, Yabut J, Chan GH, Cai X, Latham AH, Hehman J, Stypinski D, Brejda J, Zhou C, Thornton B, Bateman KP, Fraser I, Stoch SA.

Clin Pharmacol Ther. 2017 Apr;101(4):519-530. doi: 10.1002/cpt.525. Epub 2016 Dec 10.

PMID:
27943276
3.

In vitro and in vivo characterisation of the metabolism and disposition of suvorexant in humans.

Cui D, Cabalu T, Yee KL, Small J, Li X, Liu B, Maciolek C, Smith S, Liu W, McCrea JB, Prueksaritanont T.

Xenobiotica. 2016 Oct;46(10):882-95. doi: 10.3109/00498254.2015.1129565. Epub 2016 Feb 10.

PMID:
26864332
4.

Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.

Roecker AJ, Mercer SP, Bergman JM, Gilbert KF, Kuduk SD, Harrell CM, Garson SL, Fox SV, Gotter AL, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4992-4999. doi: 10.1016/j.bmcl.2014.12.081. Epub 2015 Jan 6.

PMID:
25613676
5.

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23.

PMID:
25577040
6.

Drug-drug interactions related to altered absorption and plasma protein binding: theoretical and regulatory considerations, and an industry perspective.

Hochman J, Tang C, Prueksaritanont T.

J Pharm Sci. 2015 Mar;104(3):916-29. doi: 10.1002/jps.24306. Epub 2014 Dec 30. Review.

PMID:
25557998
7.

Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.

Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. doi: 10.1016/j.bmcl.2014.08.041. Epub 2014 Aug 26.

PMID:
25248679
8.

siRNA-mediated knockdown of P450 oxidoreductase in rats: a tool to reduce metabolism by CYPs and increase exposure of high clearance compounds.

Burke RS, Somasuntharam I, Rearden P, Brown D, Deshmukh SV, DiPietro MA, DiMuzio J, Eisenhandler R, Fauty SE, Gibson C, Gindy ME, Hamilton KA, Knemeyer I, Koeplinger KA, Kwon HW, Lifsted TQ, Menzel K, Patel M, Pudvah N, Rudd DJ, Seitzer J, Strapps WR, Prueksaritanont T, Thompson CD, Hochman JH, Carr BA.

Pharm Res. 2014 Dec;31(12):3445-60. doi: 10.1007/s11095-014-1433-0. Epub 2014 Jul 1.

PMID:
24980206
9.

Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.

Roecker AJ, Mercer SP, Harrell CM, Garson SL, Fox SV, Gotter AL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 May 1;24(9):2079-85. doi: 10.1016/j.bmcl.2014.03.052. Epub 2014 Mar 26.

PMID:
24704030
10.

Pitavastatin is a more sensitive and selective organic anion-transporting polypeptide 1B clinical probe than rosuvastatin.

Prueksaritanont T, Chu X, Evers R, Klopfer SO, Caro L, Kothare PA, Dempsey C, Rasmussen S, Houle R, Chan G, Cai X, Valesky R, Fraser IP, Stoch SA.

Br J Clin Pharmacol. 2014 Sep;78(3):587-98. doi: 10.1111/bcp.12377.

11.

The effect of the neonatal Fc receptor on human IgG biodistribution in mice.

Chen N, Wang W, Fauty S, Fang Y, Hamuro L, Hussain A, Prueksaritanont T.

MAbs. 2014 Mar-Apr;6(2):502-8. doi: 10.4161/mabs.27765. Epub 2014 Jan 9.

12.

Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.

Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ.

ChemMedChem. 2014 Feb;9(2):311-22. doi: 10.1002/cmdc.201300447. Epub 2013 Dec 27.

PMID:
24376006
13.

Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).

Mercer SP, Roecker AJ, Garson S, Reiss DR, Meacham Harrell C, Murphy KL, Bruno JG, Bednar RA, Lemaire W, Cui D, Cabalu TD, Tang C, Prueksaritanont T, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6620-4. doi: 10.1016/j.bmcl.2013.10.045. Epub 2013 Oct 30.

PMID:
24215892
14.

Drug-drug interaction studies: regulatory guidance and an industry perspective.

Prueksaritanont T, Chu X, Gibson C, Cui D, Yee KL, Ballard J, Cabalu T, Hochman J.

AAPS J. 2013 Jul;15(3):629-45. doi: 10.1208/s12248-013-9470-x. Epub 2013 Mar 30. Review.

15.

In vitro assessment of drug-drug interaction potential of boceprevir associated with drug metabolizing enzymes and transporters.

Chu X, Cai X, Cui D, Tang C, Ghosal A, Chan G, Green MD, Kuo Y, Liang Y, Maciolek CM, Palamanda J, Evers R, Prueksaritanont T.

Drug Metab Dispos. 2013 Mar;41(3):668-81. doi: 10.1124/dmd.112.049668. Epub 2013 Jan 4.

PMID:
23293300
16.

The impact of glycosylation on the pharmacokinetics of a TNFR2:Fc fusion protein expressed in Glycoengineered Pichia Pastoris.

Liu L, Gomathinayagam S, Hamuro L, Prueksaritanont T, Wang W, Stadheim TA, Hamilton SR.

Pharm Res. 2013 Mar;30(3):803-12. doi: 10.1007/s11095-012-0921-3. Epub 2012 Nov 8.

PMID:
23135825
17.

The impact of sialic acids on the pharmacokinetics of a PEGylated erythropoietin.

Liu L, Li H, Hamilton SR, Gomathinayagam S, Rayfield WJ, van Maanen M, Yin KC, Hong L, Prueksaritanont T.

J Pharm Sci. 2012 Dec;101(12):4414-8. doi: 10.1002/jps.23320. Epub 2012 Sep 16.

PMID:
22987365
18.

UGT2B17 genetic polymorphisms dramatically affect the pharmacokinetics of MK-7246 in healthy subjects in a first-in-human study.

Wang YH, Trucksis M, McElwee JJ, Wong PH, Maciolek C, Thompson CD, Prueksaritanont T, Garrett GC, Declercq R, Vets E, Willson KJ, Smith RC, Klappenbach JA, Opiteck GJ, Tsou JA, Gibson C, Laethem T, Panorchan P, Iwamoto M, Shaw PM, Wagner JA, Harrelson JC.

Clin Pharmacol Ther. 2012 Jul;92(1):96-102. doi: 10.1038/clpt.2012.20. Epub 2012 Jun 6.

19.

ADME of biologics-what have we learned from small molecules?

Prueksaritanont T, Tang C.

AAPS J. 2012 Sep;14(3):410-9. doi: 10.1208/s12248-012-9353-6. Epub 2012 Apr 7. Review.

20.

Lymphatic transport and catabolism of therapeutic proteins after subcutaneous administration to rats and dogs.

Wang W, Chen N, Shen X, Cunningham P, Fauty S, Michel K, Wang B, Hong X, Adreani C, Nunes CN, Johnson CV, Yin KC, Groff M, Zou Y, Liu L, Hamuro L, Prueksaritanont T.

Drug Metab Dispos. 2012 May;40(5):952-62. doi: 10.1124/dmd.111.043604. Epub 2012 Feb 10.

PMID:
22328584
21.

Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.

Coleman PJ, Schreier JD, Cox CD, Breslin MJ, Whitman DB, Bogusky MJ, McGaughey GB, Bednar RA, Lemaire W, Doran SM, Fox SV, Garson SL, Gotter AL, Harrell CM, Reiss DR, Cabalu TD, Cui D, Prueksaritanont T, Stevens J, Tannenbaum PL, Ball RG, Stellabott J, Young SD, Hartman GD, Winrow CJ, Renger JJ.

ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3.

PMID:
22307992
22.

Pharmacokinetics of IgG1 monoclonal antibodies produced in humanized Pichia pastoris with specific glycoforms: a comparative study with CHO produced materials.

Liu L, Stadheim A, Hamuro L, Pittman T, Wang W, Zha D, Hochman J, Prueksaritanont T.

Biologicals. 2011 Jul;39(4):205-10. doi: 10.1016/j.biologicals.2011.06.002. Epub 2011 Jul 1.

PMID:
21723741
23.

Theoretical analysis of interplay of therapeutic protein drug and circulating soluble target: temporal profiles of 'free' and 'total' drug and target.

Tang C, Prueksaritanont T.

Pharm Res. 2011 Oct;28(10):2447-57. doi: 10.1007/s11095-011-0471-0. Epub 2011 May 26.

PMID:
21614635
24.

Monoclonal antibodies with identical Fc sequences can bind to FcRn differentially with pharmacokinetic consequences.

Wang W, Lu P, Fang Y, Hamuro L, Pittman T, Carr B, Hochman J, Prueksaritanont T.

Drug Metab Dispos. 2011 Sep;39(9):1469-77. doi: 10.1124/dmd.111.039453. Epub 2011 May 24.

PMID:
21610128
25.

Pyridyl amides as potent inhibitors of T-type calcium channels.

Reger TS, Yang ZQ, Schlegel KA, Shu Y, Mattern C, Cube R, Rittle KE, McGaughey GB, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Renger JJ, Barrow JC.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089. Epub 2011 Jan 26.

PMID:
21316226
26.

Impact of methionine oxidation in human IgG1 Fc on serum half-life of monoclonal antibodies.

Wang W, Vlasak J, Li Y, Pristatsky P, Fang Y, Pittman T, Roman J, Wang Y, Prueksaritanont T, Ionescu R.

Mol Immunol. 2011 Mar;48(6-7):860-6. doi: 10.1016/j.molimm.2010.12.009. Epub 2011 Jan 21.

PMID:
21256596
27.

Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.

Yang ZQ, Schlegel KA, Shu Y, Reger TS, Cube R, Mattern C, Coleman PJ, Small J, Hartman GD, Ballard J, Tang C, Kuo Y, Prueksaritanont T, Nuss CE, Doran S, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Taylor AB, Zeng W, Fang W, Chavez-Eng C, Troyer MD, Luk JA, Laethem T, Cook WO, Renger JJ, Barrow JC.

ACS Med Chem Lett. 2010 Aug 24;1(9):504-9. doi: 10.1021/ml100170e. eCollection 2010 Dec 9.

28.

Indazole derivatives as novel bradykinin B1 receptor antagonists.

Bodmer-Narkevitch V, Anthony NJ, Cofre V, Jolly SM, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG, Kuduk SD.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7011-4. doi: 10.1016/j.bmcl.2010.09.121. Epub 2010 Sep 29.

PMID:
20971001
29.

Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.

Schlegel KA, Yang ZQ, Reger TS, Shu Y, Cube R, Rittle KE, Bondiskey P, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Uebele VN, Renger JJ, Barrow JC.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8.

PMID:
20673719
30.

Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.

Coleman PJ, Schreier JD, Roecker AJ, Mercer SP, McGaughey GB, Cox CD, Hartman GD, Harrell CM, Reiss DR, Doran SM, Garson SL, Anderson WB, Tang C, Prueksaritanont T, Winrow CJ, Renger JJ.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4201-5. doi: 10.1016/j.bmcl.2010.05.047. Epub 2010 May 25.

PMID:
20610153
31.

Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.

Cox CD, Breslin MJ, Whitman DB, Schreier JD, McGaughey GB, Bogusky MJ, Roecker AJ, Mercer SP, Bednar RA, Lemaire W, Bruno JG, Reiss DR, Harrell CM, Murphy KL, Garson SL, Doran SM, Prueksaritanont T, Anderson WB, Tang C, Roller S, Cabalu TD, Cui D, Hartman GD, Young SD, Koblan KS, Winrow CJ, Renger JJ, Coleman PJ.

J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c.

PMID:
20565075
32.

Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.

Barrow JC, Rittle KE, Reger TS, Yang ZQ, Bondiskey P, McGaughey GB, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Marino MJ, Kuzmick Graufelds V, Uebele VN, Renger JJ.

ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. eCollection 2010 May 13.

33.

Prediction of human clearance of therapeutic proteins: simple allometric scaling method revisited.

Wang W, Prueksaritanont T.

Biopharm Drug Dispos. 2010 May;31(4):253-63. doi: 10.1002/bdd.708.

PMID:
20437464
34.

Use of in vivo animal models to assess pharmacokinetic drug-drug interactions.

Tang C, Prueksaritanont T.

Pharm Res. 2010 Sep;27(9):1772-87. doi: 10.1007/s11095-010-0157-z. Epub 2010 Apr 29. Review.

PMID:
20428930
35.

Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.

Bell IM, Gallicchio SN, Wood MR, Quigley AG, Stump CA, Zartman CB, Fay JF, Li CC, Lynch JJ, Moore EL, Mosser SD, Prueksaritanont T, Regan CP, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG.

ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. doi: 10.1021/ml900016y. eCollection 2010 Apr 8.

36.

Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.

Schmidt A, Kimmel DB, Bai C, Scafonas A, Rutledge S, Vogel RL, McElwee-Witmer S, Chen F, Nantermet PV, Kasparcova V, Leu CT, Zhang HZ, Duggan ME, Gentile MA, Hodor P, Pennypacker B, Masarachia P, Opas EE, Adamski SA, Cusick TE, Wang J, Mitchell HJ, Kim Y, Prueksaritanont T, Perkins JJ, Meissner RS, Hartman GD, Freedman LP, Harada S, Ray WJ.

J Biol Chem. 2010 May 28;285(22):17054-64. doi: 10.1074/jbc.M109.099002. Epub 2010 Mar 31.

37.

Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.

Coleman PJ, Schreier JD, McGaughey GB, Bogusky MJ, Cox CD, Hartman GD, Ball RG, Harrell CM, Reiss DR, Prueksaritanont T, Winrow CJ, Renger JJ.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2311-5. doi: 10.1016/j.bmcl.2010.01.138. Epub 2010 Feb 8.

PMID:
20207138
38.

An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo.

Cherrin C, Haskell K, Howell B, Jones R, Leander K, Robinson R, Watkins A, Bilodeau M, Hoffman J, Sanderson P, Hartman G, Mahan E, Prueksaritanont T, Jiang G, She QB, Rosen N, Sepp-Lorenzino L, Defeo-Jones D, Huber HE.

Cancer Biol Ther. 2010 Apr 1;9(7):493-503. Epub 2010 Apr 1.

39.

Stereospecific reduction of a potent kinesin spindle protein (KSP) inhibitor in human tissues.

Li C, Lu B, Garbaccio RM, Tasber ES, Fraley ME, Hartman GD, Ye J, Harrelson JC, Prueksaritanont T.

Biochem Pharmacol. 2010 May 15;79(10):1526-33. doi: 10.1016/j.bcp.2010.01.024. Epub 2010 Jan 28.

PMID:
20109439
40.

Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Mitchell HJ, Dankulich WP, Hartman GD, Prueksaritanont T, Schmidt A, Vogel RL, Bai C, McElwee-Witmer S, Zhang HZ, Chen F, Leu CT, Kimmel DB, Ray WJ, Nantermet P, Gentile MA, Duggan ME, Meissner RS.

J Med Chem. 2009 Aug 13;52(15):4578-81. doi: 10.1021/jm900880r.

PMID:
19606870
41.

Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid concentrations in rhesus monkeys.

Tang C, Kuo Y, Pudvah NT, Ellis JD, Michener MS, Egbertson M, Graham SL, Cook JJ, Hochman JH, Prueksaritanont T.

Biochem Pharmacol. 2009 Sep 15;78(6):642-7. doi: 10.1016/j.bcp.2009.05.026. Epub 2009 May 27.

PMID:
19481060
42.

Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.

Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ.

ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069.

PMID:
19418500
43.

Impact of methionine oxidation on the binding of human IgG1 to Fc Rn and Fc gamma receptors.

Bertolotti-Ciarlet A, Wang W, Lownes R, Pristatsky P, Fang Y, McKelvey T, Li Y, Li Y, Drummond J, Prueksaritanont T, Vlasak J.

Mol Immunol. 2009 May;46(8-9):1878-82. doi: 10.1016/j.molimm.2009.02.002. Epub 2009 Mar 6.

PMID:
19269032
44.

Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences.

Roller S, Cui D, Laspina C, Miller-Stein C, Rowe J, Wong B, Prueksaritanont T.

Xenobiotica. 2009 Jan;39(1):33-45. doi: 10.1080/00498250802546861 .

PMID:
19219746
45.

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.

Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, Connolly TM, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Marino MJ, Graufelds VK, DiLella AG, Reynolds IJ, Vargas HM, Bunting PB, Woltmann RF, Magee MM, Koblan KS, Renger JJ.

J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26.

PMID:
18817368
46.

Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.

Kuduk SD, Chang RK, Dipardo RM, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5107-10. doi: 10.1016/j.bmcl.2008.07.126. Epub 2008 Aug 5.

PMID:
18722115
47.

Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.

Cox CD, Coleman PJ, Breslin MJ, Whitman DB, Garbaccio RM, Fraley ME, Buser CA, Walsh ES, Hamilton K, Schaber MD, Lobell RB, Tao W, Davide JP, Diehl RE, Abrams MT, South VJ, Huber HE, Torrent M, Prueksaritanont T, Li C, Slaughter DE, Mahan E, Fernandez-Metzler C, Yan Y, Kuo LC, Kohl NE, Hartman GD.

J Med Chem. 2008 Jul 24;51(14):4239-52. doi: 10.1021/jm800386y. Epub 2008 Jun 25.

PMID:
18578472
48.

2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Su DS, Lim JL, Tinney E, Wan BL, Murphy KL, Reiss DR, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Pettibone DJ, Yu J, Tang C, Prueksaritanont T, Freidinger RM, Bock MG, Anthony NJ.

J Med Chem. 2008 Jul 10;51(13):3946-52. doi: 10.1021/jm800199h. Epub 2008 Jun 14.

PMID:
18553956
49.

Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.

Shipe WD, Barrow JC, Yang ZQ, Lindsley CW, Yang FV, Schlegel KA, Shu Y, Rittle KE, Bock MG, Hartman GD, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Uebele VN, Nuss CE, Connolly TM, Doran SM, Fox SV, Kraus RL, Marino MJ, Graufelds VK, Vargas HM, Bunting PB, Hasbun-Manning M, Evans RM, Koblan KS, Renger JJ.

J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10.

PMID:
18540666
50.

CYP2C75-involved autoinduction of metabolism in rhesus monkeys of methyl 3-chloro-3'-fluoro-4'-{(1R)-1-[({1-[(trifluoroacetyl)amino]cyclopropyl}carbonyl)amino]ethyl}-1,1'-biphenyl-2-carboxylate (MK-0686), a bradykinin B1 receptor antagonist.

Tang C, Carr BA, Poignant F, Ma B, Polsky-Fisher SL, Kuo Y, Strong-Basalyga K, Norcross A, Richards K, Eisenhandler R, Carlini EJ, Di Marco CN, Kuduk SD, Yu NX, Raab CE, Rushmore T, Frederick CB, Bock MG, Prueksaritanont T.

J Pharmacol Exp Ther. 2008 Jun;325(3):935-46. doi: 10.1124/jpet.107.136044. Epub 2008 Feb 29.

PMID:
18310472

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