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Page 1
Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.
Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ. Raheem IT, et al. Among authors: coleman pj. J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. J Med Chem. 2015. PMID: 26397965
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD, Huff JR, Kimmel DB, Leu CT, Meissner RS, Merkle K, Nagy R, Pennypacker B, Perkins JJ, Prueksaritanont T, Rodan GA, Varga SL, Wesolowski GA, Zartman AE, Rodan SB, Duggan ME. Hutchinson JH, et al. Among authors: coleman pj. J Med Chem. 2003 Oct 23;46(22):4790-8. doi: 10.1021/jm030306r. J Med Chem. 2003. PMID: 14561098
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Coleman PJ, Brashear KM, Askew BC, Hutchinson JH, McVean CA, Duong LT, Feuston BP, Fernandez-Metzler C, Gentile MA, Hartman GD, Kimmel DB, Leu CT, Lipfert L, Merkle K, Pennypacker B, Prueksaritanont T, Rodan GA, Wesolowski GA, Rodan SB, Duggan ME. Coleman PJ, et al. J Med Chem. 2004 Sep 23;47(20):4829-37. doi: 10.1021/jm049874c. J Med Chem. 2004. PMID: 15369386
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Cox CD, Torrent M, Breslin MJ, Mariano BJ, Whitman DB, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Schaber MD, Lobell RB, Tao W, South VJ, Kohl NE, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Li C, Mahan E, Lu B, Hartman GD. Cox CD, et al. Among authors: coleman pj. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3175-9. doi: 10.1016/j.bmcl.2006.03.040. Epub 2006 Apr 5. Bioorg Med Chem Lett. 2006. PMID: 16603356
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.
Coleman PJ, Schreier JD, Cox CD, Fraley ME, Garbaccio RM, Buser CA, Walsh ES, Hamilton K, Lobell RB, Rickert K, Tao W, Diehl RE, South VJ, Davide JP, Kohl NE, Yan Y, Kuo L, Prueksaritanont T, Li C, Mahan EA, Fernandez-Metzler C, Salata JJ, Hartman GD. Coleman PJ, et al. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5390-5. doi: 10.1016/j.bmcl.2007.07.046. Epub 2007 Aug 6. Bioorg Med Chem Lett. 2007. PMID: 17761419
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Roecker AJ, Coleman PJ, Mercer SP, Schreier JD, Buser CA, Walsh ES, Hamilton K, Lobell RB, Tao W, Diehl RE, South VJ, Davide JP, Kohl NE, Yan Y, Kuo LC, Li C, Fernandez-Metzler C, Mahan EA, Prueksaritanont T, Hartman GD. Roecker AJ, et al. Among authors: coleman pj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5677-82. doi: 10.1016/j.bmcl.2007.07.074. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17766111
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Garbaccio RM, Tasber ES, Neilson LA, Coleman PJ, Fraley ME, Olson C, Bergman J, Torrent M, Buser CA, Rickert K, Walsh ES, Hamilton K, Lobell RB, Tao W, South VJ, Diehl RE, Davide JP, Yan Y, Kuo LC, Li C, Prueksaritanont T, Fernandez-Metzler C, Mahan EA, Slaughter DE, Salata JJ, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Among authors: coleman pj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5671-6. doi: 10.1016/j.bmcl.2007.07.067. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17804233
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. Cox CD, et al. Among authors: coleman pj. J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c. J Med Chem. 2010. PMID: 20565075
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. Coleman PJ, et al. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4201-5. doi: 10.1016/j.bmcl.2010.05.047. Epub 2010 May 25. Bioorg Med Chem Lett. 2010. PMID: 20610153
159 results