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Page 1
Proline bis-amides as potent dual orexin receptor antagonists.
Bergman JM, Roecker AJ, Mercer SP, Bednar RA, Reiss DR, Ransom RW, Meacham Harrell C, Pettibone DJ, Lemaire W, Murphy KL, Li C, Prueksaritanont T, Winrow CJ, Renger JJ, Koblan KS, Hartman GD, Coleman PJ. Bergman JM, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. doi: 10.1016/j.bmcl.2008.01.001. Epub 2008 Jan 8. Bioorg Med Chem Lett. 2008. PMID: 18207395
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
Coleman PJ, Askew BC, Hutchinson JH, Whitman DB, Perkins JJ, Hartman GD, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Merkle KM, Lynch R, Lynch JJ, Rodan SB, Duggan ME. Coleman PJ, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2463-5. doi: 10.1016/s0960-894x(02)00396-7. Bioorg Med Chem Lett. 2002. PMID: 12161158
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.
Brashear KM, Hunt CA, Kucer BT, Duggan ME, Hartman GD, Rodan GA, Rodan SB, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Barrish A, Homnick CF, Hutchinson JH, Coleman PJ. Brashear KM, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3483-6. doi: 10.1016/s0960-894x(02)00743-6. Bioorg Med Chem Lett. 2002. PMID: 12419389
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. Among authors: hartman gd. 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: hartman gd. 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
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. Yang ZQ, et al. Among authors: hartman gd. J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817368
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. Whitman DB, et al. Among authors: hartman gd. ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069. ChemMedChem. 2009. PMID: 19418500
Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Melamed JY, Zartman AE, Kett NR, Gotter AL, Uebele VN, Reiss DR, Condra CL, Fandozzi C, Lubbers LS, Rowe BA, McGaughey GB, Henault M, Stocco R, Renger JJ, Hartman GD, Bilodeau MT, Trotter BW. Melamed JY, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4700-3. doi: 10.1016/j.bmcl.2010.04.143. Epub 2010 May 5. Bioorg Med Chem Lett. 2010. PMID: 20510609
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: hartman gd. J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c. J Med Chem. 2010. PMID: 20565075
171 results