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336 results

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Page 1
Identification of a novel RAMP-independent CGRP receptor antagonist.
Zartman CB, Bell IM, Gallicchio SN, Graham SL, Kane SA, Mallee JJ, Rutledge RZ, Salvatore CA, Vacca JP, Williams TM. Zartman CB, et al. Among authors: graham sl. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6705-8. doi: 10.1016/j.bmcl.2011.09.056. Epub 2011 Sep 21. Bioorg Med Chem Lett. 2011. PMID: 21982500
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB. Bell IM, et al. Among authors: graham sl. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Dinsmore CJ, Zartman CB, Bergman JM, Abrams MT, Buser CA, Culberson JC, Davide JP, Ellis-Hutchings M, Fernandes C, Graham SL, Hartman GD, Huber HE, Lobell RB, Mosser SD, Robinson RG, Williams TM. Dinsmore CJ, et al. Among authors: graham sl. Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43. doi: 10.1016/j.bmcl.2003.11.051. Bioorg Med Chem Lett. 2004. PMID: 14741259
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Williams TM, Stump CA, Nguyen DN, Quigley AG, Bell IM, Gallicchio SN, Zartman CB, Wan BL, Penna KD, Kunapuli P, Kane SA, Koblan KS, Mosser SD, Rutledge RZ, Salvatore C, Fay JF, Vacca JP, Graham SL. Williams TM, et al. Among authors: graham sl. Bioorg Med Chem Lett. 2006 May 15;16(10):2595-8. doi: 10.1016/j.bmcl.2006.02.051. Epub 2006 Mar 9. Bioorg Med Chem Lett. 2006. PMID: 16527483
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Burgey CS, Stump CA, Nguyen DN, Deng JZ, Quigley AG, Norton BR, Bell IM, Mosser SD, Salvatore CA, Rutledge RZ, Kane SA, Koblan KS, Vacca JP, Graham SL, Williams TM. Burgey CS, et al. Among authors: graham sl. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5052-6. doi: 10.1016/j.bmcl.2006.07.044. Epub 2006 Aug 2. Bioorg Med Chem Lett. 2006. PMID: 16889959
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hochman JH, McMasters DR, Miller-Stein C, Moore EL, Mosser SD, Pudvah NT, Quigley AG, Salvatore CA, Stump CA, Theberge CR, Wong BK, Zartman CB, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Bell IM, et al. Among authors: graham sl. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6165-9. doi: 10.1016/j.bmcl.2006.09.045. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2006. PMID: 17027263
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.
Shaw AW, Paone DV, Nguyen DN, Stump CA, Burgey CS, Mosser SD, Salvatore CA, Rutledge RZ, Kane SA, Koblan KS, Graham SL, Vacca JP, Williams TM. Shaw AW, et al. Among authors: graham sl. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4795-8. doi: 10.1016/j.bmcl.2007.06.062. Epub 2007 Jun 26. Bioorg Med Chem Lett. 2007. PMID: 17616394
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).
Paone DV, Shaw AW, Nguyen DN, Burgey CS, Deng JZ, Kane SA, Koblan KS, Salvatore CA, Mosser SD, Johnston VK, Wong BK, Miller-Stein CM, Hershey JC, Graham SL, Vacca JP, Williams TM. Paone DV, et al. Among authors: graham sl. J Med Chem. 2007 Nov 15;50(23):5564-7. doi: 10.1021/jm070668p. Epub 2007 Oct 11. J Med Chem. 2007. PMID: 17929795
Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine.
Salvatore CA, Hershey JC, Corcoran HA, Fay JF, Johnston VK, Moore EL, Mosser SD, Burgey CS, Paone DV, Shaw AW, Graham SL, Vacca JP, Williams TM, Koblan KS, Kane SA. Salvatore CA, et al. Among authors: graham sl. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21. doi: 10.1124/jpet.107.130344. Epub 2007 Nov 26. J Pharmacol Exp Ther. 2008. PMID: 18039958
336 results