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Items: 1 to 20 of 103

1.

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.

Luo G, Chen L, Conway CM, Denton R, Keavy D, Gulianello M, Huang Y, Kostich W, Lentz KA, Mercer SE, Schartman R, Signor L, Browning M, Macor JE, Dubowchik GM.

ACS Med Chem Lett. 2012 Feb 27;3(4):337-41. doi: 10.1021/ml300021s. eCollection 2012 Apr 12.

2.

Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.

Luo G, Chen L, Conway CM, Denton R, Keavy D, Signor L, Kostich W, Lentz KA, Santone KS, Schartman R, Browning M, Tong G, Houston JG, Dubowchik GM, Macor JE.

J Med Chem. 2012 Dec 13;55(23):10644-51. doi: 10.1021/jm3013147. Epub 2012 Nov 15.

PMID:
23153230
3.

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.

J Pharmacol Exp Ther. 2008 Feb;324(2):416-21. Epub 2007 Nov 26.

4.

Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.

Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA.

J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11.

5.

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.

Chaturvedula PV, Mercer SE, Pin SS, Thalody G, Xu C, Conway CM, Keavy D, Signor L, Cantor GH, Mathias N, Moench P, Denton R, Macci R, Schartman R, Whiterock V, Davis C, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3157-61. doi: 10.1016/j.bmcl.2013.04.012. Epub 2013 Apr 12.

PMID:
23632269
6.

Pharmacologic Characterization of AMG 334, a Potent and Selective Human Monoclonal Antibody against the Calcitonin Gene-Related Peptide Receptor.

Shi L, Lehto SG, Zhu DX, Sun H, Zhang J, Smith BP, Immke DC, Wild KD, Xu C.

J Pharmacol Exp Ther. 2016 Jan;356(1):223-31. doi: 10.1124/jpet.115.227793. Epub 2015 Nov 11.

7.

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.

8.

Inhibition of capsaicin-induced increase in dermal blood flow by the oral CGRP receptor antagonist, telcagepant (MK-0974).

Sinclair SR, Kane SA, Van der Schueren BJ, Xiao A, Willson KJ, Boyle J, de Lepeleire I, Xu Y, Hickey L, Denney WS, Li CC, Palcza J, Vanmolkot FH, Depré M, Van Hecken A, Murphy MG, Ho TW, de Hoon JN.

Br J Clin Pharmacol. 2010 Jan;69(1):15-22. doi: 10.1111/j.1365-2125.2009.03543.x.

10.

Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines.

Civiello RL, Han X, Beno BR, Chaturvedula PV, Herbst JJ, Xu C, Conway CM, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1229-32. doi: 10.1016/j.bmcl.2016.01.026. Epub 2016 Jan 16.

PMID:
26832218
11.

Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.

Joshi P, Anderson C, Binch H, Hadida S, Yoo S, Bergeron D, Decker C, terHaar E, Moore J, Garcia-Guzman M, Termin A.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):845-9. doi: 10.1016/j.bmcl.2013.12.089. Epub 2013 Dec 26. Erratum in: Bioorg Med Chem Lett. 2014 Apr 15;24(8):2009.

PMID:
24405707
12.

Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine.

Durham PL, Vause CV.

CNS Drugs. 2010 Jul;24(7):539-48. doi: 10.2165/11534920-000000000-00000.

13.

Immunohistochemical localization of the calcitonin gene-related peptide binding site in the primate trigeminovascular system using functional antagonist antibodies.

Miller S, Liu H, Warfvinge K, Shi L, Dovlatyan M, Xu C, Edvinsson L.

Neuroscience. 2016 Jul 22;328:165-83. doi: 10.1016/j.neuroscience.2016.04.046. Epub 2016 May 4.

PMID:
27155150
14.

Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure.

Degnan AP, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Denton R, Han X, Macci R, Mathias NR, Moench P, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Macor JE, Dubowchik GM.

J Med Chem. 2008 Aug 28;51(16):4858-61. doi: 10.1021/jm800546t. Epub 2008 Jul 30.

PMID:
18665579
15.

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.

Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Macci R, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Chaturvedula PV, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4723-7. doi: 10.1016/j.bmcl.2012.05.074. Epub 2012 Jun 1.

PMID:
22727645
17.

Calcitonin gene-related peptide and its role in migraine pathophysiology.

Arulmani U, Maassenvandenbrink A, Villalón CM, Saxena PR.

Eur J Pharmacol. 2004 Oct 1;500(1-3):315-30. Review.

PMID:
15464043
18.

The tortuous road to an ideal CGRP function blocker for the treatment of migraine.

Davis CD, Xu C.

Curr Top Med Chem. 2008;8(16):1468-79. Review.

PMID:
18991732
19.

The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.

Bell IM, Bednar RA, Corcoran HA, Fay JF, Gallicchio SN, Johnston VK, Hershey JC, Miller-Stein CM, Moore EL, Mosser SD, Roller SA, Salvatore CA, Theberge CR, Wong BK, Blair Zartman C, Kane SA, Williams TM, Graham SL, Vacca JP.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. doi: 10.1016/j.bmcl.2009.06.057. Epub 2009 Jun 17.

PMID:
19577468
20.

CGRP antagonists and antibodies for the treatment of migraine.

Vécsei L, Szok D, Csáti A, Tajti J.

Expert Opin Investig Drugs. 2015 Jan;24(1):31-41. Epub 2014 Sep 15.

PMID:
25219387

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