Publications by authors named "Samuel L Graham"

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Invention of novel 3-aminopiperidin-2-ones as calcitonin gene-related peptide receptor antagonists.
Donnette D Staas, Ian M Bell, Christopher S Burgey, James Z Deng, Steven N Gallicchio, Samuel L Graham

Bioorg Med Chem Lett· November 2024

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Identification of second-generation P2X3 antagonists for treatment of pain.
Anthony T Ginnetti, Daniel V Paone, Shaun R Stauffer, Craig M Potteiger, Anthony W Shaw, Samuel L Graham

Bioorg Med Chem Lett· May 2018

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Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.
Melissa Egbertson, Georgia B McGaughey, Steven M Pitzenberger, Shaun R Stauffer, Craig A Coburn, Samuel L Graham

Bioorg Med Chem Lett· November 2015

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[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
Ian M Bell, Steven N Gallicchio, Craig A Stump, Joseph G Bruno, Hong Fan, Samuel L Graham

ACS Med Chem Lett· September 2013

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MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Ian M Bell, Craig A Stump, Steven N Gallicchio, Donnette D Staas, C Blair Zartman, Samuel L Graham

Bioorg Med Chem Lett· June 2012

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Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Shawn J Stachel, Thomas G Steele, Alessia Petrocchi, Sharie J Haugabook, Georgia McGaughey, Samuel L Graham

Bioorg Med Chem Lett· January 2012

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Identification of a novel RAMP-independent CGRP receptor antagonist.
C Blair Zartman, Ian M Bell, Steven N Gallicchio, Samuel L Graham, Stefanie A Kane

Bioorg Med Chem Lett· November 2011

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Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
Christopher A Salvatore, Eric L Moore, Amy Calamari, Jacquelynn J Cook, Maria S Michener, Samuel L Graham

J Pharmacol Exp Ther· April 2010

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Identification of potent, highly constrained CGRP receptor antagonists.
Craig A Stump, Ian M Bell, Rodney A Bednar, John F Fay, Steven N Gallicchio, Samuel L Graham

Bioorg Med Chem Lett· April 2010

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Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.
Hong Zhu, Mary B Young, Philippe G Nantermet, Samuel L Graham, Dennis Colussi

Bioorg Med Chem Lett· March 2010

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Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid concentrations in rhesus monkeys.
Cuyue Tang, Yuhsin Kuo, Nicole T Pudvah, Joan D Ellis, Maria S Michener, Samuel L Graham

Biochem Pharmacol· September 2009

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A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.
Ivory D Hills, M Katharine Holloway, Pablo de León, Ashley Nomland, Hong Zhu, Samuel L Graham

Bioorg Med Chem Lett· September 2009

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The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Ian M Bell, Rodney A Bednar, Halea A Corcoran, John F Fay, Steven N Gallicchio, Samuel L Graham

Bioorg Med Chem Lett· August 2009

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Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Shawn J Stachel, Craig A Coburn, Diane Rush, Kristen L G Jones, Hong Zhu, Samuel L Graham

Bioorg Med Chem Lett· June 2009

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First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
Sethu Sankaranarayanan, Marie A Holahan, Dennis Colussi, Ming-Chih Crouthamel, Viswanath Devanarayan, Samuel L Graham

J Pharmacol Exp Ther· January 2009

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The discovery of highly potent CGRP receptor antagonists.
Craig A Stump, Ian M Bell, Rodney A Bednar, Joseph G Bruno, John F Fay, Samuel L Graham

Bioorg Med Chem Lett· January 2009

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Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.
Thomas G Steele, Ivory D Hills, Ashley A Nomland, Pablo de León, Timothy Allison, Samuel L Graham

Bioorg Med Chem Lett· January 2009

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Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.
Philippe G Nantermet, Hemaka A Rajapakse, Mathew G Stanton, Shaun R Stauffer, James C Barrow, Samuel L Graham

ChemMedChem· January 2009

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Potent benzimidazolone-based CGRP receptor antagonists.
Cory R Theberge, Rodney A Bednar, Ian M Bell, Halea A Corcoran, John F Fay, Samuel L Graham

Bioorg Med Chem Lett· December 2008

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Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
James C Barrow, Shaun R Stauffer, Kenneth E Rittle, Phung L Ngo, ZhiQiang Yang, Samuel L Graham

J Med Chem· October 2008

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Synthesis of the (3R,6S)-3-amino-6-(2,3-difluorophenyl)azepan-2-one of telcagepant (MK-0974), a calcitonin gene-related peptide receptor antagonist for the treatment of migraine headache.
Christopher S Burgey, Daniel V Paone, Anthony W Shaw, James Z Deng, Diem N Nguyen, Samuel L Graham

Org Lett· August 2008

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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.
Christopher A Salvatore, James C Hershey, Halea A Corcoran, John F Fay, Victor K Johnston, Samuel L Graham

J Pharmacol Exp Ther· February 2008

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Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.
Diem N Nguyen, Daniel V Paone, Anthony W Shaw, Christopher S Burgey, Scott D Mosser, Samuel L Graham

Bioorg Med Chem Lett· January 2008

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Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Keith P Moore, Hong Zhu, Hemaka A Rajapakse, Georgia B McGaughey, Dennis Colussi, Samuel L Graham

Bioorg Med Chem Lett· November 2007

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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).
Daniel V Paone, Anthony W Shaw, Diem N Nguyen, Christopher S Burgey, James Z Deng, Samuel L Graham

J Med Chem· November 2007

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