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, Christopher A, Hershey, James C, Corcoran, Halea A, Fay, John F, Johnston, Victor K, Moore, Eric L, Mosser, Scott D, Burgey, Christopher S, Paone, Daniel V, Shaw, Anthony W, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M, Koblan, Kenneth S, Kane, Stefanie A
Published in The Journal of pharmacology and experimental therapeutics (01.02.2008)
Published in The Journal of pharmacology and experimental therapeutics (01.02.2008)
Get full text
Journal Article
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, Daniel V, Shaw, Anthony W, Nguyen, Diem N, Burgey, Christopher S, Deng, James Z, Kane, Stefanie A, Koblan, Kenneth S, Salvatore, Christopher A, Mosser, Scott D, Johnston, Victor K, Wong, Bradley K, Miller-Stein, Cynthia M, Hershey, James C, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M
Published in Journal of medicinal chemistry (15.11.2007)
Published in Journal of medicinal chemistry (15.11.2007)
Get full text
Journal Article
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist
Salvatore, Christopher A, Moore, Eric L, Calamari, Amy, Cook, Jacquelynn J, Michener, Maria S, O'Malley, Stacey, Miller, Patricia J, Sur, Cyrille, Williams, Jr, David L, Zeng, Zhizhen, Danziger, Andrew, Lynch, Joseph J, Regan, Christopher P, Fay, John F, Tang, Yui S, Li, Chi-Chung, Pudvah, Nicole T, White, Rebecca B, Bell, Ian M, Gallicchio, Steven N, Graham, Samuel L, Selnick, Harold G, Vacca, Joseph P, Kane, Stefanie A
Published in The Journal of pharmacology and experimental therapeutics (01.04.2010)
Published in The Journal of pharmacology and experimental therapeutics (01.04.2010)
Get full text
Journal Article
Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid concentrations in rhesus monkeys
Tang, Cuyue, Kuo, Yuhsin, Pudvah, Nicole T., Ellis, Joan D., Michener, Maria S., Egbertson, Melissa, Graham, Samuel L., Cook, Jacquelynn J., Hochman, Jerome H., Prueksaritanont, Thomayant
Published in Biochemical pharmacology (15.09.2009)
Published in Biochemical pharmacology (15.09.2009)
Get full text
Journal Article
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
Lindsley, Stacey R., Moore, Keith P., Rajapakse, Hemaka A., Selnick, Harold G., Young, Mary Beth, Zhu, Hong, Munshi, Sanjeev, Kuo, Lawrence, McGaughey, Georgia B., Colussi, Dennis, Crouthamel, Ming-Chih, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Simon, Adam J., Seabrook, Guy R., Hazuda, Daria J., Pudvah, Nicole T., Hochman, Jerome H., Graham, Samuel L., Vacca, Joseph P., Nantermet, Philippe G.
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
Get full text
Journal Article
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors
Zhu, Hong, Young, Mary B., Nantermet, Philippe G., Graham, Samuel L., Colussi, Dennis, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Shi, Xiao-ping, Tugusheva, Katherine, Holahan, Marie A., Michener, Maria S., Cook, Jacquelynn J., Simon, Adam, Hazuda, Daria J., Vacca, Joseph P., Rajapakse, Hemaka A.
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Get full text
Journal Article
Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice
Kohl, N E, Omer, C A, Conner, M W, Anthony, N J, Davide, J P, deSolms, S J, Giuliani, E A, Gomez, R P, Graham, S L, Hamilton, K
Published in Nature medicine (01.08.1995)
Published in Nature medicine (01.08.1995)
Get more information
Journal Article
Design and Synthesis of 2,3,5-Substituted Imidazolidin-4-one Inhibitors of BACE-1
Barrow, James C., Rittle, Kenneth E., Ngo, Phung L., Selnick, Harold G., Graham, Samuel L., Pitzenberger, Steven M., McGaughey, Georgia B., Colussi, Dennis, Lai, Ming-Tain, Huang, Qian, Tugusheva, Katherine, Espeseth, Amy S., Simon, Adam J., Munshi, Sanjeev K., Vacca, Joseph P.
Published in ChemMedChem (09.07.2007)
Published in ChemMedChem (09.07.2007)
Get full text
Journal Article
Biochemical and cell-based assays for characterization of BACE-1 inhibitors
Pietrak, Beth L., Crouthamel, Ming-Chih, Tugusheva, Katherine, Lineberger, Janet E., Xu, Min, DiMuzio, Jillian M., Steele, Thomas, Espeseth, Amy S., Stachel, Shawn J., Coburn, Craig A., Graham, Samuel L., Vacca, Joseph P., Shi, Xiao-Ping, Simon, Adam J., Hazuda, Daria J., Lai, Ming-Tain
Published in Analytical biochemistry (01.07.2005)
Published in Analytical biochemistry (01.07.2005)
Get full text
Journal Article
Invention of novel 3-aminopiperidin-2-ones as calcitonin gene-related peptide receptor antagonists
Staas, Donnette D., Bell, Ian M., Burgey, Christopher S., Deng, James Z., Gallicchio, Steven N., Lim, John J., Paone, Daniel V., Potteiger, Craig M., Shaw, Anthony W., Stevenson, Heather, Stump, Craig A., Blair Zartman, C., Moore, Eric L., Bruno, Joseph G., Mosser, Scott D., White, Rebecca B., Kane, Stefanie A., Salvatore, Christopher A., Graham, Samuel L., Williams, Theresa M., Selnick, Harold G., Fraley, Mark E.
Published in Bioorganic & medicinal chemistry letters (01.11.2024)
Published in Bioorganic & medicinal chemistry letters (01.11.2024)
Get full text
Journal Article
Identification of second-generation P2X3 antagonists for treatment of pain
Ginnetti, Anthony T., Paone, Daniel V., Stauffer, Shaun R., Potteiger, Craig M., Shaw, Anthony W., Deng, James, Mulhearn, James J., Nguyen, Diem N., Segerdell, Carolyn, Anquandah, Juliana, Calamari, Amy, Cheng, Gong, Leitl, Michael D., Liang, Annie, Moore, Eric, Panigel, Jacqueline, Urban, Mark, Wang, Jixin, Fillgrove, Kerry, Tang, Cuyue, Cook, Sean, Kane, Stefanie, Salvatore, Christopher A., Graham, Samuel L., Burgey, Christopher S.
Published in Bioorganic & medicinal chemistry letters (01.05.2018)
Published in Bioorganic & medicinal chemistry letters (01.05.2018)
Get full text
Journal Article
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
Sankaranarayanan, Sethu, Holahan, Marie A, Colussi, Dennis, Crouthamel, Ming-Chih, Devanarayan, Viswanath, Ellis, Joan, Espeseth, Amy, Gates, Adam T, Graham, Samuel L, Gregro, Allison R, Hazuda, Daria, Hochman, Jerome H, Holloway, Katharine, Jin, Lixia, Kahana, Jason, Lai, Ming-tain, Lineberger, Janet, McGaughey, Georgia, Moore, Keith P, Nantermet, Philippe, Pietrak, Beth, Price, Eric A, Rajapakse, Hemaka, Stauffer, Shaun, Steinbeiser, Melissa A, Seabrook, Guy, Selnick, Harold G, Shi, Xiao-Ping, Stanton, Matthew G, Swestock, John, Tugusheva, Katherine, Tyler, Keala X, Vacca, Joseph P, Wong, Jacky, Wu, Guoxin, Xu, Min, Cook, Jacquelynn J, Simon, Adam J
Published in The Journal of pharmacology and experimental therapeutics (01.01.2009)
Published in The Journal of pharmacology and experimental therapeutics (01.01.2009)
Get full text
Journal Article
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
Egbertson, Melissa, McGaughey, Georgia B., Pitzenberger, Steven M., Stauffer, Shaun R., Coburn, Craig A., Stachel, Shawn J., Yang, Wenjin, Barrow, James C., Neilson, Lou Anne, McWherter, Melody, Perlow, Debra, Fahr, Bruce, Munshi, Sanjeev, Allison, Timothy J., Holloway, Katharine, Selnick, Harold G., Yang, ZhiQiang, Swestock, John, Simon, Adam J., Sankaranarayanan, Sethu, Colussi, Dennis, Tugusheva, Katherine, Lai, Ming-Tain, Pietrak, Beth, Haugabook, Shari, Jin, Lixia, Chen, I.-W., Holahan, Marie, Stranieri-Michener, Maria, Cook, Jacquelynn J., Vacca, Joseph, Graham, Samuel L.
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Get full text
Journal Article
Discovery of pyrrolidine-based β-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency
Stachel, Shawn J., Steele, Thomas G., Petrocchi, Alessia, Haugabook, Sharie J., McGaughey, Georgia, Katharine Holloway, M., Allison, Timothy, Munshi, Sanjeev, Zuck, Paul, Colussi, Dennis, Tugasheva, Katherine, Wolfe, Abigail, Graham, Samuel L., Vacca, Joseph P.
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Get full text
Journal Article
Macrocyclic Inhibitors of β-Secretase: Functional Activity in an Animal Model
Stachel, Shawn J, Coburn, Craig A, Sankaranarayanan, Sethu, Price, Eric A, Pietrak, Beth L, Huang, Qian, Lineberger, Janet, Espeseth, Amy S, Jin, Lixia, Ellis, Joan, Holloway, M. Katharine, Munshi, Sanjeev, Allison, Timothy, Hazuda, Daria, Simon, Adam J, Graham, Samuel L, Vacca, Joseph P
Published in Journal of medicinal chemistry (19.10.2006)
Published in Journal of medicinal chemistry (19.10.2006)
Get full text
Journal Article
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
Burgey, Christopher S, Paone, Daniel V, Shaw, Anthony W, Deng, James Z, Nguyen, Diem N, Potteiger, Craig M, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M
Published in Organic letters (07.08.2008)
Published in Organic letters (07.08.2008)
Get full text
Journal Article
Discovery of aminoheterocycles as a novel β-secretase inhibitor class: pH dependence on binding activity part 1
Stachel, Shawn J., Coburn, Craig A., Rush, Diane, Jones, Kristen L.G., Zhu, Hong, Rajapakse, Hemaka, Graham, Samuel L., Simon, Adam, Katharine Holloway, M., Allison, Tim J., Munshi, Sanjeev K., Espeseth, Amy S., Zuck, Paul, Colussi, Dennis, Wolfe, Abigail, Pietrak, Beth L., Lai, Ming-Tain, Vacca, Joseph P.
Published in Bioorganic & medicinal chemistry letters (01.06.2009)
Published in Bioorganic & medicinal chemistry letters (01.06.2009)
Get full text
Journal Article
MK-8825: A potent and selective CGRP receptor antagonist with good oral activity in rats
Bell, Ian M., Stump, Craig A., Gallicchio, Steven N., Staas, Donnette D., Zartman, C. Blair, Moore, Eric L., Sain, Nova, Urban, Mark, Bruno, Joseph G., Calamari, Amy, Kemmerer, Amanda L., Mosser, Scott D., Fandozzi, Christine, White, Rebecca B., Zrada, Matthew M., Selnick, Harold G., Graham, Samuel L., Vacca, Joseph P., Kane, Stefanie A., Salvatore, Christopher A.
Published in Bioorganic & medicinal chemistry letters (15.06.2012)
Published in Bioorganic & medicinal chemistry letters (15.06.2012)
Get full text
Journal Article
Discovery and X-ray Crystallographic Analysis of a Spiropiperidine Iminohydantoin Inhibitor of β-Secretase
Barrow, James C, Stauffer, Shaun R, Rittle, Kenneth E, Ngo, Phung L, Yang, ZhiQiang, Selnick, Harold G, Graham, Samuel L, Munshi, Sanjeev, McGaughey, Georgia B, Holloway, M. Katharine, Simon, Adam J, Price, Eric A, Sankaranarayanan, Sethu, Colussi, Dennis, Tugusheva, Katherine, Lai, Ming-Tain, Espeseth, Amy S, Xu, Min, Huang, Qian, Wolfe, Abigail, Pietrak, Beth, Zuck, Paul, Levorse, Dorothy A, Hazuda, Daria, Vacca, Joseph P
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
Get full text
Journal Article