Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity
Schenkel, Laurie B, Olivieri, Philip R, Boezio, Alessandro A, Deak, Holly L, Emkey, Renee, Graceffa, Russell F, Gunaydin, Hakan, Guzman-Perez, Angel, Lee, Josie H, Teffera, Yohannes, Wang, Weiya, Youngblood, Beth D, Yu, Violeta L, Zhang, Maosheng, Gavva, Narender R, Lehto, Sonya G, Geuns-Meyer, Stephanie
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition
Boezio, Alessandro A., Andrews, Kristin, Boezio, Christiane, Chu-Moyer, Margaret, Copeland, Katrina W., DiMauro, Erin F., Foti, Robert S., Fremeau, Robert T., Gao, Hua, Geuns-Meyer, Stephanie, Graceffa, Russell F., Gunaydin, Hakan, Huang, Hongbing, La, Daniel S., Ligutti, Joseph, Moyer, Bryan D., Peterson, Emily A., Yu, Violeta, Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid
Weiss, Matthew M, Williamson, Toni, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dineen, Thomas A, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, Rattan, Claire, San Miguel, Tisha, Sickmier, E.Allen, Wahl, Robert C, Wen, Paul H, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Journal Article
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na V 1.7 inhibition
Boezio, Alessandro A, Andrews, Kristin, Boezio, Christiane, Chu-Moyer, Margaret, Copeland, Katrina W, DiMauro, Erin F, Foti, Robert S, Fremeau, Jr, Robert T, Gao, Hua, Geuns-Meyer, Stephanie, Graceffa, Russell F, Gunaydin, Hakan, Huang, Hongbing, La, Daniel S, Ligutti, Joseph, Moyer, Bryan D, Peterson, Emily A, Yu, Violeta, Weiss, Matthew M
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors
Dineen, Thomas A, Weiss, Matthew M, Williamson, Toni, Acton, Paul, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dunn, Robert T, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, San Miguel, Tisha, Sickmier, E. Allen, Vargas, Hugo M, Wahl, Robert C, Wen, Paul H, Whittington, Douglas A, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Journal Article
Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Jr, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Novel 2,3-Dihydro-1,4-Benzoxazines as Potent and Orally Bioavailable Inhibitors of Tumor-Driven Angiogenesis
La, Daniel S, Belzile, Julie, Bready, James V, Coxon, Angela, DeMelfi, Thomas, Doerr, Nicholas, Estrada, Juan, Flynn, Julie C, Flynn, Shaun R, Graceffa, Russell F, Harriman, Shawn P, Larrow, Jay F, Long, Alexander M, Martin, Matthew W, Morrison, Michael J, Patel, Vinod F, Roveto, Philip M, Wang, Ling, Weiss, Matthew M, Whittington, Douglas A, Teffera, Yohannes, Zhao, Zhiyang, Polverino, Anthony J, Harmange, Jean-Christophe
Published in Journal of medicinal chemistry (27.03.2008)
Published in Journal of medicinal chemistry (27.03.2008)
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Journal Article
Naphthamides as Novel and Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Design, Synthesis, and Evaluation
Harmange, Jean-Christophe, Weiss, Matthew M, Germain, Julie, Polverino, Anthony J, Borg, George, Bready, James, Chen, Danlin, Choquette, Deborah, Coxon, Angela, DeMelfi, Tom, DiPietro, Lucian, Doerr, Nicholas, Estrada, Juan, Flynn, Julie, Graceffa, Russell F, Harriman, Shawn P, Kaufman, Stephen, La, Daniel S, Long, Alexander, Martin, Matthew W, Neervannan, Sesha, Patel, Vinod F, Potashman, Michele, Regal, Kelly, Roveto, Phillip M, Schrag, Michael L, Starnes, Charlie, Tasker, Andrew, Teffera, Yohannes, Wang, Ling, White, Ryan D, Whittington, Douglas A, Zanon, Roger
Published in Journal of medicinal chemistry (27.03.2008)
Published in Journal of medicinal chemistry (27.03.2008)
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Journal Article
Evaluation of a Series of Naphthamides as Potent, Orally Active Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitors
Weiss, Matthew M, Harmange, Jean-Christophe, Polverino, Anthony J, Bauer, David, Berry, Loren, Berry, Virginia, Borg, George, Bready, James, Chen, Danlin, Choquette, Deborah, Coxon, Angela, DeMelfi, Tom, Doerr, Nicholas, Estrada, Juan, Flynn, Julie, Graceffa, Russell F, Harriman, Shawn P, Kaufman, Stephen, La, Daniel S, Long, Alexander, Neervannan, Sesha, Patel, Vinod F, Potashman, Michele, Regal, Kelly, Roveto, Phillip M, Schrag, Michael L, Starnes, Charlie, Tasker, Andrew, Teffera, Yohannes, Whittington, Douglas A, Zanon, Roger
Published in Journal of medicinal chemistry (27.03.2008)
Published in Journal of medicinal chemistry (27.03.2008)
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Journal Article
Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 1. N-Cyanoguanidine Bioisosteres Possessing in Vivo Bladder Selectivity
Butera, John A, Antane, Madelene M, Antane, Schuyler A, Argentieri, Thomas M, Freeden, Chris, Graceffa, Russell F, Hirth, Bradford H, Jenkins, Douglas, Lennox, Joseph R, Matelan, Edward, Norton, N. Wesley, Quagliato, Dominick, Sheldon, Jeffrey H, Spinelli, Walter, Warga, Dawn, Wojdan, Alexandra, Woods, Morgan
Published in Journal of medicinal chemistry (23.03.2000)
Published in Journal of medicinal chemistry (23.03.2000)
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Journal Article
Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 2. Selective and Potent Benzylamino Cyclobutenediones
Gilbert, Adam M, Antane, Madelene M, Argentieri, Thomas M, Butera, John A, Francisco, Gerardo D, Freeden, Chris, Gundersen, Eric G, Graceffa, Russell F, Herbst, David, Hirth, Bradford H, Lennox, Joseph R, McFarlane, Geraldine, Norton, N. Wesley, Quagliato, Dominick, Sheldon, Jeffrey H, Warga, Dawn, Wojdan, Alexandra, Woods, Morgan
Published in Journal of medicinal chemistry (23.03.2000)
Published in Journal of medicinal chemistry (23.03.2000)
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Journal Article
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na(v)1.7 inhibition
Boezio, Alessandro A., Andrews, Kristin, Boezio, Christiane, Chu-Moyer, Margaret, Copeland, Katrina W., DiMauro, Erin F., Foti, Robert S., Fremeau, Robert T., Gao, Hua, Geuns-Meyer, Stephanie, Graceffa, Russell F., Gunaydin, Hakan, Huang, Hongbing, La, Daniel S., Ligutti, Joseph, Moyer, Bryan D., Peterson, Emily A., Yu, Violeta, Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Design, synthesis, and evaluations
Harmange, Jean-Christophe, Weiss, Matthew M., Germain, Julie, Polverino, Anthony J., Borg, George, Bready, James, Chen, Danlin, Choquette, Deborah, Coxon, Angela, DeMelfi, Tom, DiPietro, Lucian, Doerr, Nicholas, Estrada, Juan, Flynn, Julie, Graceffa, Russell F., Harriman, Shawn P., Kaufman, Stephen, La, Daniel S., Long, Alexander, Martin, Matthew W., Neervannan, Sesha, Patel, Vinod F., Potashman, Michele, Regal, Kelly, Roveto, Phillip M., Schrag, Michael L., Starnes, Charlie, Tasker, Andrew, Teffera, Yohannes, Wang, Ling, White, Ryan D., Whittington, Douglas A., Zanon, Roger
Published in Journal of medicinal chemistry (27.03.2008)
Published in Journal of medicinal chemistry (27.03.2008)
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Journal Article
1,3-disubstituted-2-thioxo-imidazolidine-4,5-diones as potassium channel openers
BUTERA JOHN A, ELOKDAH HASSAN M, SULKOWSKI THEODORE S, GRACEFFA RUSSELL F, LENNOX JOSEPH R, PRIMEAU JOHN L
Year of Publication 03.10.2006
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Year of Publication 03.10.2006
Patent
1,3-disubstituted-2-thioxo-imidazolidine-4,5-diones as potassium channel openers
Butera, John A, Elokdah, Hassan M, Sulkowski, Theodore S, Primeau, John L, Lennox, Joseph R, Graceffa, Russell F
Year of Publication 03.10.2006
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Year of Publication 03.10.2006
Patent