Search Results - "Kaller, Matthew R"

Discovery of TRPM8 Antagonist (S)‑6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine by Horne, Daniel B, Biswas, Kaustav, Brown, James, Bartberger, Michael D, Clarine, Jeffrey, Davis, Carl D, Gore, Vijay K, Harried, Scott, Horner, Michelle, Kaller, Matthew R, Lehto, Sonya G, Liu, Qingyian, Ma, Vu V, Monenschein, Holger, Nguyen, Thomas T, Yuan, Chester C, Youngblood, Beth D, Zhang, Maosheng, Zhong, Wenge, Allen, Jennifer R, Chen, Jian Jeffrey, Gavva, Narender R

“…Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a…”
Get full text

Synthesis and structure–activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors by Reichelt, Andreas, Bailis, Julie M., Bartberger, Michael D., Yao, Guomin, Shu, Hong, Kaller, Matthew R., Allen, John G., Weidner, Margaret F., Keegan, Kathleen S., Dao, Jennifer H.

“…The Cell division cycle 7 (Cdc7) protein kinase is essential for DNA replication and maintenance of genome stability. We systematically explored thiazole-based…”
Get full text

Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe by Tamayo, Nuria A, Bourbeau, Matthew P, Allen, Jennifer R, Ashton, Kate S, Chen, Jian Jeffrey, Kaller, Matthew R, Nguyen, Thomas T, Nishimura, Nobuko, Pettus, Liping H, Walton, Mary, Belmontes, Brian, Moriguchi, Jodi, Chen, Kui, McCarter, John D, Hanestad, Kelly, Chung, Grace, Ninniri, Maria Stefania S, Sun, Jan, Poppe, Leszek, Spahr, Chris, Hui, John, Jia, Lei, Wu, Tian, Dahal, Upendra P, Edson, Katheryne Z, Payton, Marc

“…Chromosomal instability (CIN) is a hallmark of cancer that results from errors in chromosome segregation during mitosis. Targeting of CIN-associated…”
Get full text

Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid by 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

“…A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and…”
Get full text

Optimization of Potency and Pharmacokinetic Properties of Tetrahydroisoquinoline Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists by Horne, Daniel B, Tamayo, Nuria A, Bartberger, Michael D, Bo, Yunxin, Clarine, Jeffrey, Davis, Carl D, Gore, Vijay K, Kaller, Matthew R, Lehto, Sonya G, Ma, Vu V, Nishimura, Nobuko, Nguyen, Thomas T, Tang, Phi, Wang, Weiya, Youngblood, Beth D, Zhang, Maosheng, Gavva, Narender R, Monenschein, Holger, Norman, Mark H

“…Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous…”
Get full text

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility by Rzasa, Robert M., Frohn, Michael J., Andrews, Kristin L., Chmait, Samer, Chen, Ning, Clarine, Jeffrey G., Davis, Carl, Eastwood, Heather A., Horne, Daniel B., Hu, Essa, Jones, Adrie D., Kaller, Matthew R., Kunz, Roxanne K., Miller, Silke, Monenschein, Holger, Nguyen, Thomas, Pickrell, Alexander J., Porter, Amy, Reichelt, Andreas, Zhao, Xiaoning, Treanor, James J.S., Allen, Jennifer R.

“…[Display omitted] We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors…”
Get full text

Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors by 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

“…We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4…”
Get full text

Stereoselective Synthesis of anti-N-Protected 3-Amino-1,2-epoxides by Nucleophilic Addition to N-tert-Butanesulfinyl Imine of a Glyceraldehyde Synthon by Harried, Scott S, Croghan, Michael D, Kaller, Matthew R, Lopez, Patricia, Zhong, Wenge, Hungate, Randall, Reider, Paul J

“…A di-O-TBS protected glyceraldehyde synthon was condensed with Ellman’s reagent to form a bench-stable N-tert-butanesulfinyl imine 6, which served as a common…”
Get full text

Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors by Wood, Stephen, Wen, Paul H, Zhang, Jianhua, Zhu, Li, Luo, Yi, Babu-Khan, Safura, Chen, Kui, Pham, Roger, Esmay, Joel, Dineen, Thomas A, Kaller, Matthew R, Weiss, Matthew M, Hitchcock, Stephen A, Citron, Martin, Zhong, Wenge, Hickman, Dean, Williamson, Toni

“…Sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-site APP-cleaving enzyme 1 (BACE1) and the γ-secretase complex produces the…”
Get more information

A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase by Kaller, Matthew R, Harried, Scott S, Albrecht, Brian, Amarante, Patricia, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Brown, Ryan, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Graceffa, Russell, Hickman, Dean, Judd, Ted, Kriemen, Chuck, La, Daniel, Li, Vivian, Lopez, Patricia, Luo, Yi, Masse, Craig, Monenschein, Holger, Nguyen, Thomas, Pennington, Lewis D, Miguel, Tisha San, Sickmier, E. Allen, Wahl, Robert C, Weiss, Matthew M, Wen, Paul H, Williamson, Toni, Wood, Stephen, Xue, May, Yang, Bryant, Zhang, Jianhua, Patel, Vinod, Zhong, Wenge, Hitchcock, Stephen

“…β-Secretase inhibitors are potentially disease-modifying treatments for Alzheimer's disease. Previous efforts in our laboratory have resulted in…”
Get full text

Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors by RZASA, Robert M, KALLER, Matthew R, XIAOLING XIONG, WENGE ZHONG, NORMAN, Mark H, GANG LIU, MAGAL, Ella, NGUYEN, Thomas T, OSSLUND, Timothy D, POWERS, David, SANTORA, Vincent J, VISWANADHAN, Vellarkad N, WANG, Hui-Ling

“…Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in the early development of the nervous system. Deregulation of CDK5…”
Get full text

Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors by Kaller, Matthew R., Zhong, Wenge, Henley, Charles, Magal, Ella, Nguyen, Thomas, Powers, David, Rzasa, Robert M., Wang, Weiya, Xiong, Xiaoling, Norman, Mark H.

“…A series of 6-oxo-1,6-dihydropyridines were prepared and found to have potent CDK5 inhibition. Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein…”
Get full text

Design and synthesis of quinolin-2(1 H)-one derivatives as potent CDK5 inhibitors by Zhong, Wenge, Liu, Hu, Kaller, Matthew R., Henley, Charles, Magal, Ella, Nguyen, Thomas, Osslund, Timothy D., Powers, David, Rzasa, Robert M., Wang, Hui-Ling, Wang, Weiya, Xiong, Xiaoling, Zhang, Jiandong, Norman, Mark H.

“…A novel series of quinolin-2(1 H)-one derivatives were synthesized and found to have potent CDK5 inhibitory activities. Cyclin-dependent kinase 5 (CDK5) is a…”
Get full text

Synthesis and conformational analysis of α,α-difluoroalkyl heteroaryl ethers by Horne, Daniel B., Bartberger, Michael D., Kaller, Matthew R., Monenschein, Holger, Zhong, Wenge, Hitchcock, Stephen A.

“…We report the efficient synthesis of difluoroalkyl aryl ethers from the rearrangement of heteroaryl ketones and aldehydes, mediated by xenon difluoride and…”
Get full text

Structure–activity relationships of 3,4-dihydro-1 H-quinazolin-2-one derivatives as potential CDK5 inhibitors by Rzasa, Robert M., Kaller, Matthew R., Liu, Gang, Magal, Ella, Nguyen, Thomas T., Osslund, Timothy D., Powers, David, Santora, Vincent J., Viswanadhan, Vellarkad N., Wang, Hui-Ling, Xiong, Xiaoling, Zhong, Wenge, Norman, Mark H.

“…3,4-Dihydroquinazolin-2(1 H)-one derivatives have been synthesized and evaluated for their inhibition of cyclin-dependent kinase 5. Cyclin-dependent kinase 5…”
Get full text