Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux
Rzasa, Robert M., Hu, Essa, Rumfelt, Shannon, Chen, Ning, Andrews, Kristin L., Chmait, Samer, Falsey, James R., Zhong, Wenge, Jones, Adrie D., Porter, Amy, Louie, Steven W., Zhao, Xiaoning, Treanor, James J.S., Allen, Jennifer R.
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
Get full text
Journal Article
Discovery of Highly Selective and Potent p38 Inhibitors Based on a Phthalazine Scaffold
Herberich, Brad, Cao, Guo-Qiang, Chakrabarti, Partha P, Falsey, James R, Pettus, Liping, Rzasa, Robert M, Reed, Anthony B, Reichelt, Andreas, Sham, Kelvin, Thaman, Maya, Wurz, Ryan P, Xu, Shimin, Zhang, Dawei, Hsieh, Faye, Lee, Matthew R, Syed, Rashid, Li, Vivian, Grosfeld, David, Plant, Matthew H, Henkle, Bradley, Sherman, Lisa, Middleton, Scot, Wong, Lu Min, Tasker, Andrew S
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
Get full text
Journal Article
Isolation and identification of eukaryotic initiation factor 4A as a molecular target for the marine natural product Pateamine A
Low, Woon-Kai, Dang, Yongjun, Schneider-Poetsch, Tilman, Shi, Zonggao, Choi, Nam Song, Rzasa, Robert M, Shea, Helene A, Li, Shukun, Park, Kaapjoo, Ma, Gil, Romo, Daniel, Liu, Jun O
Published in Methods in enzymology (2007)
Published in Methods in enzymology (2007)
Get more information
Journal Article
Discovery and in Vivo Evaluation of (S)‑N‑(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)‑9H‑purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease
Cushing, Timothy D., Hao, Xiaolin, Shin, Youngsook, Andrews, Kristin, Brown, Matthew, Cardozo, Mario, Chen, Yi, Duquette, Jason, Fisher, Ben, Gonzalez-Lopez de Turiso, Felix, He, Xiao, Henne, Kirk R., Hu, Yi-Ling, Hungate, Randall, Johnson, Michael G., Kelly, Ron C., Lucas, Brian, McCarter, John D., McGee, Lawrence R., Medina, Julio C., San Miguel, Tisha, Mohn, Deanna, Pattaropong, Vatee, Pettus, Liping H., Reichelt, Andreas, Rzasa, Robert M., Seganish, Jennifer, Tasker, Andrew S., Wahl, Robert C., Wannberg, Sharon, Whittington, Douglas A., Whoriskey, John, Yu, Gang, Zalameda, Leeanne, Zhang, Dawei, Metz, Daniela P.
Published in Journal of medicinal chemistry (08.01.2015)
Published in Journal of medicinal chemistry (08.01.2015)
Get full text
Journal Article
Palladium-Catalyzed Chemoselective Monoarylation of Hydrazides for the Synthesis of [1,2,4]Triazolo[4,3-a]pyridines
Reichelt, Andreas, Falsey, James R, Rzasa, Robert M, Thiel, Oliver R, Achmatowicz, Michal M, Larsen, Robert D, Zhang, Dawei
Published in Organic letters (19.02.2010)
Published in Organic letters (19.02.2010)
Get full text
Journal Article
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility
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.
Published in Bioorganic & medicinal chemistry (01.12.2014)
Published in Bioorganic & medicinal chemistry (01.12.2014)
Get full text
Journal Article
Novel Vanilloid Receptor-1 Antagonists: 2. Structure−Activity Relationships of 4-Oxopyrimidines Leading to the Selection of a Clinical Candidate
Doherty, Elizabeth M, Fotsch, Christopher, Bannon, Anthony W, Bo, Yunxin, Chen, Ning, Dominguez, Celia, Falsey, James, Gavva, Narender R, Katon, Jodie, Nixey, Thomas, Ognyanov, Vassil I, Pettus, Liping, Rzasa, Robert M, Stec, Markian, Surapaneni, Sekhar, Tamir, Rami, Zhu, Jiawang, Treanor, James J. S, Norman, Mark H
Published in Journal of medicinal chemistry (26.07.2007)
Published in Journal of medicinal chemistry (26.07.2007)
Get full text
Journal Article
Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer’s disease
Chen, Jian Jeffrey, Qian, Wenyuan, Biswas, Kaustav, Yuan, Chester, Amegadzie, Albert, Liu, Qingyian, Nixey, Thomas, Zhu, Joe, Ncube, Mqhele, Rzasa, Robert M., Chavez, Frank, Chen, Ning, DeMorin, Frenel, Rumfelt, Shannon, Tegley, Christopher M., Allen, Jennifer R., Hitchcock, Stephen, Hungate, Randy, Bartberger, Michael D., Zalameda, Leeanne, Liu, Yichin, McCarter, John D., Zhang, Jianhua, Zhu, Li, Babu-Khan, Safura, Luo, Yi, Bradley, Jodi, Wen, Paul H., Reid, Darren L., Koegler, Frank, Dean, Charles, Hickman, Dean, Correll, Tiffany L., Williamson, Toni, Wood, Stephen
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Get full text
Journal Article
3-Amino-7-phthalazinylbenzoisoxazoles as a Novel Class of Potent, Selective, and Orally Available Inhibitors of p38α Mitogen-Activated Protein Kinase
Pettus, Liping H, Xu, Shimin, Cao, Guo-Qiang, Chakrabarti, Partha P, Rzasa, Robert M, Sham, Kelvin, Wurz, Ryan P, Zhang, Dawei, Middleton, Scott, Henkle, Bradley, Plant, Matthew H, Saris, Christiaan J. M, Sherman, Lisa, Wong, Lu Min, Powers, David A, Tudor, Yanyan, Yu, Violeta, Lee, Matthew R, Syed, Rashid, Hsieh, Faye, Tasker, Andrew S
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
Get full text
Journal Article
Chromenones as potent bradykinin B1 antagonists
Bryan, Marian C., Biswas, Kaustav, Peterkin, Tanya A.N., Rzasa, Robert M., Arik, Leyla, Lehto, Sonya G., Sun, Hong, Hsieh, Feng-Yin, Xu, Cen, Fremeau, Robert T., Allen, Jennifer R.
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Get full text
Journal Article
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors
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
Published in Bioorganic & medicinal chemistry (15.10.2007)
Published in Bioorganic & medicinal chemistry (15.10.2007)
Get full text
Journal Article
Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors
Kaller, Matthew R., Zhong, Wenge, Henley, Charles, Magal, Ella, Nguyen, Thomas, Powers, David, Rzasa, Robert M., Wang, Weiya, Xiong, Xiaoling, Norman, Mark H.
Published in Bioorganic & medicinal chemistry letters (01.12.2009)
Published in Bioorganic & medicinal chemistry letters (01.12.2009)
Get full text
Journal Article
Novel Vanilloid Receptor-1 Antagonists: 1. Conformationally Restricted Analogues of trans-Cinnamides
Norman, Mark H, Zhu, Jiawang, Fotsch, Christopher, Bo, Yunxin, Chen, Ning, Chakrabarti, Partha, Doherty, Elizabeth M, Gavva, Narender R, Nishimura, Nobuko, Nixey, Thomas, Ognyanov, Vassil I, Rzasa, Robert M, Stec, Markian, Surapaneni, Sekhar, Tamir, Rami, Viswanadhan, Vellarkad N, Treanor, James J. S
Published in Journal of medicinal chemistry (26.07.2007)
Published in Journal of medicinal chemistry (26.07.2007)
Get full text
Journal Article
Design and synthesis of quinolin-2(1 H)-one derivatives as potent CDK5 inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (01.10.2007)
Published in Bioorganic & medicinal chemistry letters (01.10.2007)
Get full text
Journal Article
Total Synthesis and Immunosuppressive Activity of (−)-Pateamine A and Related Compounds: Implementation of a β-Lactam-Based Macrocyclization
Romo, Daniel, Rzasa, Robert M, Shea, Helene A, Park, Kaapjoo, Langenhan, Joseph M, Sun, Luo, Akhiezer, Alexander, Liu, Jun O
Published in Journal of the American Chemical Society (02.12.1998)
Published in Journal of the American Chemical Society (02.12.1998)
Get full text
Journal Article
AZETIDINE AND PIPERIDINE COMPOUNDS USEFUL AS PDE10 INHIBITORS
CHEN JIAN J, QIAN WENYUAN, LIU QINGYIAN, FROHN MICHAEL J, ZHONG WENGE, RZASA ROBERT M, KALLER MATTHEW RICHARD, PICKRELL ALEXANDER J, ALLEN JENNIFER R, NGUYEN THOMAS T
Year of Publication 05.03.2015
Get full text
Year of Publication 05.03.2015
Patent
PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
NISHIMURA NOBUKO, LOW JONATHAN D, AMEGADZIE ALBERT, HARRINGTON PAUL E, MA VU VAN, WHITE RYAN, ALLEN JENNIFER R, SMITH ADRIAN L, SHAM KELVIN, XUE QIUFEN, QIAN WENYUAN, RUMFELT SHANNON, FROHN MICHAEL J, GUZMAN PEREZ ANGEL, BROWN JAMES, RZASA ROBERT M, MINATTI ANA ELENA, LOPEZ PATRICIA
Year of Publication 06.11.2015
Get full text
Year of Publication 06.11.2015
Patent
NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS
HARRINGTON ESSA HU, CHEN JIAN J, LIU QINGYIAN, RUMFELT SHANNON, FROHN MICHAEL J, ZHONG WENGE, RZASA ROBERT M, PICKRELL ALEXANDER J, ALLEN JENNIFER R
Year of Publication 19.06.2013
Get full text
Year of Publication 19.06.2013
Patent