Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Catherine Angela Hulford"'
Autor:
Michael St. Pierre, Catherine Angela Hulford, David J. Bernhardson, Brian R. Preston, Benjamin A. Thuma, Peter H. Thompson, John F. Sagal, Kristin E. Price, Thomas Andrew Brandt, Lehner Richard S
Publikováno v:
Organic Process Research & Development. 18:57-65
The development and optimization of a scalable synthesis of sodium-dependent glucose cotransporter 2 inhibitor, ertugliflozin, for the treatment of type-2 diabetes is described. Highlights of the chemistry are a concise, four-step synthesis of a stru
Autor:
David W. Piotrowski, Michael Herr, Liuqing Wei, Matthew F. Sammons, E. Jason Kiser, Sandra M. Jennings, Stephen W. Wright, Catherine Angela Hulford, James F. Hallissey
Publikováno v:
Organic Process Research & Development. 17:934-939
A convergent route to multigram quantities of a mineralocorticoid antagonist 3 is described. Starting from (R)-phenylglycinol, the synthesis of cis 2,5-morpholine 2 is accomplished utilizing a de-e...
Autor:
Xiangyang Chen, E. Jason Kiser, David W. Piotrowski, Robert A. Wade, Cuiman Cai, Matthew F. Sammons, Catherine Angela Hulford, Daniel Merritt Bowles, Sandra M. Jennings, Agustin Casimiro-Garcia, Charles Boos
Publikováno v:
Tetrahedron Letters. 52:7025-7029
The large scale synthesis of functionalized 2-pyridylboronate 8 and optimization of its Suzuki–Miyaura coupling to chloropyrazoline (R)-7 to provide a scalable synthesis of mineralocorticoid antagonist (R)-1 is described.
Autor:
Marvin J. Meyers, Paula M. Loria, Li She, Xiangyang Chen, David W. Piotrowski, Neil Raheja, Agustin Casimiro-Garcia, Kun Song, Catherine M. Ambler, Liuqing Wei, Graciela B. Arhancet, Derek Vrieze, Sandra M. Jennings, Carine M. Boustany-Kari, Catherine Angela Hulford, Rena Eudy, Cuiman Cai, Mary Ellen Banker, David Hepworth, Tereece Banks, Matthew F. Sammons, Donna N. Petersen
Publikováno v:
Journal of medicinal chemistry. 57(10)
A novel series of nonsteroidal mineralocorticoid receptor (MR) antagonists identified as part of our strategy to follow up on the clinical candidate PF-03882845 (2) is reported. Optimization departed from the previously described pyrazoline 3a and fo
Autor:
Matthew F. Dunn, John Charles Kath, Anil Mistry, F. Christopher Bi, Daniel Tyler Richter, Sabrina X. Zhao, Leonard Buckbinder, Jacquelyn Klug-McLeod, Daniel W. Kung, Gary Erik Aspnes, Michael P. Zawistoski, Robert M. Oliver, Seungil Han, Peter C. Bonnette, Ethan Ung, Molly A. McGlynn, Angel Guzman-Perez, Catherine Angela Hulford, Matthew C. Griffor, John R. Soglia, Jonathan N. Bauman, Michael Joseph Luzzio, Daniel P. Walker, Christopher Autry, Amit S. Kalgutkar, W. Gregory Roberts, Jian-Cheng Li, Beth Cooper
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(23)
The synthesis and SAR for a series of diaminopyrimidines as PYK2 inhibitors are described. Using a combination of library and traditional medicinal chemistry techniques, a FAK-selective chemical series was transformed into compounds possessing good P
Autor:
Susan Deborah Lagreca, Daniel Tyler Richter, Kevin Coleman, Matt Wessel, John Charles Kath, Catherine Angela Hulford, Martin A. Berliner, Erika Schmitt, Walter Gregory Roberts, Jing Lin, Matt Griffor, Michael Joseph Luzzio, Eric S. Marr, Pamela Whalen, Christofer Autry, Beth Cooper, Jitesh P. Jani, Earling Emerson, Nandini Chaturbhai Patel, Luis Martinez-Alsina, Lili Yao, Marianne J. Lorenzen, Felix Vajdos, Ethan Ung
Publikováno v:
Cancer research. 68(6)
Cancer cells are characterized by the ability to grow in an anchorage-independent manner. The activity of the nonreceptor tyrosine kinase, focal adhesion kinase (FAK), is thought to contribute to this phenotype. FAK localizes in focal adhesion plaque
Autor:
Lydia C. Pan, Vishwas M. Paralkar, D.T. Crawford, Thomas A. Owen, Thomas A. Brown, Kelly R. Long, Steven L. Smock, John E. Hambor, Mei Li, Peter C. Bonnette, Leonard Buckbinder, John Charles Kath, W. Gregory Roberts, David F. Gebhard, Hollis A. Simmons, Angel Guzman-Perez, Michael Joseph Luzzio, Catherine Angela Hulford, Hua Zhu Ke, Amy P. Baumann, Lisa M. Olson, Hong Qi, William A. Grasser
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America. 104(25)
Bone is accrued and maintained primarily through the coupled actions of bone-forming osteoblasts and bone-resorbing osteoclasts. Cumulative in vitro studies indicated that proline-rich tyrosine kinase 2 (PYK2) is a positive mediator of osteoclast fun
Autor:
Erika S. Roberts, Matt Griffor, Martin A. Berliner, John Charles Kath, Luis Martinez-Alsina, Huiping Xu, Catherine Angela Hulford, Matthew David Wessel, Jing Lin, Lili Yao, Marianne J. Lorenzen, Jitesh P. Jani, Christopher Autry, Pamela Whalen, Vajdos Felix, Nandini Chaturbhai Patel, Daniel Tyler Richter, Ethan Ung, Erling Emerson, Susan Deborah Lagreca, Kevin G. Coleman, Walter Gregory Roberts, Eric S. Marr, Beth C. Vetelino
Publikováno v:
Molecular Cancer Therapeutics. 8:A86-A86
Focal adhesion kinase (FAK) is a non-tyrosine kinase that localizes to focal adhesion plaques. It is activated in response to intergin binding to cellular ligands and when phosphorylated inhibits anoikis allowing for anchorage independent cell growth