Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Robert K. Orr"'
Autor:
Anna Fryszkowska, Chihui An, Oscar Alvizo, Goutami Banerjee, Keith A. Canada, Yang Cao, Duane DeMong, Paul N. Devine, Da Duan, David M. Elgart, Iman Farasat, Donald R. Gauthier, Erin N. Guidry, Xiujuan Jia, Jongrock Kong, Nikki Kruse, Katrina W. Lexa, Alexey A. Makarov, Benjamin F. Mann, Erika M. Milczek, Vesna Mitchell, Jovana Nazor, Claudia Neri, Robert K. Orr, Peter Orth, Eric M. Phillips, James N. Riggins, Wes A. Schafer, Steven M. Silverman, Christopher A. Strulson, Nandhitha Subramanian, Rama Voladri, Hao Yang, Jie Yang, Xiang Yi, Xiyun Zhang, Wendy Zhong
Publikováno v:
Science (New York, N.Y.). 376(6599)
The emergence of new therapeutic modalities requires complementary tools for their efficient syntheses. Availability of methodologies for site-selective modification of biomolecules remains a long-standing challenge, given the inherent complexity and
Autor:
Barbara Pio, Ravi P. Nargund, Yan Guo, Daniel Kosinski, Josien Hubert B, Michael Wright, Michele Pachanski, Harry R. Chobanian, Xiaoping Zhang, Richard Tschirret-Guth, Melissa Kirkland, Andrew D. Howard, Sarah Souza, Eric R. Ashley, Robert K. Orr, Steven L. Colletti, Joel Mane, Jerry Di Salvo, Michael W. Miller, Boonlert Cheewatrakoolpong, Koppara Samuel, William K. Hagmann, James Lamca, Juliann Ehrhart, Maria E. Trujillo, Jackie Shang, Qing Chen, Adam B. Weinglass, Randal M. Bugianesi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1842-1848
GPR40 (FFAR1 or FFA1) is a G protein-coupled receptor, primarily expressed in pancreatic islet β-cells and intestinal enteroendocrine cells. When activated by fatty acids, GPR40 elicits increased insulin secretion from islet β-cells only in the pre
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:938-944
The evolution of a scalable process for the preparation of methylcyclobutanol-pyridyl ether 1 is described. Key aspects of this development including careful control of the stereochemistry, elimination of chromatography, and application to kilogram-s
Autor:
Steven F. Oliver, Eric R. Ashley, Christopher Wise, Robert K. Orr, Eric B. Sirota, Rebecca T. Ruck, Joseph F. Leone, Jamie M. McCabe Dunn, Andrew Nolting, Andrew W. Gibson, Alan M. Hyde, Jon A. Jurica
Publikováno v:
Green Chemistry. 20:2519-2525
Herein we describe the route scouting and process development efforts toward a green and sustainable synthesis of the HCV NS5b cyclic prodrug nucleoside (CPN) 1. Through the discovery and development of a crystallization-induced dynamic resolution an
Autor:
Robert K. Orr, William J. Morris, Cameron J. Cowden, Jian Cui, Jay Milan, Steven P. Miller, Mathew Thomas Maust, Jeffrey Eckert
Publikováno v:
The Journal of Organic Chemistry. 82:2957-2964
The synthesis of the γ-secretase modulator MK-8428 (1) is described. The synthesis is highlighted by an enzyme-catalyzed reaction to access 3,4,5-trifluoro-(S)-phenylglycine, a 1-pot activation/displacement/deprotection sequence to introduce the ami
Autor:
Melissa Kirkland, Randal M. Bugianesi, Melodie Christensen, Maria E. Trujillo, Michele Pachanski, Richard Tschirret-Guth, Josien Hubert B, Adam B. Weinglass, Sarah Souza, Ravi P. Nargund, Christopher W. Plummer, Andrew D. Howard, Joel Mane, Louis-Charles Campeau, Robert K. Orr, Daniel Kosinski, Xiaoping Zhang, Boonlert Cheewatrakoolpong, Jerry Di Salvo, Michael W. Miller, William K. Hagmann, Helen Chen, Steven L. Colletti, Andrew Nolting, Michael Wright, Matthew J. Clements, Murali Rajagopalan
Publikováno v:
ACS Medicinal Chemistry Letters. 8:221-226
GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial agonists elicits insulin secr
Autor:
Robert K. Orr, Jamie M. McCabe Dunn, Edward C. Sherer, Rebecca T. Ruck, Mikhail Reibarkh, Ana Bellomo, Bryon Simmons
Publikováno v:
Chemical Science
The direct and chemoselective 3′-phosphoramidation, phosphorylation and acylation of nucleosides are described.
The direct and chemoselective 3′-phosphoramidation, phosphorylation and acylation of nucleosides are described. Upon the discover
The direct and chemoselective 3′-phosphoramidation, phosphorylation and acylation of nucleosides are described. Upon the discover
Autor:
Robert K. Orr, Harry R. Chobanian, Barbara Pio, Jamie M. McCabe Dunn, Louis-Charles Campeau, Rebecca T. Ruck, Andrew Nolting, Christopher W. Plummer
Publikováno v:
Synthesis. 49:657-666
A convergent three-step method for the synthesis of 2-substituted chromans is described. These results have been accomplished via the Heck coupling of readily accessible allylic alcohols and 2-iodophenols, followed by reduction and Mitsunobu cyclizat
Autor:
Peter E. Maligres, Melodie Christensen, Christopher W. Plummer, Andrew Nolting, Louis-Charles Campeau, Robert K. Orr, Rebecca T. Ruck, Michael Shevlin, Joshua Lee, Matthew T. Tudge, Mark Weisel
Publikováno v:
The Journal of Organic Chemistry. 81:824-830
α- and β-substitution of dihydrocinnamates has been shown to increase the biological activity of various drug candidates. Recently, we identified enantio- and diastereopure α-methyl-β-cyclopropyldihydrocinnamates to be important pharmacophores in
Autor:
Harold B. Wood, Kunal Desai, Daming Feng, Jamie McCabe-Dunn, Yi-Heng Chen, Edward C. Sherer, Jane Y. Wu, Marc Poirier, Hong Li, Dongfang Meng, Ting Zhang, Kenneth P. Ellsworth, Liangqin Guo, Teruyuki Nishimura, Jiayi Xu, Tomokazu Hirabayashi, Sunita V. Dewnani, Patrick Andre, Louis-Charles Campeau, Richard Tschirret-Guth, Isao Sakurada, Paul Reichert, Cameron J. Smith, Robert K. Orr, Lisa M. Sonatore, Wayne M. Geissler, Thomas Bateman, Kazuto Araki, Joe Metzger, Alan Hruza, Richard A. Berger, Dann L. Parker, Tianying Jian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5437-5443
Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds were evaluated in rat IV/PO pharmacokinetic (PK) s