Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Andrew, Nolting"'
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:
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, 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:
Andrew Nolting, Daniel Zewge, Jacob M. Janey, Zhiguo J. Song, David M. Tellers, Paul N. Devine, Steven F. Oliver, David M. Tschaen, Dietrich Steinhuebel, Peter G. Dormer
Publikováno v:
Organic Process Research & Development. 18:423-430
A practical synthesis of a macrocyclic HCV protease inhibitor, MK-1220, is described. The key features are a new synthesis of the trisubstituted isoquinoline, Sonogashira fragment coupling, and a high-yielding, 18-membered macrolactam formation.
Autor:
Aaron M. Dumas, Peter E. Maligres, Michael Shevlin, Rebecca T. Ruck, Cheol K. Chung, Ed Cleator, Andrew Nolting, Jacqueline D. Hicks, Guy R. Humphrey, Nelo R. Rivera
Publikováno v:
Organic letters. 18(6)
The development of a convergent and highly stereoselective synthesis of an HCV NS3/4a protease inhibitor possessing a unique spirocyclic and macrocyclic architecture is described. A late-stage spirocyclization strategy both enabled rapid structure–
Autor:
Charles Lee Jayne, Francisco Velazquez, Zhuyan Guo, Donald M. Sperbeck, Murali Rajagopalan, Duane Burnette, Karen Marcantonio, Shouwu Miao, Sathesh Bhat, Santhosh Neelamkavil, Linda Brockunier, Stacia Kargman, Yan Xia, Rebecca T. Ruck, Vincent J. Colandrea, John A. Howe, Nicole Buist, Andrew Nolting, Yongxin Han, Pinto Patrick A, Thomas Bara, Mark Cartwright, Robert Chase, Martin C. Clasby, Srikanth Venkatraman, Randy R. Miller, Keith Eagen, Samuel Chackalamannil, Josien Hubert B, Chad Bennett, Mariappan V. Chelliah, Ian W. Davies, Austin Chen, Shah Unmesh G, Sony Agrawal, Dipshikha Biswas, Jin Wu, Aileen Soriano
Publikováno v:
ACS medicinal chemistry letters. 7(1)
We have been focused on identifying a structurally different next generation inhibitor to MK-5172 (our Ns3/4a protease inhibitor currently under regulatory review), which would achieve superior pangenotypic activity with acceptable safety and pharmac
Autor:
Ian W. Davies, Paul N. Devine, Robert A. Reamer, David M. Tschaen, Fei Zhang, Daniel Zewge, Jeffrey T. Kuethe, David R. Lieberman, Zhihui Peng, Kevin M. Belyk, David M. Tellers, Guy R. Humphrey, Peter G. Dormer, Michel Journet, Andrew Nolting, Marjorie S. Waters, Dalian Zhao, Zhiguo J. Song
Publikováno v:
The Journal of Organic Chemistry. 76:7804-7815
Development of a practical synthesis of MK-7009, a 22-membered macrocycle, is described. A variety of ring-closing strategies were evaluated, including ring-closing metathesis, intermolecular palladium-catalyzed cross-couplings, and macrolactamizatio
Autor:
Edward C. Sherer, Robert K. Orr, Wayne M. Geissler, Kazuto Araki, Thomas Bateman, Ting Zhang, Xiaoxia Qian, Kenneth P. Ellsworth, Teruyuki Nishimura, Andrew Nolting, Patrick Andre, Yi-Heng Chen, Paul Reichert, Kunal Desai, Harold B. Wood, Liangqin Guo, Dann L. Parker, Dongfang Meng, Cameron J. Smith, Lisa M. Sonatore, Tianying Jian, Richard Tschirret-Guth, Alan Hruza, Min Shu, Louis-Charles Campeau, Isao Sakurada
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(21)
Using structure based drug design (SBDD), a novel class of potent coagulation Factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds demonstrated oral bioavailability in rat IV
Autor:
Izzat T. Raheem, Abbas M. Walji, Daniel Klein, John M. Sanders, David A. Powell, Pravien Abeywickrema, Guillaume Barbe, Amrith Bennet, Karla Childers, Melodie Christensen, Sophie−Dorothee Clas, David Dubost, Mark Embrey, Jay Grobler, Michael J. Hafey, Timothy J. Hartingh, Daria J. Hazuda, Jeffrey T. Kuethe, Jamie McCabe Dunn, Michael D. Miller, Keith P. Moore, Andrew Nolting, Natasa Pajkovic, Sangita Patel, Zuihui Peng, Vanessa Rada, Paul Rearden, John D. Schreier, John Sisko, Thomas G. Steele, Jean-François Truchon, John Wai, Min Xu, Paul J. Coleman
Publikováno v:
Journal of Medicinal Chemistry. 59:486-486