Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Andrei Shavnya"'
Publikováno v:
Organic Letters. 15:6226-6229
A novel palladium-catalyzed sulfination of aryl and heteroaryl halides is described. This reaction operates under mild conditions and provides access to a wide range of aryl and heteroaryl sulfinates, a useful and versatile class of synthetic interme
Autor:
Asaad S. Nematalla, Andrei Shavnya, Kevin B. Bahnck, Susan C. Lilley, Michael John Munchhof, Yong Tao, David R. Bill, Michael Waldo
Publikováno v:
Organic Process Research & Development. 17:1510-1516
A practical large-scale synthesis was developed for 1, a DGAT-1 inhibitor, involving an aza-Michael reaction, amidation, Dieckman cyclization, and conjugate addition of cyanamide followed by cyclization, to form the fused 4-amino-7,8-dihydropyrido[4,
Autor:
Andrei Shavnya, Melissa P. Andrews, David R. Bill, Karki Kapil Kumar, Asaad S. Nematalla, Susan C. Lilley, Kevin B. Bahnck, Mark W. Bundesmann, Leena Patel, Christian Perreault, Tung Le, Gary Erik Aspnes, Michael Waldo, Michael John Munchhof, Mohammed Nihlawi, Robert L. Dow, Qifang Li, David J. Bernhardson, Yong Tao
Publikováno v:
Synthesis. 44:3152-3157
A practical access to an unprecedented, fused bicyclic 4-amino-2-alkoxy-7,8-dihydropyrido[4,3- d ]pyrimidin-5-one scaffold is developed. The synthesis of the potent inhibitor, 2-{4-[4-amino-2-methoxy-5-oxo-7,8-dihydropyrido[4,3- d ]pyrimidin-6(5 H )-
Autor:
Michael Robbins, George T. Tkalcevic, Nandini Chaturbhai Patel, Michael John Munchhof, Andrei Shavnya, Qifang Li, Christopher S. Jones, Susan Deborah Lagreca, Gary Borzillo, Tracey Boyden, Larry A Reiter, Kathleen Pelletier, Luis Martinez-Alsina
Publikováno v:
ACS Medicinal Chemistry Letters. 3:106-111
Inhibitors of the Hedgehog signaling pathway have generated a great deal of interest in the oncology area due to the mounting evidence of their potential to provide promising therapeutic options for patients. Herein, we describe the discovery strateg
Autor:
James P. Driscoll, Eric B. McElroy, Christopher S. Jones, Matthew Frank Brown, Jonathan L. Doty, William H. Brissette, Sharon L. Ripp, Mark J. Mitton-Fry, Marc I. Smeets, Thomas M. Harris, Kristen A. Trevena, Amy S. Antipas, Jeffrey M. Casavant, Laura Cook Blumberg, David A. Reim, Lawrence A. Reiter, Michael John Munchhof, Sandra P. McCurdy, Andrei Shavnya
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4069-4072
5-F substitution of an aminothiazole moiety within a series of thrombopoietin receptor agonists leads to potent agents with an improved hepatic safety profile in rodent toxicology studies.
Autor:
James H. Roache, Eric B. McElroy, Timothy Joseph Paradis, Aikomari Guzman-Martinez, Sara A. Burrell, Robert S. Foti, Matthew Frank Brown, Greg D. Lundquist, Kevin B. Bahnck, James P. Driscoll, Andrei Shavnya, Laurie Tylaska, Ronald P. Gladue, Michael B. Fisher, Poss Christopher Stanley, Molly A. McGlynn, William H. Brissette, Yi Lu, Brett M. Lillie, Laura Cook Blumberg, Flavia Fedeles, Matthew Merrill Hayward, Richard M. Shepard, Kristen A. Trevena, Paul D. Lira
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3109-3112
The synthesis, biological activity, and pharmacokinetic profile of CCR1 antagonists are described.
Autor:
Xinjun Hou, Kristin M. Lundy DeMello, Carol F. Petras, Subas M. Sakya, Cheng Hengmiao, Martha L. Minich, Donald W. Mann, Bryson Rast, Burton H. Jaynes, Michelle L. Haven, Scott B. Seibel, Andrei Shavnya, Jin Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1067-1072
The structure-activity relationship toward canine COX-1 and COX-2 in vitro whole blood activity of 4-hydrogen versus 4-cyano substituted 5-aryl or 5-heteroatom substituted N-phenyl versus N-2-pyridyl sulfone pyrazoles is discussed. The differences be
Autor:
Suzanne H. St. Denis, Michelle L. Haven, Scott B. Seibel, Carol F. Petras, Subas M. Sakya, Lisa A. Lund, Annette M. Silvia, Michael P. Lynch, Bryson Rast, Cheng Hengmiao, Martha L. Minich, Burton H. Jaynes, Kristin M. Lundy DeMello, Donald W. Mann, Andrei Shavnya, Anne Hickman, Ziegler Carl B, David A. Koss, David M. George, Robert J. Rafka, Jin Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:288-292
Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COX enzymes are described. The studies led to the iden
Autor:
Rhonda M. Crosson, David A. Koss, Michelle L. Haven, Carolyn Rose Kilroy, Martha L. Minich, Robert J. Rafka, Eric L. Nimz, Morton Barry James, Scott B. Seibel, Lisa A. Lund, Carol F. Petras, Kristin M. Lundy DeMello, Chao Li, Annette M. Silvia, Bryson Rast, Kathleen M. Callaghan, Andrei Shavnya, Michael P. Lynch, Subas M. Sakya, Ziegler Carl B, Jin Li, Nicole L. Kolosko, Bronk Brian Scott, Donald W. Mann, Jason K. Dutra, Burton H. Jaynes, Henry Cheng, Glen W. Kirk
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:95-98
Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to the identification of 12a as a lead candidate for further progre
Autor:
Andrei Shavnya, Christian Perreault, Benjamin N. Rocke, Michael Herr, Vincent Mascitti, Jana Polivkova, Kevin B. Bahnck, Sophie Y. Lavergne
Publikováno v:
ChemInform. 45
Organozinc reagents react with the SO2 surrogate DABSO, and the resulting zinc sulfinate salts are alkylated in situ to afford sulfones. This transformation has a broad scope and is compatible with a wide range of structural motifs of medicinal chemi