Bryson Rast
Pfizer
24 Papers
222 Citations
Bryson Rast is an academic researcher from Pfizer. The author has contributed to research in topics: Alkyl & Nucleophilic substitution. The author has an hindex of 11, co-authored 24 publications.
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Papers
Patent
Triazolopyridine compounds as pim kinase inhibitors
Shelley Allen,Celeste Laura L,T. Gregg Davis,Robert Kirk Delisle,Julie Marie Greschuk,Stefan Gross,Erik James Hicken,Leila J. Jackson,Joseph P. Lyssikatos,Nicholas C. Kallan,Marmsater Fredrik P,Mark Munson,Pheneger Jed,Bryson Rast,Robinson John E,Stephen T. Schlachter,George T. Topalov,A. Dale Wright,Qian Zhao +18 more
- 18 Aug 2009
TL;DR: In this article, the compounds of Formula (I) are defined as receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.
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5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.
Subas M. Sakya,Kristin M. Lundy DeMello,Martha L. Minich,Bryson Rast,Andrei Shavnya,Robert J. Rafka,David A. Koss,Cheng Hengmiao,Jin Li,Burton H. Jaynes,Ziegler Carl B,Donald W. Mann,Carol F. Petras,Scott B. Seibel,Annette M. Silvia,David M. George,Lisa A. Lund,Suzanne H. St. Denis,Anne Hickman,Michelle L. Haven,Michael P. Lynch +20 more
TL;DR: Structure-activity relationship studies of the novel 2-di and trifluoromethyl-5-alkylamino pyrazo-1-yl derivatives led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats.
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Efficient synthesis of 5-alkyl amino and thioether substituted pyrazoles
Subas M. Sakya,Bryson Rast +1 more
TL;DR: Nucleophilic substitution reactions of 1-(4-methylsulfonyl-2-pyridyl)-5-chloro pyrazoles with various substitutions at the 4 position with amine nucleophiles and thiols occur under mild conditions to provide the 5-alkyl amino and thioether pyrazole in high yields as mentioned in this paper.
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Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Jin Li,Kristin M. Lundy DeMello,Henry Cheng,Subas M. Sakya,Bronk Brian Scott,Robert J. Rafka,Burton H. Jaynes,Ziegler Carl B,Carolyn Rose Kilroy,Donald W. Mann,Eric L. Nimz,Michael P. Lynch,Michelle L. Haven,Nicole L. Kolosko,Martha L. Minich,Chao Li,Jason K. Dutra,Bryson Rast,Rhonda M. Crosson,Morton Barry James,Glen W. Kirk,Kathleen M. Callaghan,David A. Koss,Andrei Shavnya,Lisa A. Lund,Scott B. Seibel,Carol F. Petras,Annette M. Silvia +27 more
TL;DR: The in vitro and in vivo activity of 12a for the canine COX-2 enzyme as well as its in vivo efficacy and pharmacokinetic properties in dog are highlighted.
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5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure–activity relationship studies of 5-alkylethers and 5-thioethers
Subas M. Sakya,Cheng Hengmiao,Kristin M. Lundy DeMello,Andrei Shavnya,Martha L. Minich,Bryson Rast,Jason K. Dutra,Chao Li,Robert J. Rafka,David A. Koss,Jin Li,Burton H. Jaynes,Ziegler Carl B,Donald W. Mann,Carol F. Petras,Scott B. Seibel,Annette M. Silvia,David M. George,Anne Hickman,Michelle L. Haven,Michael P. Lynch +20 more
TL;DR: Structure-activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described, with excellent potency and selectivity and less selective than the ether analogs in a canine whole blood COX-2 assay.
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