Zobrazeno 1 - 10
of 61
pro vyhledávání: '"Gregory A. Stephenson"'
Publikováno v:
Journal of Pharmaceutical Sciences. 108:476-484
Our goals were to evaluate the effects of (i) hydrostatic pressure alone and (ii) its combined effect with shear stress during compaction, on the polymorphic transformation (form C → A) of a model drug, chlorpropamide. The powder was either subject
Publikováno v:
Crystal Growth & Design. 16:737-748
High energy solids, such as salts, co-crystals, or amorphous solid dispersions, have been widely used to generate supersaturated aqueous solutions and improve drug bioavailability. However, most research on solubility enhancing strategies has focused
Publikováno v:
Molecular Pharmaceutics. 12:3766-3775
Crystallization of trehalose dihydrate (C12H22O11·2H2O) was induced by storing tablets of amorphous anhydrous trehalose (C12H22O11) at 65% RH (RT). Our goal was to evaluate the advantages and limitations of two approaches of profiling spatial distri
Autor:
Jeffrey Thomas Vicenzi, Paul A. Stroud, Gregory A. Rener, Gregory A. Stephenson, Marie Kissane, Scott Alan Frank, Radhe K. Vaid, Sathish K. Boini, Charles A. Alt, Laura A. McKee, Christopher P. Ley
Publikováno v:
Tetrahedron Letters. 54:6587-6591
The identification and development of an aldehyde–bisulfite adduct as an isolable starting material in the synthesis of the CETP inhibitor Evacetrapib are described. The physical properties of the sodium and potassium analogs are compared, and the
Autor:
Reinhard Matthew Robert, James A. Monn, Bryan G. Johnson, Xushan Wang, Matthew John Valli, Beverly A. Heinz, Mark G. Bures, Steven S. Henry, Brian G. Getman, Joan H. Carter, John T. Catlow, Junliang Hao, David L. McKinzie, Steven Marc Massey, Marc Herin, Steven Swanson, Gregory A. Stephenson
Publikováno v:
Journal of Medicinal Chemistry. 56:4442-4455
As part of our ongoing interest in identifying novel agonists acting at metabotropic glutamate (mGlu) 2/3 receptors, we have explored the effect of structural modifications of 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate (LY354740), a po
Autor:
Gregory A. Stephenson, Bret A. Astleford, Dana L. T. Laird, John R. Rizzo, Adam D. McFarland, Todd D. Maloney, Nicholas A. Magnus, J. Craig Ruble, James P. Wepsiec
Publikováno v:
The Journal of Organic Chemistry. 78:5768-5774
Serotonin norepinephrine reuptake inhibitor (SNRI) pyrrolidinyl ether 2 was synthesized by employing a dynamic kinetic resolution (DKR) with enantio- and diastereoselective hydogenation on β-keto-γ-lactam 8 to afford β-hydroxy-γ-lactam 9 with 96%
Autor:
Gustavo Pascual, Smriti Iyengar, Gregory A. Stephenson, Laura J. Martin, Sandra Ann Filla, Craig E. Thomas, Susan K. Hemrick-Luecke, Kirk W. Johnson, Jikesh Arvind Shah, Eric George Tromiczak, Magnus Wilhelm Walter, Karsten Fynboe, Lance Allen Pfeifer, Mark A. Muhlhauser, Juan A. Rincón, Nicolas Dreyfus, Chunjin Ding, Jia Shaojuan, María Luz de la Puente, Beverly A. Heinz, Lee A. Phebus, Michael P. Johnson, Simon James Richards, Thomas J. Perun, Michael J. McCoy, Pilar Lopez, Hamideh Zarrinmayeh, Thierry Masquelin, Rosa Maria A. Simmons, Douglas Linn Gernert, Oscar de Frutos, Elizabeth M. Joshi, Denise Morrow, Wayne W. Weber, Anette M. Johansson, Linda K. Thompson, Eric P. Seest, Valentina O. Badescu, Javier Mendiola, Jason K. Myers, Patrick L. Love
Publikováno v:
ACS Medicinal Chemistry Letters. 4:560-564
The objective of the described research effort was to identify a novel serotonin and norepinephrine reuptake inhibitor (SNRI) with improved norepinephrine transporter activity and acceptable metabolic stability and exhibiting minimal drug-drug intera
Publikováno v:
Crystal Growth & Design. 13:581-589
Crystal structure prediction methods have been used to explore the potential energy landscape for crystals of a melatonin agonist (MA). All known experimental polymorphs were found in the search for crystal packing alternatives with a single molecule
Autor:
Diseroad Benjamin Alan, Raj Suryanarayanan, Gregory A. Stephenson, Naveen K. Thakral, Aktham Aburub, Timothy Andrew Woods, Jeffrey A. Peterson, Robert J. Behme
Publikováno v:
Molecular pharmaceutics. 13(12)
Disproportionation propensity of salts (HCl, HBr, heminapadisylate) and adipic acid cocrystal of corticotropin releasing hormone receptor-1 antagonist was studied using model free kinetics. Using thermogravimetic weight loss profile or heat flow curv
Autor:
Hong Yu, Sean P. Hollinshead, Anne B. Need, Akihiko Kato, Daniel Ray Mayhugh, Diseroad Benjamin Alan, Paul L. Ornstein, Jon K. Reel, Patrick Gianpietro Spinazze, Jeff Schkeryantz, David S. Bredt, Oscar de Frutos, Beverly A. Heinz, Kevin Matthew Gardinier, Debra Luffer-Atlas, F. Craig Stevens, Vanessa N. Barth, Warren J. Porter, Timothy Andrew Woods, Douglas Linn Gernert, Gregory A. Stephenson, Jeffrey M. Witkin, Kevin D. Burris, Prashant V. Desai, Patric James Hahn, Scott D. Gleason, Steven Swanson, Chunjin Ding, Albert Khilevich
Publikováno v:
Journal of medicinal chemistry. 59(10)
Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is one member of this family and is highly expressed within the hippocampus relative to the c