Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Varie David Lee"'
Autor:
Jens-Christoph Baumann, Nathan D. Ide, Neil G. Stevenson, Didier Schils, Pere Talavera, Jared W. Fennell, Lucie E. Lovelle, David P. Elder, Vincent Antonucci, Michael J. Burns, Dirk Lauwers, Andrew Teasdale, Michael Urquhart, Tetsuji Itoh, Dennie S. Welch, Roland Brown, Rolf Schulte Oestrich, Susanne A. Stalford, Jeffrey M. Kallemeyn, Robert Molzahn, Varie David Lee, Elizabeth M. Covey-Crump, Gregory W. Sluggett, Fabrice Gallou, Guido Jordine, Martin A. Ott, Eric L. Elliott, Looker Adam
Publikováno v:
Organic Process Research & Development. 23:2470-2481
The ICH M7 guidance provides a series of flexible control options for the control of (potentially) mutagenic impurities (PMIs) that fully align with key risk-based principles. This includes option ...
Autor:
Dirk Lauwers, Guido Jordine, David P. Elder, Varie David Lee, Neil G. Stevenson, Mark McLaughlin, Eric L. Elliott, Jens-Christoph Baumann, Barber Christopher Gordon, Nathan D. Ide, Jeffrey M. Kallemeyn, Lucie E. Lovelle, Elizabeth M. Covey-Crump, Andrew Teasdale, Jared W. Fennell, Fabrice Gallou, Looker Adam, Pere Talavera, Martin A. Ott, Didier Schils, Roland Brown, Rolf Schulte Oestrich, Vincent Antonucci, Michael Urquhart, Robert Molzahn, Dennie S. Welch
Publikováno v:
Regulatory toxicology and pharmacology : RTP. 90
The ICH M7 Option 4 control of (potentially) mutagenic impurities is based on the use of scientific principles in lieu of routine analytical testing. This approach can reduce the burden of analytical testing without compromising patient safety, provi
Improved Synthesis of C4α- and C4β-Methyl Analogues of 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylate
Autor:
J. Craig Ruble, James A. Monn, Dana L. T. Laird, Molly D. Brady, Steven S. Henry, Varie David Lee
Publikováno v:
Organic Letters. 14:2662-2665
An efficient and divergent synthesis of C4α- and C4β-methyl-substituted analogues of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate, which are important tools in the study of metabotropic glutamate receptor function, has been achieved. By taking adv
Autor:
Jacob R. Remacle, Amy C. DeBaillie, Christopher P. Ley, Thomas Michael Wilson, Nicholas A. Magnus, Varie David Lee, Perry Clark Heath, Timothy M. Braden, Jonas Y. Buser
Publikováno v:
Organic Process Research & Development. 16:830-835
This article describes the development and optimization of chemical reactions and subsequent multikilogram preparation of the glucokinase activator (R)-1 to fund clinical evaluation as a potential therapeutic for type II diabetes. The major process d
Autor:
Joel P. Bercu, Keith M. DeVries, Courtney M. Callis, David K. Robbins, Varie David Lee, Linda K. Dow
Publikováno v:
Organic Process Research & Development. 14:986-992
Controlling impurities during drug development improves product quality and minimizes safety risks to the patient. Recent regulatory guidance on genotoxic impurities (GTIs) state that identified GTIs are unusually toxic and require lower reporting, i
Publikováno v:
Organic Process Research & Development. 13:285-291
The assessment and control of genotoxic impurities (GTI) in pharmaceutical products has received considerable attention in recent years. Molecular functional groups that render starting materials and synthetic intermediates useful as reactive buildin
Autor:
Moher Eric D, John Allan Rieck, Richard D. Miller, Tracy K. Ditsworth, David A. Hay, Sandra S. K. Borders, Mindy B. Forst, Richard C. Hoying, and Duane A. Pierson, Joseph A. Turpin, Varie David Lee, Ryan J. Linder, Jason S. Cronin, David D. Anderson, and Jacob R. Remacle, Molly D. Brady, Hoard David W, Paul N. Dodson, Christopher A. Beck
Publikováno v:
Organic Process Research & Development. 11:546-559
A pilot-plant scale desymmetrization of the cyclic meso-epoxide 4b, using a chiral lithium amide prepared from symmetrical diamine 17, was designed and implemented to provide allylic alcohol 3b in high yield and greater than 99% ee. This chiral alcoh
Autor:
Thomas H. Corbett, Jian Liang, Rima S. Al-awar, Lisa Polin, David A. Hay, Chuan Shih, James Abraham Aikins, Vasu Vasudevan, Richard E. Moore, Lowell Lee Gibson, Juiwanna Kushner, Kathryn White, James Edward Ray, Michael J. Martinelli, Eric D. Moher, Susan Pugh, Varie David Lee, Tony Y. Zhang, Chiab Simpson, John E. Munroe
Publikováno v:
Investigational New Drugs. 23:213-224
Cryptophycins-1 and 52 (epoxides) were discovered to have in-vitro and in-vivo antitumor activity in the early 1990s. The chlorohydrins of these, Cryptophycins-8 and 55 (also discovered in the early 1990s) were markedly more active, but could not be
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 48:139-148
Partial ergoline agonists such as (R)-4-(dipropylamino)-1,3,4,5-tetrahydrobenz[cd]-indole-6-carboxamide (LY228729, 1a) mimic a locked conformational analog of serotonin and in fact possess potent in vitro activity as agonists of the 5-HT1A receptor.
Autor:
John Brennan, Varie David Lee, Milton J. Zmijewski, John Allan Rieck, David A. Hay, Jason S. Cronin, Barbara Shreve Briggs
Publikováno v:
Tetrahedron Letters. 39:8405-8408
Cryptophycin fragment A ( 1 ) was prepared in high enantiomeric purity in 10 steps from ( R )-carvone. A stereoselective bioreduction of ( R )-carvone to neodihydrocarveol and a regioselective Baeyer-Villiger oxidation of cyclohexanone 8 with pertrif