Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Jonathan L. Doty"'
Autor:
Brett M. Lillie, Matthew Frank Brown, Bret D. Perry, Mark Edward Flanagan, Chakrapani Subramanyam, Kudlacz Elizabeth M, Jianmin Sun, Michael B. Fisher, Todd Andrew Blumenkopf, Chang Shang-Poa, Perry S. Sawyer, Timothy J. Strelevitz, Sandra P. McCurdy, William H. Brissette, Craig R. Kent, Paul S. Changelian, Jonathan L. Doty, Michael John Munchhof, David A Whipple, Jeffrey M. Casavant, Michael Hines, Kelly S. Magnuson, Eileen A. Elliott
Publikováno v:
Journal of Medicinal Chemistry. 53:8468-8484
There is a critical need for safer and more convenient treatments for organ transplant rejection and autoimmune disorders such as rheumatoid arthritis. Janus tyrosine kinases (JAK1, JAK3) are expressed in lymphoid cells and are involved in the signal
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:
John A. Ragan, Paul D. Hill, Y. Lu, Ruth E. McDermott, Jonathan L. Doty, Beth Cooper, Matthew A. Marx, Brian P. Jones, Raggon Jeffrey W, Michael John Munchhof, Jeffrey M. Casavant
Publikováno v:
Organic Process Research & Development. 7:676-683
The multihundred-gram synthesis of [2-(3-methyl-3H-imidazol-4-yl)-thieno[3,2-b]pyridin-7-yl]-(2-methyl-1H-indol-5-yl)-amine (1) is described utilizing a Stille cross-coupling of an iodothienopyridine (3) with 5-(tributylstannyl)-1-methylimidazole (11
Development of a Scaleable Route for the Production of cis-N-Benzyl-3-methylamino-4-methylpiperidine
Autor:
Wilcox Glenn Ernest, Weiling Cai, Mark Edward Flanagan, Stefan Abele, Jeffrey M. Casavant, Mike Munchhoff, David H. Brown Ripin, Ton Vries, David A. Whipple, Kees Pouwer, Cliff Meltz, Jianmin Sun, Keith E. McCarthy, Klaus Laue, John J. Teixeira, Christian Koecher, Jonathan L. Doty, Bharat Kiritkumar Shah, Todd Andrew Blumenkopf
Publikováno v:
Organic Process Research & Development. 7:115-120
The synthesis of cis-N-benzyl-3-methylamino-4-methylpiperidine (5) via hydroboration of tetrahydropyridine 3 followed by oxidation and reductive amination was optimized and scaled up to produce 10-kg quantities of product. Three routes to 3 were iden
Autor:
Lilli Ann Wolf-Gouveia, Paul D. Lira, Eric B. McElroy, Lisa Marie Thomasco, Matthew Frank Brown, Christopher S. Jones, Jonathan L. Doty, Lawrence A. Reiter, Sandra P. McCurdy, Anthony Marfat, Sharon L. Ripp, Mark J. Mitton-Fry, William H. Brissette, Andrei Shavnya, Linde Robert Gerald, Thomas M. Harris, Kristen A. Trevena, Qifang Li, Laura Cook Blumberg, Amy S. Antipas, James P. Driscoll, Michael John Munchhof, Jeffrey M. Casavant
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1428-1430
Recently, we disclosed a series of potent pyrimidine benzamide-based thrombopoietin receptor agonists. Unfortunately, the structural features required for the desired activity conferred physicochemical properties that were not favorable for the devel
Autor:
David G. Perregaux, Perry S. Sawyer, Mark Edward Flanagan, Michael John Munchhof, Kelly S. Magnuson, Jonathan L. Doty, Craig R. Kent, Paul S. Changelian, Thomas M. Harris, Jianmin Sun, David A. Whipple, Cyrille Kuhn, Kudlacz Elizabeth M, Deborah J. Moshinsky
Publikováno v:
Blood. 111:2155-2157
PF-956980 is a selective inhibitor of JAK3, related in structure to CP-690550, a compound being evaluated in clinical trials for rheumatoid arthritis and prevention of allograft rejection. PF-956980 has been evaluated against a panel of 30 kinases, a
Autor:
Matthew David Doroski, Joel T. Arcari, Mark S. Plummer, Andrea Marra, Thomas M. Harris, Justin I. Montgomery, Usa Reilly, Carol A. Menard, Michael D. Huband, Anthony Marfat, Jinshan Michael Chen, Christy Thoma, Karen L. Leach, John P. O'Donnell, Seung Won Chung, Loren M. Price, Joseph A. Abramite, Charlene R. Desbonnet, Eric B. McElroy, Veerabahu Shanmugasundaram, Michael Melnick, Shenping Liu, Matthew Frank Brown, Mark C. Noe, Joseph S. Warmus, Juntyma J. Engtrakul, Daniel P. Uccello, Donn G. Wishka, Robert M. Oliver, Rose Barham, Joseph Penzien, Jonathan L. Doty, John D. Knafels, Ye Che, Lisa Mullins, Elizabeth M. Collantes
Publikováno v:
Journal of medicinal chemistry. 55(2)
In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid 1a.
Autor:
Diana Sperger, Laura Cook Blumberg, Emilio J. Mangual, Kristen A. Trevena, Christopher S. Jones, Jonathan L. Doty, Fangning Zhang, William H. Brissette, Marc I. Smeets, Qifang Li, Paul D. Lira, Amy S. Antipas, Lilli Ann Wolf-Gouveia, Sandra P. McCurdy, Lisa Marie Thomasco, Andrei Shavnya, Sharon L. Ripp, Richard M. Shepard, Liling Zhang, Chakrapani Subramanyam, Linde Robert Gerald, Michael John Munchhof, Lawrence A. Reiter, James P. Driscoll
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(19)
A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation a
Autor:
Elisabeth Knauth, Matthew A. Marx, Michael John Munchhof, Beth Cooper, Catherine Soderstrom, Jianmin Sun, R.Carla Higdon, Ann Marie Rossi, Jean S. Beebe, Stephen M. Hillerman, Susan B. Sobolov, Jeffery M. Casavant, Jonathan L. Doty
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(1)
Novel classes of thienopyrimidines and thienopyridines have been identified as potent inhibitors of VEGFR-2 kinase. The synthesis and SAR of these compounds is presented, along with successful efforts to diminish EGFR activity present in the lead ser
Publikováno v:
Tetrahedron Letters. 34:961-962
N-Cbz or N-Boc protected 3,6-dihydro-1,2-oxazines 1 on treatment with LDA at −78°C undergo a novel rearrangement to provide synthetically useful N-Cbz or N-Boc protected dihydro-2-furanylamines 2.