Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Mark E. Webster"'
Autor:
Brian P. Jones, Barbara J. Sitter, Ruchi Mehta, Anil Rane, Chad A. Lewis, Jacob C. DeForest, Elizabeth Greenberg, Nga M. Do, Emma McInturff, Bao D. Nguyen, Kris N. Jones, Michael J. Karmilowicz, Mark E. Webster, Howard W. Ward, Brian Samas, Sarah H. Griffin, Rajesh Kumar, Phil Dietrich, Christina G. Connor, Kevin M. Doyle, J. Christopher McWilliams, Shane A. Eisenbeis
Publikováno v:
Organic Process Research & Development. 25:608-615
The development of a commercial route toward the JAK1 inhibitor abrocitinib is described. The application of a late-stage Lossen rearrangement provided the desired cis-diaminocyclobutane, which was...
Autor:
R. Matt Weekly, Zhihui Peng, Hahdi H. Perfect, Teresa W. Makowski, Jade D. Nelson, Eric C. Hansen, Michele T. Drexler, David Place, Pascal Dube, Mark Olivier, Paul Bowles, Jason Mustakis, Nga M. Do, Stephane Caron, John J. Salisbury, John A. Ragan, Kris N. Jones, Tomislav A. Ljubicic, Shengquan Duan, Corey L. Stanchina, Brian P. Jones, Steven J. Brenek, Brian C. Vanderplas, Mark E. Webster
Publikováno v:
Organic Process Research & Development. 18:66-81
A practical synthesis of SGLT2 inhibitor candidate ertugliflozin (1) has been developed for potential commercial application. The highly telescoped process involves only three intermediate isolations over a 12-step sequence. The dioxa-bicyclo[3.2.1]o
Autor:
Michael J. Janusz, R.L. Walter, John C. VanRens, Biswanath De, Lily C. Hsieh, Jane Far-Jine Djung, Cynthia Monesa Clark, Steven K. Laughlin, Marlene Mekel, Mark Sabat, Matthew J. Laufersweiler, Todd A. Brugel, Townes Jennifer Anne, Adam Golebiowski, Roger G. Bookland, Mark E. Webster, Michael P. Clark
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2285-2289
4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production. One of the compounds (6e
Autor:
Farr Robert A, Edward W. Huber, Ramnik S. Shah, Richard A. Schnettler, Christian T. Goralski, Mark E. Webster, C. Richard Nevill, Bruce Baron, Timothy James-Norman Watson, Phillip L. Nyce, and Cynthia L. Rand, Boyd L. Harrison, Rajesh K. Mishra, Stephen W. Horgan, Franz J. Weiberth
Publikováno v:
Organic Process Research & Development. 4:477-487
MDL 103371 is a N-methyl-d-aspartate (NMDA)-type glycine receptor antagonist for the potential treatment of stroke. Evaluation of five different synthetic routes, which included Stille, Suzuki, enol ether, Knoevenagel, and the Mukaiyama coupling reac
Autor:
Neal J. Fetner, Robert J. Cregge, Mark E. Webster, and Mark A. Nitz, Michael A. DesJardin, David W. Freund, David W. Burkhouse, Hoops John F, Richard E. Donaldson, Robert C. Clouse, Stephen W. Horgan, Gerald P. Heinrich, Daniel R. Henton, J. Russell McConnell, Robert T. Keaten, Christian T. Goralski, Kathy P. Barton, Michael E. LeTourneau, and Alexey Margolin, Sandra K. Stolz-Dunn
Publikováno v:
Organic Process Research & Development. 3:241-247
MDL 28,726 is a key intermediate in the synthesis of the ACE inhibitors MDL 27,210A and MDL 100,240. An efficient nine-step synthesis of this tricyclic acid, which has three chiral centers, was developed beginning with 3,4-dihydro-2H-pyran. A key ste
Autor:
Ramnik S. Shah, and David L. Wenstrup, Timothy T. Curran, Timothy Watson, Mark E. Webster, David A. Hay
Publikováno v:
Organic Process Research & Development. 2:357-365
An efficient synthesis of (1S,4R)-(−)-4-tert-butyldimethylsilyloxy-2-cyclopentenyl acetate and (1R,4S)-(−)-4-tert-butyldimethylsilyloxy-2-cyclopentenol is described utilizing a furfuryl alcohol rearrangement, followed by a lithium aluminum hydrid
Autor:
Julie L. Geary, Melinda A. Correll, J. Chuck Poole, Xiao-Gao Liu, Larry D. Bratton, Fred E. Boyer, Thomas N. Thompson, Teng-Man Chen, Arun K. Mandagere, Bryan K. Jones, Kin-Kai Hwang, Mark E. Webster, Robert W. Knippenberg, Maynard George D, Stephen W. Horgan, Deborah E. Logan, Tieu-Binh Le, Kudlacz Elizabeth M, David L. Wenstrup, Burkholder Timothy P, Raymond S. Gross, David W. Freund
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2531-2536
We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors.1 Here we report the synthesis and structure-activity relationships for a series of analogs of M
Autor:
Tieu-Binh Le, S. A. Shatzer, Burkholder Timothy P, Maynard George D, Stephen W. Horgan, Kudlacz Elizabeth M, Robert W. Knippenberg, Mark E. Webster
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:951-956
We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 (IC50=3.11 nM) and NK2 (IC50=8.40 nM) receptors. The chemical synthesis of MDL 105,212 and the SAR of a series of racemi
Autor:
S. A. Shatzer, Burkholder Timothy P, Robert W. Knippenberg, Tieu-Binh Le, Maynard George D, Mark E. Webster, Stephen W. Horgan, Kudlacz Elizabeth M
Publikováno v:
ChemInform. 27
We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 (IC50=3.11 nM) and NK2 (IC50=8.40 nM) receptors. The chemical synthesis of MDL 105,212 and the SAR of a series of racemi
Autor:
Ramnik S. Shah, Mark E. Webster, Timothy T. Curran, David A. Hay, Timothy J. N. Watson, David L. Wenstrup
Publikováno v:
ChemInform. 30