Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Istvan Kaldor"'
Autor:
Matthew Jude Sharp, Will L. Canoy, Kae M. Bullock, Eric Eugene Boros, Xiao-ming M. Zhou, Richard T. Matsuoka, Greg A. Erickson, Vassil I. Elitzin, Mark B. Mitchell, Matthew C. Salmon, David H. Igo, Nicole M. Deschamps, Daniel W. Reynolds, Andrew D. Brown, Gregory E. Peckham, Istvan Kaldor, Jennifer F. Toczko, Shannon Condon, Carpenter Andrew J, Elie Amine Tabet, Jing M. Fang, Biren K. Joshi, Lianming Michael Wu, Jeremy D. Cobb
Publikováno v:
Organic Process Research & Development. 20:1469-1475
Practical and scalable syntheses were developed that were used to prepare multikilogram batches of GSK1292263A (1) and GSK2041706A (15), two potent G protein-coupled receptor 119 (GPR119) agonists. Both syntheses employed relatively cheap and readily
Autor:
Eric E. Boros, Istvan Kaldor
Publikováno v:
Journal of Heterocyclic Chemistry. 52:302-305
3-Bromothieno[3,2-c]pyridine-4-(5H)-one (1) was prepared from (2E)-3-(4-bromo-2-thienyl)-2-propenoic acid (3) by the Eloy–Deryckere thermal benzo/heteropyridinone synthesis. A telescoped procedure was developed, which reduces some of the risk assoc
Publikováno v:
Journal of Heterocyclic Chemistry. 50:863-867
An imidazolidinone intermediate (3) used in the synthesis of novel HIV-entry inhibitors was prepared on multihundred gram scales in four steps and 40% overall yield. The penultimate step in the synthesis involved regioselective N-cyclization of N-(2-
Autor:
Eric E. Boros, Robert L. Dobbins, Maggie S. McIntyre, Ryan Klein, David J. Cowan, Xi Liang, Xiaozhou Yao, Andrew A. Young, Kristin M. Patterson, Paul L. Feldman, John Ray, Christine L. Merrill, Lindsey T. Harston, Jeff L. Ambroso, Jon L. Collins, Shane Roller, Michael J. Bishop, Judith S. Prescott, Christopher Joseph Aquino, Alan Cunningham, Don L. Anderson, Istvan Kaldor, Wu Yulin, Lihong Chen, Josephine Yuen
Publikováno v:
Journal of Medicinal Chemistry. 56:5094-5114
The apical sodium-dependent bile acid transporter (ASBT) transports bile salts from the lumen of the gastrointestinal (GI) tract to the liver via the portal vein. Multiple pharmaceutical companies have exploited the physiological link between ASBT an
Publikováno v:
Journal of Heterocyclic Chemistry. 48:733-736
2-Methyl-4-(trifluoromethyl)-1H-indole-5-carbonitrile is a key intermediate in the synthesis of selective androgen receptor modulators discovered in these laboratories. A practical and convergent synthesis of the title compound starting from 4-nitro-
Autor:
Lihong Chen, Jonathan Y. Bass, David N. Deaton, Aaron B. Miller, Justin A. Caravella, Istvan Kaldor, Robert B. McFadyen, Stacey A. Jones, Dan Todd, Paul Kenneth Spearing, Kevin P. Madauss, Adwoa Akwabi-Ameyaw, Derek J. Parks, Richard Dana Caldwell, Frank Navas, Yaping Liu, Katrina L. Creech, G. Bruce Wisely, Harry B. Marr, Shawn P. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4339-4343
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the se
Autor:
Christie Schulte, Curt D. Haffner, J. Chuck Poole, Eric E. Boros, John C. Ulrich, David J. Cowan, Tiffany Carpenter, Eugene L. Stewart, J. Darren Stuart, Frank Preugschat, David N. Deaton, Tara Renae Rheault, Todd W. Shearer, Barry G. Shearer, J. David Becherer, Michael R. Jeune, Istvan Kaldor, Lisa M. Shewchuk, Terrence L. Smalley
Publikováno v:
Journal of medicinal chemistry. 58(17)
Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure-activity relationships (SAR) of the 4-, 6-, and 8-substituents of the quinoline ring resulted in the identification of ap
Autor:
Eric E. Boros, Istvan Kaldor
Publikováno v:
ChemInform. 46
The title compound (III) is synthesized from thienylpropenoic acid (I) by the Eloy—Deryckere thermal benzo/heteropyridone synthesis.
Autor:
John C. Ulrich, Petrov Kimberly, Tiffany Carpenter, David J. Cowan, J. Darren Stuart, J. David Becherer, Eugene L. Stewart, Frank Preugschat, David N. Deaton, W. Wallace Harrington, Yu Guo, Naphtali Milliken, Barry G. Shearer, Michael R. Jeune, Istvan Kaldor, Terrence L. Smalley, Curt D. Haffner, Brad R. Henke, Rodolfo Cadilla, Todd W. Shearer, Eric E. Boros, Christie Schulte
Publikováno v:
Journal of medicinal chemistry. 58(8)
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in
Autor:
Istvan Kaldor, Ronald George Sherrill, Furfine Eric Steven, David J. Reynolds, John F. Miller, Richard J. Hazen, Michael Stephen Brieger, Andrew Spaltenstein
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3496-3500
A novel series of tyrosine-derived HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and two protease inhibitor-resistant viruses. All of the compounds had wild-type antiviral activities tha