Zobrazeno 1 - 10
of 135
pro vyhledávání: '"Matthew J. Wyvratt"'
Autor:
Catherine Abbadie, Raul F. Alvaro, Lin-Lin Shiao, Mark Rosenbach, Lisa F. Frey, Marc D. Chioda, Ravi P. Nargund, Richard Hajdu, Kathleen Sullivan, Robert J. DeVita, Joseph F. Leone, Kevin M. Belyk, Jenna L. Terebetski, Amanda K. Makarewicz, Elliot J. Martel, Gino Salituro, Bindhu V. Karanam, Raman K. Bakshi, James Dellureficio, Selena Fung, Ping Liu, Linda Chang, Nina Jochnowitz, Shruti Mistry, Joyce Shuman, Linus S. Lin, Yan Guo, Maria Madeira, Shane W. Krska, Mark McLaughlin, Erin McGowan, Harry R. Chobanian, Jessica Alexander, Matthew J. Wyvratt, Qingmei Hong, Thomas J. Lanza
Publikováno v:
ACS Medicinal Chemistry Letters. 5:717-721
We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal chemistry efforts focused on optimizing of FAAH inhibition in vitro pot
Autor:
Palucki Brenda, Patrick G. Pollard, Liangqin Guo, Tung M. Fong, Matthew J. Wyvratt, Randy R. Miller, Shuwen He, Constantin Tamvakopoulos, Iyassu K. Sebhat, Qianping Peng, Ravi P. Nargund, Zhixiong Ye, Airu S. Chen, Doreen E. Cashen, David H. Weinberg, Min K. Park, Raman K. Bakshi, D. Euan MacIntyre, Howard Y. Chen, Rui Tang, Tanya MacNeil, Qingmei Hong, Alison M. Strack, Ralph A. Stearns, Jian Liu, William J. Martin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2330-2334
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
Autor:
Yingjie Lai, Ralph A. Stearns, Qianping Peng, Ravi P. Nargund, Qingmei Hong, Jian Liu, Rui Tang, Matthew J. Wyvratt, Raman K. Bakshi, Randy R. Miller, Tianying Jian, Alison M. Strack, Tanya MacNeil, Liangqin Guo, Howard Y. Chen, James Dellureficio, Iyassu K. Sebhat, Peter H. Dobbelaar, Airu S. Chen, Constantin Tamvakopoulos, David H. Weinberg, Tung M. Fong, Christopher L. Franklin, Shuwen He, Zhixiong Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4399-4405
We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds c
Autor:
Howard Y. Chen, William J. Martin, D. Euan MacIntyre, Zhixiong Ye, Raman K. Bakshi, Alison M. Strack, Doreen E. Cashen, Jian Liu, Yingjie Lai, Tianying Jian, Constantin Tamvakopoulos, Nancy N. Tsou, Shuwen He, James Dellureficio, Tung M. Fong, Peter H. Dobbelaar, David H. Weinberg, Airu S. Chen, Qingmei Hong, Iyassu K. Sebhat, Tanya MacNeil, Christopher L. Franklin, Ravi P. Nargund, Ralph A. Stearns, Rui Tang, Richard G. Ball, Matthew J. Wyvratt, Randy R. Miller, Liangqin Guo, Qianping Peng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2106-2110
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
Autor:
Marc L. Reitman, Cheng Guo, Theresa M. Kelly, Constantin Tamvakopoulos, Joseph M. Metzger, Tianying Jian, Howard Y. Chen, Arthur A. Patchett, Oksana C. Palyha, Alison M. Strack, Allan J. Goodman, Ravi P. Nargund, Peter H. Dobbelaar, Yanqing Kan, Mark Hadden, Larry Yet, Peter R. Guzzo, Qianping Peng, Linus S. Lin, Shuwen He, Lauren P. Shearman, Alan J. Henderson, Carina P. Tan, Sargent Bruce J, Xiao-Ming Guan, Scott D. Feighner, Iyassu K. Sebhat, Jie Pan, Jian Liu, Donald J. Marsh, Matthew J. Wyvratt, Andrew D. Howard, Megan Ruenz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1913-1917
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rode
Autor:
Dan A. Ostlind, Marlene D. Drag, Matthew J. Wyvratt, Pierre deMontigny, David W. Fink, Steven L. Colletti, Wesley L. Shoop, Michelle B. Ayer, Chunshi Li, Steve Salva, Michelle Zakson, Lynn M. Warmke, Peter T. Meinke, Thomas L. Shih, Dong Ok, Michael H. Fisher, B.F. Michael, Dennis M. Schmatz, Julie Lim
Publikováno v:
Journal of Medicinal Chemistry. 52:3505-3515
Nodulisporic acid A (1) is a structurally complex fungal metabolite that exhibits systemic efficacy against fleas via modulation of an invertebrate specific glutamate-gated ion channel. In order to identify a nodulisporamide suitable for monthly oral
Autor:
Tesfaye Biftu, Dennis M. Schmatz, Penny Sue Leavitt, Paul A. Liberator, Matthew J. Wyvratt, Anne Gurnett, John Mathew, Michael H. Fisher, Donald Thompson, Gilles Ouvry, Andrew Scribner, Chris Brown, Joseph A. Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1517-1521
Novel 2,3-diarylindoles bearing an amine substituent at the indole 5- and 6-positions have been synthesized and evaluated as anticoccidial agents in both in vitro and in vivo assays. Both subnanomolar in vitro activity and broad spectrum in vivo pote
Autor:
Susan Meitz, John Mathew, Penny Sue Leavitt, Anne Gurnett, Donald Thompson, Paul A. Liberator, Michael H. Fisher, Tesfaye Biftu, Dennis M. Schmatz, Andrew Scribner, Matthew J. Wyvratt, Chris Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5263-5267
Novel 5,6-diarylimidazo[2,1-b][1,3]thiazoles bearing an amine substituent at the imidazothiazole 2-position have been synthesized and evaluated as anticoccidial agents in both in vitro and in vivo assays. Both subnanomolar in vitro activity and broad
Autor:
Heather L. Sings, Mark T. Goulet, Matthew J. Wyvratt, Iyassu K. Sebhat, Liangqin Guo, Rui Tang, Ravi P. Nargund, Qianping Peng, Euan Macintyre, Feroze Ujjainwalla, Constantin Tamvakopoulos, Zhixiong Ye, Lex H.T. Van der Ploeg, David H. Weinberg, Tanya MacNeil, John Huber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3242-3247
Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed.
Autor:
Matthew J. Wyvratt, Vivien A. Warren, John P. Felix, Maria L. Garcia, Scott B. Hoyt, William H. Parsons, Kathryn A. Lyons, Xiaohua Li, Michael H. Fisher, Clare London, McHardy M. Smith, Birgit T. Priest, Gregory J. Kaczorowski, Doreen E. Cashen, William J. Martin, D. Euan MacIntyre, Brande S. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1963-1966
A series of 3-amino-1,5-benzodiazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of this series displayed subnanomolar, state-dependent sodium channel block, and