Zobrazeno 1 - 10
of 24
pro vyhledávání: '"John F. Mehlmann"'
Autor:
Pamela A. Haile, Linda N. Casillas, Bartholomew J. Votta, Gren Z. Wang, Adam K. Charnley, Xiaoyang Dong, Michael J. Bury, Joseph J. Romano, John F. Mehlmann, Bryan W. King, Karl F. Erhard, Charles R. Hanning, David B. Lipshutz, Biva M. Desai, Carol A. Capriotti, Michelle C. Schaeffer, Scott B. Berger, Mukesh K. Mahajan, Michael A. Reilly, Rakesh Nagilla, Elizabeth J. Rivera, Helen H. Sun, John K. Kenna, Allison M. Beal, Michael T. Ouellette, Mike Kelly, Gillian Stemp, Máire A. Convery, Anna Vossenkämper, Thomas T. MacDonald, Peter J. Gough, John Bertin, Robert W. Marquis
Publikováno v:
Journal of Medicinal Chemistry. 62:6482-6494
Autor:
Arthur Shu, Yiqian Lian, Huijie Li, Curt Dale Haffner, Terry Vincent Hughes, Ami S. Lakdawala, Julie A. Cox, Pamela A. Haile, Constantine Kreatsoulas, Beth Anne Knapp-Reed, Lisa M. Shewchuk, David B. Lipshutz, John F. Mehlmann, Michael T. Ouellette, Christopher J Aquino, Mark Elban, Nicole Cathleen Goodwin, Huiqiang Zhou, Adam Kenneth Charnley, Bartholomew J. Votta, Robert W. Marquis, Joseph J. Romano, Linda N. Casillas, Peter J. Gough, Máire A. Convery, John Bertin
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we report the discovery of pyrazolocarboxamides as novel, potent, and kinase selective inhibitors of receptor interacting protein 2 kinase (RIP2). Fragment based screening and design principles led to the identification of th
Autor:
Elizabeth J. Rivera, Brian Donovan, Ami S. Lakdawala, Nikolay V. Plotnikov, Xiaoyang Dong, Barry S. Brown, Robert Singhaus, Khuram W. Chaudhary, Rachel D. Totoritis, Adam Kenneth Charnley, Michael Reilly, Terry Vincent Hughes, Joseph J. Romano, Pamela A. Haile, Robert W. Marquis, Michael Jonathan Bury, John F. Mehlmann, Gren Z. Wang, Rakesh Nagilla, Bartholomew J. Votta, Barbara A. Swift, Linda N. Casillas, Demartino Michael P, Peter J. Gough, Mukesh K. Mahajan, Carol A. Capriotti, Biva M. Desai, Scott B. Berger, Carol LePage, Helen H. Sun, David B. Lipshutz, John Bertin, Máire A. Convery, Chaya Duraiswami, Michael T. Ouellette
Publikováno v:
ACS Medicinal Chemistry Letters. 11:1353-1353
Autor:
Rachel D. Totoritis, Robert Singhaus, Brian Donovan, Nikolay V. Plotnikov, John F. Mehlmann, Terry Vincent Hughes, Michael Jonathan Bury, Pamela A. Haile, Khuram W. Chaudhary, Gren Z. Wang, Peter J. Gough, Biva M. Desai, Michael T. Ouellette, Michael Reilly, Mukesh K. Mahajan, Barry S. Brown, Scott B. Berger, Xiaoyang Dong, Carol A. Capriotti, Carol LePage, Bartholomew J. Votta, Helen H. Sun, David B. Lipshutz, John Bertin, Joseph J. Romano, Adam Kenneth Charnley, Ami S. Lakdawala, Robert W. Marquis, Barbara A. Swift, Rakesh Nagilla, Máire A. Convery, Demartino Michael P, Elizabeth J. Rivera, Linda N. Casillas
Publikováno v:
ACS Med Chem Lett
[Image: see text] RIP2 kinase was recently identified as a therapeutic target for a variety of autoimmune diseases. We have reported previously a selective 4-aminoquinoline-based RIP2 inhibitor GSK583 and demonstrated its effectiveness in blocking do
Autor:
Joseph J. Romano, Jean-Luc Tran, Shu-Yun Zhang, Amaya I. Wolf, Liping Wang, H. Christian Eberl, Michael Klein, Marcus Bantscheff, Kelvin Nurse, Adam Kenneth Charnley, Ramanjulu Joshi M, Jessica L. Schneck, Stephanie Lehmann, Jim Clemens, Axel Hoos, Michael Adam, Christopher B. Hopson, Todd L. Graybill, Jeffrey Guss, Jerry L. Adams, John F. Mehlmann, Jingsong Yang, Robert Singhaus, Michael Reilly, Ana C. Puhl, Robert W. Marquis, Li Yue, John Bertin, Patrick Moore, Angel Morales, James F. Smothers, Kevin J. Duffy, Viera Kasparcova, Peter J. Gough, Giovanna Bergamini, Kevin Foley, Kamelia Behnia, Lara Kathryn Leister, Marcel Muelbaier, G. Scott Pesiridis, Neysa Nevins, James Kang, Yiqian Lian, Guosen Ye, Nestor O. Concha
Publikováno v:
Nature. 570:E53-E53
Change history: In this Letter, author Ana Puhl was inadvertently omitted; this error has been corrected online.An amendment to this paper has been published and can be accessed via a link at the top of the paper.
Autor:
Charles William Mann, Lloyd M. Garrick, Matthew D. Vera, Linda Shanno, Jeffrey C. Pelletier, John F. Rogers, Diane B. Hauze, Jay E. Wrobel, Daniel M. Green, Irene Feingold, Murty Chengalvala, John F. Mehlmann, Joseph T. Lundquist, Joshua E. Cottom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2512-2515
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has resulted in positive clinical results in reproductive tissue disorders such as endometriosis and prostate cancer. Following the recent discovery of orally active GnRH antagonists ba
Autor:
Diane B. Hauze, Michael C. Sharp, Bheem M. Bhat, Paula Green, Colleen Milligan, Daniel M. Green, Jennifer Pirrello, Peter V.N. Bodine, Ronald L. Magolda, Adam M. Gilbert, Matthew D. Vera, Yogendra P. Kharode, Valerie E. Coleburn, Luciana De Araujo Felix, Mattew G. Bursavich, Nipa Alon, Jeanne J. Matteo, Jay Wrobel, Frederick J. Bex, Jeffrey C. Pelletier, Susan Lockhead, Joseph T. Lundquist, Richard J. Murrills, Ray Unwalla, Paul J. Yaworsky, Sally Selim, John F. Mehlmann, Ho-Sun Lam
Publikováno v:
Journal of Medicinal Chemistry. 52:6962-6965
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. Hit-t
Autor:
Mark J. Evans, Paige Erin Mahaney, Jay E. Wrobel, Matthew L. Crawley, Ray Unwalla, Kim Callain Younghee, John F. Mehlmann, Joseph T. Lundquist, Douglas C. Harnish
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5289-5292
Pyrrole[2,3-d]azepines have been identified as potent agonists of the farnesoid X receptor (FXR). Based on the planar X-ray crystal structure of WAY-362450 1 in the ligand binding domain and molecular modeling studies, non-planar reduced compounds we
Autor:
Lloyd M. Garrick, John F. Mehlmann, Diane B. Hauze, Joshua E. Cottom, Daniel M. Green, Jeffrey C. Pelletier, Murty Chengalvala, Irene Feingold, Joseph T. Lundquist, John F. Rogers, Charles William Mann, Linda Shanno, Jay E. Wrobel, Christine Huselton, Wenling Kao, Kees Kenneth L
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1986-1990
A previous report described the serum LH suppression pharmacology of the 2-phenyl-4-piperazinyl-benzimidazole N-ethyluracil GnRH receptor antagonist 1 following oral administration in rats. A series of small heterocycles were appended to the 2-(4-ter
Autor:
William R. Adams, Irene Feingold, John F. Mehlmann, Cesario O Tio, Joshua E. Cottom, Jay E. Wrobel, Jeffrey C. Pelletier, Daniel M. Green, John F. Rogers, James W. Jetter, Murty Chengalvala, Joseph T. Lundquist, Charles William Mann, Linda Shanno, Ronald L. Magolda, Diane B. Hauze, Gregory S. Kopf, Christine Huselton
Publikováno v:
Journal of Medicinal Chemistry. 52:2148-2152
A potent, highly insoluble, GnRH antagonist with a 2-phenyl-4-piperazinylbenzimidazole template and a quinoxaline-2,3-dione pharmacophore was modified to maintain GnRH antagonist activity and improve in vitro pharmaceutical properties. Structural cha