Zobrazeno 1 - 10
of 60
pro vyhledávání: '"Scott D. Mosser"'
Autor:
Samuel L. Graham, Joseph G. Bruno, Scott D. Mosser, Harold G. Selnick, Sandra M. Sanabria-Bohórquez, Christopher A. Salvatore, Rebecca B. White, Melody Mcwherter, Hong Fan, Mangay Williams, Jacquelynn J. Cook, Kerry Riffel, Richard Hargreaves, Ian M. Bell, Craig A. Stump, Eric L. Moore, Liza Gantert, Steven N. Gallicchio, Mona Purcell, C. Blair Zartman, Amanda L. Kemmerer, Eric D. Hostetler, Donnette D. Staas, Stefanie A. Kane
Publikováno v:
ACS Medicinal Chemistry Letters. 4:863-868
Rational modification of the potent calcitonin gene-related peptide (CGRP) receptor antagonist MK-3207 led to a series of analogues with enhanced CNS penetrance and a convenient chemical handle for introduction of a radiolabel. A number of (11)C-trac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::728068784798afa8e15d916cf69db509
https://doi.org/10.1021/ml400199p
https://doi.org/10.1021/ml400199p
Autor:
Samuel L. Graham, Christine Fandozzi, Eric L. Moore, Donnette D. Staas, Ian M. Bell, Nova Sain, Joseph G. Bruno, Steven N. Gallicchio, Harold G. Selnick, Christopher A. Salvatore, Mark O. Urban, Rebecca B. White, Matthew M. Zrada, Amy Calamari, C. Blair Zartman, Amanda L. Kemmerer, Joseph P. Vacca, Stefanie A. Kane, Craig A. Stump, Scott D. Mosser
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3941-3945
Rational modification of the clinically tested CGRP receptor antagonist MK-3207 (3) afforded an analogue with increased unbound fraction in rat plasma and enhanced aqueous solubility, 2-[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e62e622cb95d0ea053c8a538444e4e67
https://doi.org/10.1016/j.bmcl.2012.04.105
https://doi.org/10.1016/j.bmcl.2012.04.105
Autor:
Christine Fandozzi, James J. Vornov, Reza Mazhari, Scott D. Mosser, Shil Patel, Joseph J. Lynch, Nigel J. Liverton, Rachel M Garner, Rodney A. Bednar, Blake Paterson, John A. Mccauley, Shobha Gopalakrishnan, Stanley L. Gaul, Armando Lagrutta, Richard Briscoe, Laszlo Kiss
Publikováno v:
Pharmacology Research & Perspectives
The preclinical pharmacodynamic and pharmacokinetic properties of 4-methylbenzyl (3S, 4R)-3-fluoro-4-[(Pyrimidin-2-ylamino) methyl] piperidine-1-carboxylate (CERC-301), an orally bioavailable selective N-methyl-D-aspartate (NMDA) receptor subunit 2B
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::963a29e4d8bdaffca234948b39663662
http://europepmc.org/articles/PMC4777252
http://europepmc.org/articles/PMC4777252
Autor:
Nicole Trainor, E V Lis, Anthony G. DiLella, Terrence P. McDonald, Annie Liang, Mark E. Layton, Duane R. Reiss, Michael J. Kelly, Sanderson Philip E, James Yergey, Kevin J. Rodzinak, Steven D. Young, Guy R. Seabrook, Christine Fandozzi, Michael E. Cunningham, Scott D. Mosser, Mark O. Urban, John F. Fay, Hao Wang, Kenneth S. Koblan, Rodney A. Bednar
Publikováno v:
ACS Chemical Neuroscience. 2:352-362
A series of 3-substituted aminocyclopentanes has been identified as highly potent and selective NR2B receptor antagonists. Incorporation of a 1,2,4-oxadiazole linker and substitution of the pendant phenyl ring led to the discovery of orally bioavaila
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd2684ec1a091b2da7e8fdaae9487129
https://doi.org/10.1021/cn200013d
https://doi.org/10.1021/cn200013d
Autor:
Anthony W. Shaw, Theresa M. Williams, Joseph P. Vacca, Scott D. Mosser, Sean Yu, Christopher A. Salvatore, Craig M. Potteiger, Stefanie A. Kane, Diem N. Nguyen, Christopher S. Burgey, James Z. Deng, Shane Roller, Daniel V. Paone, Harold G. Selnick
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2683-2686
In our ongoing efforts to develop CGRP receptor antagonists for the treatment of migraine, we aimed to improve upon telecagepant by targeting a compound with a lower projected clinical dose. Imidazoazepanes were identified as potent caprolactam repla
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e6e3b8d2d0a8e489087ed560280589f
https://doi.org/10.1016/j.bmcl.2010.12.054
https://doi.org/10.1016/j.bmcl.2010.12.054
Autor:
Scott D. Mosser, Joseph P. Vacca, Eric L. Moore, Rodney A. Bednar, Shane Roller, John F. Fay, Kathy M. Schirripa, Harold G. Selnick, Michael R. Wood, June J. Kim, Joseph G. Bruno, Christopher A. Salvatore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6827-6830
A previously utilized quinoline-for- N -phenylamide replacement strategy was employed against a central amide in a novel class of CGRP receptor antagonists. A unique and unexpected substitution pattern was ultimately required to maintain reasonable a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eec70e90291b9b8a02fdc7f9b0e97ab5
https://doi.org/10.1016/j.bmcl.2010.08.105
https://doi.org/10.1016/j.bmcl.2010.08.105
Autor:
Joseph P. Vacca, Eric L. Moore, Joseph G. Bruno, Craig A. Stump, Christopher A. Salvatore, Harold G. Selnick, Stefanie A. Kane, Amy G. Quigley, Rodney A. Bednar, Ian M. Bell, Kathy M. Schirripa, John F. Fay, Scott D. Mosser, Shane Roller, Michael R. Wood, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5787-5790
A novel class of CGRP receptor antagonists was rationally designed by modifying a highly potent, but structurally complex, CGRP receptor antagonist. Initial modifications focused on simplified structures, with increased flexibility. Subsequent to the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b8f1786a9f3caf835e3719393c88bbc
https://doi.org/10.1016/j.bmcl.2009.07.134
https://doi.org/10.1016/j.bmcl.2009.07.134
Autor:
Xu-Fang Zhang, Samuel L. Graham, Theresa M. Williams, Craig A. Stump, Victor K. Johnston, Scott D. Mosser, Joseph G. Bruno, C. Blair Zartman, Steven N. Gallicchio, Joseph P. Vacca, Eric L. Moore, Christopher A. Salvatore, John F. Fay, Rodney A. Bednar, Amy G. Quigley, Cory R. Theberge, Ian M. Bell, Stefanie A. Kane
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:214-217
Rational modification of a previously identified spirohydantoin lead structure has identified a series of potent spiroazaoxindole CGRP receptor antagonists. The azaoxindole was found to be a general replacement for the hydantoin that consistently imp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba289d690e0a68c717df88f7fd1e7e54
https://doi.org/10.1016/j.bmcl.2008.10.106
https://doi.org/10.1016/j.bmcl.2008.10.106
Autor:
J. Christopher Culberson, Steven M. Pitzenberger, Charles A. Omer, Michael J. Bogusky, Scott D. Mosser, Kenneth S. Koblan, S. Jane Desolms, E A Giuliani
Publikováno v:
Protein Science. 4:681-688
Farnesyl-protein transferase (FPTase) catalyzes the posttranslational farnesylation of the cysteine residue located in the carboxyl-terminal tetrapeptide of the Ras oncoprotein. Prenylation of this residue is essential for the membrane association an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51f0fe75826118ddc05251871d2f8ece
https://doi.org/10.1002/pro.5560040408
https://doi.org/10.1002/pro.5560040408
Autor:
Jacquelynn J. Cook, Rodney A. Bednar, Thomayant Prueksaritanont, Yvonne M. Leonard, Michael R. Wood, Qin Mei, Richard W. Ransom, Ronald K. Chang, Emily D. Adarayn, Robert M. DiPardo, Jian Yu, Audrey A. Wallace, Wei Lemaire, Scott D. Kuduk, Kathy L. Murphy, G. R. Sitko, Scott D. Mosser, Christina N. Di Marco, Mark G. Bock, Frank C. Clayton, Bang-Lin Wan, Kathy M. Schirripa, Marie A. Holahan, Roger M. Freidinger, Dennis L. Bohn, Douglas J. Pettibone, Raymond S.L. Chang, Cuyue Tang, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:716-720
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f489daa5ddd1907e6d600a79ad35db5d
https://doi.org/10.1016/j.bmcl.2007.11.050
https://doi.org/10.1016/j.bmcl.2007.11.050