Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Duane R. Reiss"'
Autor:
Andres D. Ramirez, Anthony L. Gotter, Steven V. Fox, Pamela L. Tannenbaum, Lihang eYao, Spencer J. Tye, Terrence eMcDonald, Joseph eBrunner, Susan L. Garson, Duane R. Reiss, Scott D. Kuduk, Paul J. Coleman, Jason M. Uslaner, Robert eHodgson, Susan E. Browne, John J. Renger, Christopher J. Winrow
Publikováno v:
Frontiers in Neuroscience, Vol 7 (2013)
Dual orexin receptor antagonists (DORAs) are a potential treatment for insomnia that function by blocking both the orexin 1 and orexin 2 receptors. The objective of the current study was to further confirm the impact of therapeutic mechanisms targeti
Externí odkaz:
https://doaj.org/article/7a637e4e89e342579deeac811d80cf1d
Autor:
Michael J. Breslin, Paul J. Coleman, Duane R. Reiss, Christopher D. Cox, Anthony L. Gotter, Joanne Stevens, Scott M. Doran, John D. Schreier, Donghui Cui, Christopher J. Winrow, John J. Renger, Steven V. Fox, Charles M. Harrell, Pamela L. Tannenbaum, Susan L. Garson
Publikováno v:
Neuropharmacology. 62:978-987
Orexin (hypocretin) neuropeptides promote wakefulness by signaling through two G-protein coupled receptors, Orexin 1 Receptor (OX(1)R) and Orexin 2 Receptor (OX(2)R). MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(
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
Autor:
Douglas J. Pettibone, Mark G. Bock, Scott D. Kuduk, Cuyue Tang, Thomayant Prueksaritanont, Kathy L. Murphy, Richard W. Ransom, Samson M. Jolly, Duane R. Reiss, Neville J. Anthony, Vera Bodmer-Narkevitch, Victoria Cofre
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7011-7014
A new class of indazole-derived bradykinin B1 antagonists and their structure–activity relationships (SAR) is reported. A number of compounds were found to have low-nanomolar affinity for the human B1 receptor and possess acceptable P-gp and pharma
Autor:
Thomayant Prueksaritanont, Christopher J. Winrow, Duane R. Reiss, Georgia B. McGaughey, John J. Renger, Christopher D. Cox, George D. Hartman, Paul J. Coleman, C. Meacham Harrell, Richard G. Ball, John D. Schreier, Michael J. Bogusky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2311-2315
Orexins are neuropeptides that regulate wakefulness and arousal. Small molecule antagonists of orexin receptors may provide a novel therapy for the treatment of insomnia and other sleep disorders. In this Letter we describe the design and synthesis o
Autor:
John J. Renger, Chunze Li, Michael J. Bogusky, Yuxing Li, Scott M. Doran, David B. Whitman, Wei Lemaire, John D. Schreier, Joseph G. Bruno, Karen M. Brashear, Duane R. Reiss, Thomayant Prueksaritanont, Rodney A. Bednar, C. Meacham Harrell, Susan L. Garson, Paul J. Coleman, Richard L. Kraus, Christopher D. Cox, George D. Hartman, Kenneth S. Koblan, Michael J. Breslin, Christopher J. Winrow
Publikováno v:
ChemMedChem. 4:1069-1074
Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we describe discovery of a dual (OX(1)R/OX(2)R) orexin receptor antagonist featuring a 1,4-diazepan
Autor:
Duane R. Reiss, Ronald K. Chang, Scott D. Kuduk, Kathy L. Murphy, Douglas J. Pettibone, Thomayant Prueksaritanont, Robert M. DiPardo, Cuyue Tang, Mark G. Bock, Christina N. Di Marco, Richard W. Ransom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5107-5110
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitabl
Autor:
Thomayant Prueksaritanont, Douglas J. Pettibone, Paul J. Coleman, Richard W. Ransom, Swati P. Mercer, Wei Lemaire, Kenneth S. Koblan, Jeffrey M. Bergman, Chunze Li, Anthony J. Roecker, Rodney A. Bednar, C. Meacham Harrell, Christopher J. Winrow, Kathy L. Murphy, Duane R. Reiss, George D. Hartman, John J. Renger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1425-1430
A series of OX2R/OX1R dual orexin antagonists was prepared based on a proline bis-amide identified as a screening lead. Through a combination of classical and library synthesis, potency enhancing replacements for both amide portions were discovered.
Autor:
J. Fred Hess, Kathy M. Schirripa, Robert M. DiPardo, Christina N. Di Marco, Kathy L. Murphy, C. Meacham Harrell, Nova Sain, Jenny Wai, Marie A. Holahan, Douglas J. Pettibone, Ronald K. Chang, Mark G. Bock, Richard W. Ransom, June J. Kim, Jacquelynn J. Cook, Duane R. Reiss, Mark O. Urban, Cuyue Tang, Scott D. Kuduk, Thomayant Prueksaritanont, Michael R. Wood
Publikováno v:
Journal of Medicinal Chemistry. 50:272-282
A series of biphenylaminocyclopropane carboxamide based bradykinin B1 receptor antagonists has been developed that possesses good pharmacokinetic properties and is CNS penetrant. Discovery that the replacement of the trifluoropropionamide in the lead
Autor:
Qinghua Song, Ronald C. Hendrickson, John J. Renger, James Conway, Paul J. Coleman, Rhonda R. Taylor, Duane R. Reiss, Daniel S Spellman, Christopher J. Winrow, Ronald A. Miller
Publikováno v:
Journal of Neurogenetics
The combination of stable isotope labeling of amino acids in mammals (SILAM) and laser capture microdissection (LCM) for selective proteomic analysis of the targeted tissues holds tremendous potential for refined characterization of proteome changes