Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Valerie J. Whiterock"'
Autor:
Sokhom S. Pin, Deborah A. Cook, John E. Macor, Laura J. Signor, Carl Davis, Valerie J. Whiterock, Gene M. Dubowchik, Richard Schartman, Ping Chen, Chaturvedula Prasad, Kimberly A. Widmann, George Thalody, Walter Kostich, Robert Macci, John J. Herbst, Stephen E. Mercer, Charles M. Conway, Cen Xu
Publikováno v:
Bioorganicmedicinal chemistry letters. 31
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant (BHV-3500, BMS-742413) is a high affinity antagonist of the CGRP receptor (hCGRP Ki = 0.023 nM) that has demons
Autor:
Valerie J. Whiterock, Xiang-Jun Jiang, Guanglin Luo, Carl D. Davis, Charles M. Conway, Deborah Keavy, Kimberly A. Widmann, Laura J. Signor, Walter Kostich, Ling Chen, John E. Macor, Gene M. Dubowchik, Richard Schartman, Ping Chen, Michael Gulianello
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 43:128077
In our efforts to identify orally bioavailable CGRP receptor antagonists, we previously discovered a novel series of orally available azepinone derivatives that unfortunately also exhibited the unwanted property of potent time-dependent human CYP3A4
Autor:
Valerie J. Whiterock, Amy Easton, Regina Miller, Lawrence R. Marcin, Meredith Ferrante, Bradley C. Pearce, John B. Hogan, Joanne J. Bronson, Clotilde Bourin, Mendi A. Higgins, Robert G. Gentles, F. Christopher Zusi, Walter Kostich, John E. Macor, Michael Gulianello, Min Ding, Linda J. Bristow, Adam Hendricson, Kim A. Johnson, Andrew Alt, Yanling Huang, Matthew A. Seager
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:496-513
Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selec
Autor:
Andrew P. Degnan, Valerie J. Whiterock, Darrell Maxwell, Umesh Hanumegowda, Digavalli V. Sivarao, Anand Balakrishnan, Eric Shields, Joanne J. Bronson, Jeffrey M. Brown, Ryan Westphal, Amy Easton, Arun K. Senapati, Xiaoliang Zhuo, John E. Macor, Kenneth S. Santone, Michael Gulianello, Regina Miller, Melissa Hill-Drzewi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5871-5876
Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-d-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5 (mGluR5) enhances NMDA
Autor:
Valerie J. Whiterock, John E. Macor, Joanne J. Bronson, Melissa Hill-Drzewi, Regina Miller, Lizbeth Gallagher, Thaddeus F. Molski, Amy Easton, Xiaoliang Zhuo, Matthew D. Hill, Andrew P. Degnan, Xiaojun Han, Jeffrey M. Brown, Robert L. Bertekap, Haiquan Fang, Michael Gulianello, Michele Matchett, Kenneth S. Santone, Anand Balakrishnan
Publikováno v:
ACS Medicinal Chemistry Letters. 7:1082-1086
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the N-methyl-d-aspartate receptor (NMDAR). We describe the synthesis o
Autor:
Michael K. Ahlijanian, Yu-Wen Li, Valerie J. Whiterock, Ping Chen, Alda Fernandes, Digavalli V. Sivarao, Yili Yang, Arun K. Senapati, Yulia Benitex
Publikováno v:
Neuropsychopharmacology. 41:2232-2240
Schizophrenia patients exhibit dysfunctional gamma oscillations in response to simple auditory stimuli or more complex cognitive tasks, a phenomenon explained by reduced NMDA transmission within inhibitory/excitatory cortical networks. Indeed, a simp
Autor:
John E. Macor, Chaturvedula Prasad, Rex Denton, Gene M. Dubowchik, Paul Moench, Valerie J. Whiterock, Charlie M. Conway, Cen Xu, Neil Mathias, Glenn H. Cantor, Robert Macci, Richard Schartman, Laura J. Signor, Stephen E. Mercer, George Thalody, Carl D. Davis, Deborah Keavy, Sokhom S. Pin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3157-3161
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown to be efficacious as abortive migraine therapeutics with the absence of cardiovascular liabilities that are associated with triptans. Herein, we report the discovery of a hig
Autor:
George Thalody, Paul Moench, Valerie J. Whiterock, Deborah A. Cook, Charles M. Conway, Xiang-Jun Jiang, Laura J. Signor, Neil Mathias, Richard Schartman, Carl D. Davis, Cen Xu, Robert Macci, Xiaojun Han, George O. Tora, Sokhom S. Pin, John E. Macor, Gene M. Dubowchik, Andrew P. Degnan, Rita L. Civiello
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1870-1873
Various substituted indazole and benzoxazolone amino acids were investigated as d -tyrosine surrogates in highly potent CGRP receptor antagonists. Compound 3, derived from the 7-methylindazole core, afforded a 30-fold increase in CGRP binding potency
Autor:
Arun K. Senapati, Valerie J. Whiterock, Fukang Yang, Lawrence B. Snyder, Andrew P. Degnan, Ryan Westphal, Hong Huang, Gail K. Mattson, Digavalli V. Sivarao, Anand Balakrishnan, Michael Gulianello, Michele Matchett, Eric Shields, Kenneth S. Santone, Joanne J. Bronson, John E. Macor, Amy Easton, Yanling Huang, Regina Miller
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(17)
Herein we describe the structure activity relationships uncovered in the pursuit of an mGluR5 positive allosteric modulator (PAM) for the treatment of schizophrenia. It was discovered that certain modifications of an oxazolidinone-based chemotype aff
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5
Autor:
Amy Easton, Jeffrey M. Brown, Valerie J. Whiterock, Yanling Huang, Gail K. Mattson, Kelli M. Jones, Michele Matchett, Arun K. Senapati, Andrew P. Degnan, Frank J. Simutis, Yu-Wen Li, Lawrence B. Snyder, Alda Fernandes, Digavalli V. Sivarao, Anand Balakrishnan, Umesh Hanumegowda, Kenneth S. Santone, Eric Shields, Regina Miller, Joanne J. Bronson, Ryan Westphal, Michael Gulianello, John E. Macor, Hong Huang, Fukang Yang
Positive allosteric modulators (PAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5) are of interest due to their potential therapeutic utility in schizophrenia and other cognitive disorders. Herein we describe the discovery and optimizati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0406345b8ecda64a2e9a0876f7702b99
https://europepmc.org/articles/PMC4789665/
https://europepmc.org/articles/PMC4789665/