Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Robert Macci"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f1b018775ed0613c97b43faeac8e918
https://pubmed.ncbi.nlm.nih.gov/33096162
https://pubmed.ncbi.nlm.nih.gov/33096162
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78ac514e0ff9910e3b128930ebdf5765
https://doi.org/10.1016/j.bmcl.2013.04.012
https://doi.org/10.1016/j.bmcl.2013.04.012
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9efad766cca18838d811178ca1ce78b8
https://doi.org/10.1016/j.bmcl.2013.01.011
https://doi.org/10.1016/j.bmcl.2013.01.011
Autor:
Carl D. Davis, Laura J. Signor, Chaturvedula Prasad, George Thalody, Richard Schartman, Gene M. Dubowchik, Rita L. Civiello, John E. Macor, Charles M. Conway, Shelly X. Ren, Robert Macci, Xiaojun Han, Deborah A. Cook, Kimberly A. Widmann, Cen Xu, Sokhom S. Pin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4723-4727
We have systematically studied the effects of varying the central unnatural amino acid moiety on CGRP receptor antagonist potency and CYP inhibition in a series of ureidoamides. In this Letter, we report the discovery of compound 23, a potent CGRP re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bc3bbed405bf048163d0f84953dedba
https://doi.org/10.1016/j.bmcl.2012.05.074
https://doi.org/10.1016/j.bmcl.2012.05.074
Autor:
Neil Mathias, Sokhom S. Pin, Xiaojun Han, Paul Moench, John E. Macor, Richard Schartman, Charles M. Conway, Chaturvedula Prasad, Rex Denton, Kimberly A. Widmann, Laura J. Signor, Gene M. Dubowchik, Deborah A. Cook, Andrew P. Degnan, George Thalody, Robert Macci, Carl D. Davis, Shelly X. Ren, Cen Xu
Publikováno v:
Journal of Medicinal Chemistry. 51:4858-4861
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant CYP3A4 inhibition, and poor aqueous solubility. Herein, we describe the optimization of these
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fa440795b5aa2edcd0d1f4a3cb63ab67
https://doi.org/10.1021/jm800546t
https://doi.org/10.1021/jm800546t
Autor:
Tracey Fiedler, Matthew T. Taber, Jie Zhang, Shelly X. Ren, Robert Macci, Sokhom S. Pin, Gene M. Dubowchik, Kaitlin E. Browman, Lynn A. Balanda, Jay O. Knipe, Kevin D. Burris, Rita L. Civiello, Xiaojun Han
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2026-2030
8-Aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes represent a novel series of high-affinity corticotropin-releasing factor-1 receptor (CRF1R) antagonists. Herein we report the synthesis and SAR around the tricyclic core and the anxiolytic activity of an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af1143383cd229586f3c2af1512e57b5
https://doi.org/10.1016/j.bmcl.2007.01.008
https://doi.org/10.1016/j.bmcl.2007.01.008
Autor:
Andrew P. Degnan, Charles M. Conway, Richard Schartman, Cen Xu, John E. Macor, Richard A. Dalterio, Robert Macci, Stephen E. Mercer, Gene M. Dubowchik
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(13)
The calcitonin gene-related peptide (CGRP) receptor has been implicated in the pathogenesis of migraine. A class of urethanamide derivatives has been identified as potent inhibitors of the CGRP receptor. Compound 20 was found to be among the most pot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95006fcdbe8f416975a12c6c59656fcc
https://pubmed.ncbi.nlm.nih.gov/19467597
https://pubmed.ncbi.nlm.nih.gov/19467597
Autor:
Andrew P, Degnan, Prasad V, Chaturvedula, Charles M, Conway, Deborah A, Cook, Carl D, Davis, Rex, Denton, Xiaojun, Han, Robert, Macci, Neil R, Mathias, Paul, Moench, Sokhom S, Pin, Shelly X, Ren, Richard, Schartman, Laura J, Signor, George, Thalody, Kimberly A, Widmann, Cen, Xu, John E, Macor, Gene M, Dubowchik
Publikováno v:
Journal of medicinal chemistry. 51(16)
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant CYP3A4 inhibition, and poor aqueous solubility. Herein, we describe the optimization of these
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::26183be6c91d7db91dc9465dc6fe47a7
https://pubmed.ncbi.nlm.nih.gov/18665579
https://pubmed.ncbi.nlm.nih.gov/18665579
Autor:
John E. Macor, Paul Moench, Xiang-Jun Jiang, Xiaojun Han, Neil Mathias, Sokhom S. Pin, Valerie J. Whiterock, Deborah A. Cook, Charles M. Conway, Richard Schartman, Gene M. Dubowchik, Carl D. Davis, George O. Tora, Cen Xu, Robert Macci, Andrew P. Degnan, Rita L. Civiello, George Thalody, Laura J. Signor
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3674
0960-894X/$ see front matter 2013 Elsevier Ltd. All rights reserved. http://dx.doi.org/10.1016/j.bmcl.2013.03.063 DOI of original article: http://dx.doi.org/10.1016/j.bmcl.2013.01.011 ⇑ Corresponding authors. E-mail addresses: xiaojun.han@bms.com (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0a9c4174811786c7e2e587f8f97b7376
https://doi.org/10.1016/j.bmcl.2013.03.063
https://doi.org/10.1016/j.bmcl.2013.03.063