Potent benzimidazolone-based CGRP receptor antagonists

被引：12

作者：

Theberge, Cory R. ^{[1
]}

Bednar, Rodney A. ^{[1
]}

Bell, Ian M. ^{[1
]}

Corcoran, Halea A. ^{[3
]}

Fay, John F. ^{[1
]}

Hershey, James C. ^{[3
]}

Johnston, Victor K. ^{[2
]}

Kane, Stefanie A. ^{[2
]}

Mosser, Scott ^{[1
]}

Salvatore, Christopher A. ^{[2
]}

Williams, Theresa M. ^{[1
]}

Zartman, C. Blair ^{[1
]}

Zhang, Xu-Fang ^{[1
]}

Graham, Samuel L. ^{[1
]}

Vacca, Joseph P. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Med Chem, West Point, PA 19486 USA

[2] Merck & Co Inc, Dept Pain Res, West Point, PA 19486 USA

[3] Merck & Co Inc, Dept Bone Resp Immunol & Endocrine, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

Migraine; CGRP; Spirohydantoin; Benzimidazole;

D O I：

10.1016/j.bmcl.2008.10.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The previously disclosed spirohydantoin-based CGRP receptor antagonists were optimized for potency through modi. cation of the benzimidazolone substituents. Compounds were identified which had minimal shift in the cAMP functional assay containing 50% human serum. Blockade of CGRP-mediated vasodilation was observed with these compounds in a rhesus pharmacodynamic assay and the in vivo potency correlated with the in vitro activity in the serum-shifted functional assay. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6122 / 6125

页数：4

共 50 条

[41] AZABICYCLOALKYL BENZIMIDAZOLONE DERIVATIVES - A NOVEL CLASS OF 5-HT3 RECEPTOR ANTAGONISTS
TURCONI, M
NICOLA, M
QUINTERO, MG
GIRALDO, E
MICHELETTI, R
RIZZI, CA
DONETTI, A
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1990, 199 : 103 - MEDI
[42] Characterization of transit rates in the large intestine of mice following treatment with a CGRP antibody, CGRP receptor antibody, and small molecule CGRP receptor antagonists
Johnson, Kirk W.
Li, Xia
Huang, Xiaofang
Heinz, Beverly A.
Yu, Jianliang
Li, Baolin
[J]. HEADACHE, 2022, 62 (07): : 848 - 857
[43] Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists
Bell, Ian M.
Bednar, Rodney A.
Fay, John F.
Gallicchio, Steven N.
Hochman, Jerome H.
McMasters, Daniel R.
Miller-Stein, Cynthia
Moore, Eric L.
Mosser, Scott D.
Pudvah, Nicole T.
Quigley, Amy G.
Salvatore, Christopher A.
Stump, Craig A.
Theberge, Cory R.
Wong, Bradley K.
Zartman, C. Blair
Zhang, Xu-Fang
Kane, Stefanie A.
Graham, Samuel L.
Vacca, Joseph P.
Williams, Theresa M.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (24) : 6165 - 6169
[44] Novel oxazolidinone CGRP receptor antagonists for the acute treatment of migraine
Crowley, Brendan M.
Selnick, Hal G.
Stump, Craig A.
Stachel, Shawn J.
Potteiger, Craig M.
Nguyen, Diem N.
Quigley, Amy G.
Nomland, Ashley
Bruno, Joseph G.
Kemmerer, Amanda L.
Menzel, Karsten
White, Rebecca B.
Cui, Dan
Moore, Eric L.
Danzinger, Andrew
Paone, Dan V.
Burgey, Christopher S.
Fraley, Mark E.
Salvatore, Christopher A.
Mosser, Scott D.
Fandozzi, Christine
Kane, Stefanie A.
Graham, Samuel L.
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 248
[45] Innovative treatment of acute migraine pain with CGRP receptor antagonists
Herbert, MK
Holzer, P
[J]. ANASTHESIOLOGIE INTENSIVMEDIZIN NOTFALLMEDIZIN SCHMERZTHERAPIE, 2004, 39 (11): : 657 - 661
[46] A human in vivo model to investigate the potency of CGRP receptor antagonists
Vanmolkot, FHM
de Hoon, JNJM
[J]. CEPHALALGIA, 2004, 24 (02) : 150 - 150
[47] THE POTENTIAL OF CGRP RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN FOCUS ON MIGRAINE
Doods, Henri
[J]. NEUROPEPTIDES, 2010, 44 (06) : 526 - 527
[48] Syntheses of 3-aminopiperidinone amides as CGRP receptor antagonists
Wang, Cheng
Fraley, Mark
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2016, 252
[49] CGRP-Receptor antagonists - A fresh approach to migraine therapy?
Durham, PL
[J]. NEW ENGLAND JOURNAL OF MEDICINE, 2004, 350 (11): : 1073 - 1075
[50] CGRP receptor antagonists: an expanding drug class for acute migraine?
Negro, Andrea
Lionetto, Luana
Simmaco, Maurizio
Martelletti, Paolo
[J]. EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2012, 21 (06) : 807 - 818

← 1 2 3 4 5 →