Non-steroidal glucocorticoid agonists

被引：0

作者：

不详

机构：

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2005年 / 15卷 / 04期

关键词：

685698; 799943; beta-adrenoceptor; beta(2)-agonist; asthma; chronic obstructive pulmonary disease (COPD); corticosteroid; glucocorticoid receptor;

D O I：

10.1517/13543776.15.4.467

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New highly-selective glucocorticoid receptor agonists that are 3-bicyclyl-2-hydroxy-N-4-methyl-1-oxobenzoxazin-6-yl 2-trifluoromethylpropanamide derivatives are claimed. These compounds display reduced activity as transactivators whilst retaining high affinity for the glucocorticoid receptor and good potency as transrepressors. They should thus produce fewer side effects than currently marketed corticosteroids and are claimed to provide methods of treating eczema, psoriasis, allergic dermatitis, neurodermatitis, pruritis and hypersensitivity reactions.

引用

页码：467 / 470

页数：4

共 50 条

[1] Identification and optimization of non-steroidal glucocorticoid receptor agonists
Thomson, David S.
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 233 : 578 - 578
[2] Identification of dissociated non-steroidal glucocorticoid receptor agonists
Kuzmich, Daniel
Kirrane, Tom
Proudfoot, John
Bekkali, Younes
Zindell, Renee
Beck, Laura
Nelson, Richard
Shih, Cheng-Kon
Kukulka, Alison J.
Paw, Zofia
Reilly, Patty
Deleon, Rodney
Cardozo, Mario
Nabozny, Gerald
Thomson, David
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (18) : 5025 - 5031
[3] Advances Toward Dissociated Non-Steroidal Glucocorticoid Receptor Agonists
Regan, John
Razavi, Hossein
Thomson, David
[J]. ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 43, 2008, 43 : 141 - 154
[4] Discovery of New non-steroidal selective glucocorticoid receptor agonists
Potamitis, Constantinos
Siakouli, Dimitra
Papavasileiou, Konstantinos D.
Boulaka, Athina
Ganou, Vassiliki
Roussaki, Marina
Calogeropoulou, Theodora
Zoumpoulakis, Panagiotis
Alexis, Michael N.
Zervou, Maria
Mitsiou, Dimitra J.
[J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 2019, 186 : 142 - 153
[5] Steroidal or non-steroidal FXR agonists - Is that the question?
Verbeke, Len
Nevens, Frederik
Laleman, Wim
[J]. JOURNAL OF HEPATOLOGY, 2017, 66 (04) : 680 - 681
[6] Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists
Barnett, Heather A.
Coe, Diane M.
Cooper, Tony W. J.
Jack, Torquil I.
Jones, Haydn T.
Macdonald, Simon J. F.
McLay, Iain M.
Rayner, Natalie
Sasse, Rosemary Z.
Shipley, Tracy J.
Skone, Phil A.
Somers, Graham I.
Taylor, Simon
Uings, Iain J.
Woolven, James M.
Weingarten, Gordon G.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (01) : 158 - 162
[7] Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists
Biggadike, Keith
Caivano, Matilde
Clackers, Margaret
Coe, Diane M.
Hardy, George W.
Humphreys, Davina
Jones, Haydn T.
House, David
Miles-Williams, Annette
Skone, Philip A.
Uings, Iain
Weller, Vicki
McLay, Iain M.
Macdonald, Simon J. F.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (16) : 4846 - 4850
[8] Non-steroidal glucocorticoid agonists - The discovery of aryl pyrazoles as A-ring mimetics
Clackers, Margaret
Coe, Diane M.
Demaine, Derek A.
Hardy, George W.
Humphreys, Davina
Inglis, Graham G. A.
Johnston, Michael J.
Jones, Haydn T.
House, David
Loiseau, Richard
Minick, Doug J.
Skone, Philip A.
Uings, Iain
McLay, Iain M.
Macdonald, Simon J. F.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (17) : 4737 - 4745
[9] A design and iterative approach to non-steroidal and steroidal agonists
Biggadike, Keith
Coe, Diane M.
Mclay, Lain M.
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 233 : 671 - 671
[10] TNFα-induced glucocorticoid resistance: Effect of steroidal and non-steroidal GR agonists, formoterol and inhibition of inflammatory signalling
Rider, Christopher
Shah, Suharsh
Miller-Larsson, Anna
Proud, David
Johnson, Malcolm
Giembycz, Mark
Newton, Robert
[J]. EUROPEAN RESPIRATORY JOURNAL, 2012, 40

← 1 2 3 4 5 →