Update on the Development of Antagonists of Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTH2). From Lead Optimization to Clinical Proof-of-Concept in Asthma and Allergic Rhinitis

被引：66
作者：
Pettipher, Roy [1 ]
Whittaker, Mark [2 ]
机构：
[1] Oxagen Ltd, Abingdon OX14 4RY, Oxon, England
[2] Evotec UK Ltd, Abingdon OX14 4SA, Oxon, England
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 07期
关键词：
PROSTAGLANDIN D-2 RECEPTOR; SELECTIVE THIAZOLEACETIC ACIDS; HELPER TYPE-2 CELLS; CRTH2; ANTAGONISTS; METABOLIC-ACTIVATION; POTENT; DP2; BINDING; INFLAMMATION; DERIVATIVES;
D O I：
10.1021/jm2013997
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
[No abstract available]
引用
收藏
页码：2915 / 2931
页数：17
相关论文
共 118 条
[1]  
Armer R. E., 2005, [No title captured], Patent No. [WO 2005/121141, 2005121141, WO2005121141 A1]
[2]  
Armer R.E., 2005, GB Appl., Patent No. [GB2422830A, 2422830]
[3]  
Armer R.E., 2005, GB Appl., Patent No. [GB2422831a, 2422831]
[4]  
Armer R.E., 2005, GB Appl., Patent No. [GB2422829A, 2422829]
[5]   Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2 [J].
Armer, RE ;
Ashton, MR ;
Boyd, EA ;
Brennan, CJ ;
Brookfield, FA ;
Gazi, L ;
Gyles, SL ;
Hay, PA ;
Hunter, MG ;
Middlemiss, D ;
Whittaker, M ;
Xue, LZ ;
Pettipher, R .
JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (20) :6174-6177
[6]  
Awad M. M. A., 2004, World Pat., Patent No. [2004,035,543, 2004035543, WO 2004035543]
[7]   Structure-Activity Relationships for Degradation Reaction of 1-β-O-Acyl Glucuronides: Kinetic Description and Prediction of Intrinsic Electrophilic Reactivity under Physiological Conditions [J].
Baba, Akiko ;
Yoshioka, Tadao .
CHEMICAL RESEARCH IN TOXICOLOGY, 2009, 22 (01) :158-172
[8]   Acyl glucuronide reactivity in perspective: biological consequences [J].
Bailey, MJ ;
Dickinson, RG .
CHEMICO-BIOLOGICAL INTERACTIONS, 2003, 145 (02) :117-137
[9]   Pharmacology of AM211, a Potent and Selective Prostaglandin D2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation [J].
Bain, Gretchen ;
Lorrain, Daniel S. ;
Stebbins, Karin J. ;
Broadhead, Alex R. ;
Santini, Angelina M. ;
Prodanovich, Pat ;
Darlington, Janice ;
King, Christopher D. ;
Lee, Catherine ;
Baccei, Christopher ;
Stearns, Brian ;
Troung, Yen ;
Hutchinson, John H. ;
Prasit, Peppi ;
Evans, Jilly F. .
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2011, 338 (01) :290-301
[10]   A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma [J].
Barnes, N. ;
Pavord, I. ;
Chuchalin, A. ;
Bell, J. ;
Hunter, M. ;
Lewis, T. ;
Parker, D. ;
Payton, M. ;
Collins, L. Pearce ;
Pettipher, R. ;
Steiner, J. ;
Perkins, C. M. .
CLINICAL AND EXPERIMENTAL ALLERGY, 2012, 42 (01) :38-48
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