Novel CRTH2 antagonists: a review of patents from 2006 to 2009

Bibliography

• Roberts LJ, Sweetman BJ, Lewis RA, Increased production of prostaglandin D2 in patients with systemic mastocytosis. N Engl J Med 1980;303:1400-4
   PubMed Web of Science ®Google Scholar
• Lewis RA, Soter NA, Diamond PT, Prostaglandin D2 generation after activation of rat and human mast cells with anti-IgE. J Immunol 1982;129:1627-31
   PubMed Web of Science ®Google Scholar
• Murray JJ, Tonnel AB, Brash AR, Release of prostaglandin D2 into human airways during acute antigen challenge. N Engl J Med 1986;315:800-4
   PubMed Web of Science ®Google Scholar
• Ulven T, Kostenis E. Targeting the prostaglandin D2 receptors DP and CRTH2 for treatment of inflammation. Curr Top Med Chem 2006;6:1427-44
   PubMed Web of Science ®Google Scholar
• Hirai H, Tanaka K, Yoshie O, Prostaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2. J Exp Med 2001;193:255-61
   PubMed Web of Science ®Google Scholar
• Monneret G, Gravel S, Diamond M, Prostaglandin D2 is a potent chemoattractant for human eosinophils that acts via a novel DP receptor. Blood 2001;98:1942-8
   PubMed Web of Science ®Google Scholar
• Nagata K, Tanaka K, Ogawa K, Selective expression of a novel surface molecule by human Th2 cells in vivo. J Immunol 1999;162:1278-86
   PubMed Web of Science ®Google Scholar
• Pettipher R, Hansel TT, Armer R. Antagonism of the prostaglandin D2 receptors DP1 and CRTH2 as an approach to treat allergic diseases. Nat Rev Drug Discov 2007;6:313-25
   PubMed Web of Science ®Google Scholar
• Kostenis E, Ulven T. Emerging roles of DP and CRTH2 in allergic inflammation. Trends Mol Med 2006;12:148-58
   PubMedGoogle Scholar
• Schuligoi R, Sturm E, Luschnig P, CRTH2 and D-type prostanoid receptor antagonists as novel therapeutic agents for inflammatory diseases. Pharmacology 2010;85:372-82
   PubMed Web of Science ®Google Scholar
• Huang JL, Gao PS, Mathias RA, Sequence variants of the gene encoding chemoattractant receptor expressed on Th2 cells (CRTH2) are associated with asthma and differentially influence mRNA stability. Hum Mol Genet 2004;13:2691-7
   PubMedGoogle Scholar
• Wang JH, Xu YC, Zhao H, Genetic variations in chemoattractant receptor expressed on Th2 cells (CRTH2) is associated with asthma susceptibility in Chinese children. Mol Biol Rep 2009;36:1549-53
   PubMedGoogle Scholar
• Cameron L, Depner M, Kormann M, Genetic variation in CRTh2 influences development of allergic phenotypes. Allergy 2009;64:1478-85
   PubMed Web of Science ®Google Scholar
• Shirasaki H, Kikuchi M, Kanaizumi E, Himi T. Accumulation of CRTH2-positive leukocytes in human allergic nasal mucosa. Ann Allergy Asthma Immunol 2009;102:110-15
   PubMedGoogle Scholar
• Yahara H, Satoh T, Miyagishi C, Yokozeki H. Increased expression of CRTH2 on eosinophils in allergic skin diseases. J Eur Acad Dermatol Venereol 2010;24:75-6
   PubMed Web of Science ®Google Scholar
• Sugimoto H, Shichijo M, Iino T, An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther 2003;305:347-52
   PubMed Web of Science ®Google Scholar
• Spik I, Brenuchon C, Angeli V, Activation of the prostaglandin D2 receptor DP2/CRTH2 increases allergic inflammation in mouse. J Immunol 2005;174:3703-8
   PubMed Web of Science ®Google Scholar
• Shiraishi Y, Asano K, Nakajima T, Prostaglandin D2-induced eosinophilic airway inflammation is mediated by CRTH2 receptor. J Pharmacol Exp Ther 2005;312:954-60
   PubMed Web of Science ®Google Scholar
• Almishri W, Cossette C, Rokach J, Effects of prostaglandin D2, 15-deoxy- delta12,14-prostaglandin J2, and selective DP1 and DP2 receptor agonists on pulmonary infiltration of eosinophils in Brown Norway rats. J Pharmacol Exp Ther 2005;313:64-9
   PubMedGoogle Scholar
• Ulven T, Receveur JM, Grimstrup M, Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. J Med Chem 2006;49:6638-41
   PubMed Web of Science ®Google Scholar
• Uller L, Mathiesen JM, Alenmyr L, Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respir Res 2007;8:16
   PubMed Web of Science ®Google Scholar
• Stearns BA, Baccei C, Bain G, Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis. Bioorg Med Chem Lett 2009;19:4647-51
   PubMed Web of Science ®Google Scholar
• Lukacs NW, Berlin AA, Franz-Bacon K, CRTH2 antagonism significantly ameliorates airway hyperreactivity and downregulates inflammation-induced genes in a mouse model of airway inflammation. Am J Physiol Lung Cell Mol Physiol 2008;295:L767-79
   PubMed Web of Science ®Google Scholar
• Boehme SA, Franz-Bacon K, Chen EP, A small molecule CRTH2 antagonist inhibits FITC-induced allergic cutaneous inflammation. Int Immunol 2009;21:81-93
   PubMed Web of Science ®Google Scholar
• Stebbins KJ, Broadhead AR, Baccei CS, Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung. J Pharmacol Exp Ther 2010;332:764-75
   PubMed Web of Science ®Google Scholar
• Matsuoka T, Hirata M, Tanaka H, Prostaglandin D2 as a mediator of allergic asthma. Science 2000;287:2013-17
   PubMed Web of Science ®Google Scholar
• Schratl P, Royer JF, Kostenis E, The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking. J Immunol 2007;179:4792-9
   PubMedGoogle Scholar
• Hammad H, de Heer HJ, Soullie T, Prostaglandin D2 inhibits airway dentritic cell migration and function in steady state conditions by selective activation of the D prostanoid receptor 1. J Immunol 2003;171:3936-40
   PubMed Web of Science ®Google Scholar
• Hammad H, Kool M, Soullie T, Activation of the D prostanoid 1 receptor suppresses asthma by modulation of lung dendritic cell function and induction of regulatory T cells. J Exp Med 2007;204:357-67
   PubMed Web of Science ®Google Scholar
• Middlemiss D, Ashton MR, Boyd EA, Compounds with PGD2 antagonist activity. WO2005040112; 2005
   Google Scholar
• Liu JW, Fu Z, Wang YC, Discovery and optimization of CRTH2 and DP dual antagonists. Bioorg Med Chem Lett 2009;19:6419-23
   PubMed Web of Science ®Google Scholar
• Hirai H, Tanaka K, Takano S, Cutting edge: agonistic effect of indomethacin on a prostaglandin D2 receptor, CRTH2. J Immunol 2002;168:981-5
   PubMed Web of Science ®Google Scholar
• Stubbs VEL, Schratl P, Hartnell A, Indomethacin causes prostaglandin D2-like and eotaxin-like selective responses in eosinophils and basophils. J Biol Chem 2002;277:26012-20
   PubMed Web of Science ®Google Scholar
• Hata AN, Zent R, Breyer MD, Breyer RM. Expression and molecular pharmacology of the mouse CRTH2 receptor. J Pharmacol Exp Ther 2003;306:463-70
   PubMedGoogle Scholar
• Birkinshaw TN, Teague SJ, Beech C, Discovery of potent CRTh2 (DP2) receptor antagonists. Bioorg Med Chem Lett 2006;16:4287-90
   PubMed Web of Science ®Google Scholar
• Birkinshaw T, Bonnert R, Cook A, Novel substituted indols. WO2003101981; 2003
   Google Scholar
• Armer RE, Ashton MR, Boyd EA, Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. J Med Chem 2005;48:6174-7
   PubMed Web of Science ®Google Scholar
• Mathiesen JM, Ulven T, Martini L, Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. Mol Pharmacol 2005;68:393-402
   PubMed Web of Science ®Google Scholar
• Gervais FG, Morello JP, Beaulieu C, Identification of a potent and selective synthetic agonist at the CRTH2 receptor. Mol Pharmacol 2005;67:1834-9
   PubMedGoogle Scholar
• Ulven T, Kostenis E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem 2005;48:897-900
   PubMed Web of Science ®Google Scholar
• Mathiesen JM, Christopoulos A, Ulven T, On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Mol Pharmacol 2006;69:1441-53
   PubMed Web of Science ®Google Scholar
• Royer JF, Schratl P, Lorenz S, A novel antagonist of CRTH2 blocks eosinophil release from bone marrow, chemotaxis and respiratory burst. Allergy 2007;62:1401-9
   PubMedGoogle Scholar
• Ulven T, Gallen MJ, Nielsen MC, Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. Bioorg Med Chem Lett 2007;17:5924-7
   PubMedGoogle Scholar
• Robarge MJ, Bom DC, Tumey LN, Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists. Bioorg Med Chem Lett 2005;15:1749-53
   PubMed Web of Science ®Google Scholar
• Arimura A, Kishino J, Tanimoto N. Preparation of indole derivatives as PGD2 receptor antagonists. WO2003097042; 2003
   Google Scholar
• Tanimoto N, Hiramatsu Y, Mitsumori S, Inagaki M. Preparation of indole derivatives as PGD2 receptor antagonists. WO2003097598; 2003
   Google Scholar
• Sandham DA, Aldcroft C, Baettig U, 2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists. Bioorg Med Chem Lett 2007;17:4347-50
   PubMed Web of Science ®Google Scholar
• Rist Ø, Grimstrup M, Receveur J-M, Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorg Med Chem Lett 2010;20:1177-80
   PubMedGoogle Scholar
• Grimstrup M, Rist O, Receveur JM, Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorg Med Chem Lett 2010;20:1181-5
   PubMed Web of Science ®Google Scholar
• Mimura H, Ikemura T, Kotera O, Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2. J Pharmacol Exp Ther 2005;314:244-51
   PubMed Web of Science ®Google Scholar
• Liu JW, Wang YC, Sun Y, Tetrahydroquinoline derivatives as CRTH2 antagonists. Bioorg Med Chem Lett 2009;19:6840-4
   PubMed Web of Science ®Google Scholar
• Middlemiss D, Ashton MR, Boyd EA, Compounds having CRTH2 antagonist activity. WO2005040114; 2005
   Google Scholar
• Armer RE, Boyd EA, Brookfield FA. Preparation of pyrrolopyridine derivatives used for treating diseases mediated by prostaglandin D2 (PGD2). WO2005121141; 2005
   Google Scholar
• Armer RE, Boyd EA, Brookfield FA. Preparation of pyrrolopyridines for treating diseases mediated by PGD2 at the CRTH2 receptor. GB2422829; 2006
   Google Scholar
• Armer RE, Boyd EA, Brookfield FA. Preparation of pyrrolopyridines and their use in the treatment of diseases mediated by PGD2 at the CRTH2 receptor. GB2422830; 2006
   Google Scholar
• Armer RE, Boyd EA, Brookfield FA. Preparation of pyrrolopyridines and their use in the treatment of diseases mediated by PGD2 at the CRTH2 receptor. GB2422831; 2006
   Google Scholar
• Middlemiss D, Ashton MR, Boyd EA, Brookfield FA. Use of CRTH2 antagonist compounds in therapy. WO2005044260; 2005
   Google Scholar
• Middlemiss D, Ashton MR, Boyd EA, Brookfield FA. Substituted indol-3-yl acetic acid derivatives. GB2407318; 2005
   Google Scholar
• Boyd EA, Brookfield FA, Brennan CJ, Method for manufacture of microcrystalline (5-fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl) acetic acid. WO2006092579; 2006
   Google Scholar
• Lovell JM. Salts with CRTH2 antagonist activity. WO2007107772; 2007
   Google Scholar
• Hunter MG, Pettipher ER, Perkins CM, Use of CRTH2 antagonist compounds. WO2009063202; 2009
   Google Scholar
• Hunter MG, Pettipher ER, Perkins CM, Use of CRTH2 antagonist compounds. WO2009063215; 2009
   Google Scholar
• Announced on the Oxagen web site, available from: http://www.oxagen.co.uk/crth2.htm [Last accessed 7 February 2010]
   Google Scholar
• Armer RE, Boyd EA, Hay PA. 1-Acetic acid indole derivatives with PGD2 antagonist activity. WO2006095183; 2006
   Google Scholar
• Armer RE, Wynne GM. Compounds having CRTH2 antagonist activity. WO2008012511; 2008
   Google Scholar
• Armer RE, Pettipher ER, Whittaker M, Compounds having CRTH2 antagonists activity. WO2009090414; 2009
   Google Scholar
• Armer RE, Wynne GM. Compounds having CRTH2 antagonist activity. WO2009093026; 2009
   Google Scholar
• Armer RE, Maillol CEA, Dorgan CR, Compounds having CRTH2 antagonist activity. WO2009093029; 2009
   Google Scholar
• Available from: http://www.oxagen.co.uk/pdfs/CRTH2summary.pdf [Last accessed 7 February 2010]
   Google Scholar
• Bonnert R, Brough S, Cook T, Novel substituted indoles. WO2003101961; 2003
   Google Scholar
• Bonnert R, Dickinson M, Rasul R, Indole-3-sulphur derivatives and their use in the treatment of respiratory disorders. WO2004007451; 2004
   Google Scholar
• Bonnert RV, Luker TJ, Cumming J. Novel compounds. WO2007138282; 2007
   Google Scholar
• Bennani YL, Tumey LN, Gleason EA, Robarge MJ. Indole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof. WO2006034419; 2006
   Google Scholar
• Tumey LN, Robarge MJ, Gleason E, 3-Indolyl sultams as selective CRTh2 antagonists. Bioorg Med Chem Lett 2010;20:3287-90
   PubMed Web of Science ®Google Scholar
• Bennani YL, Tumey LN, Gleason EA, Robarge MJ. Preparation of benzimidazole acetic acids as CRTH2 receptor antagonists for the treatment of diseases responsive to inhibiting the binding of endogenous ligands to the CRTH2 receptors. WO2006034418; 2006
   Google Scholar
• Hynd G, Ray NC, Finch H, Indolizine derivatives. WO2006136859; 2006
   Google Scholar
• Hynd G, Ray NC, Finch H, Indolizine derivatives as ligands for the CRTH2 receptor. WO2007031747; 2007
   Google Scholar
• Hynd G, Ray NC, Finch H, CRTH2 antagonists. WO2008074966; 2008
   Google Scholar
• Hynd G, Montana J, Finch H, Indolizineacetic acids and their therapeutic use as ligands of the CRTH2 receptor. WO2008078069; 2008
   Google Scholar
• Hynd G, Ray NC, Finch H, Indolizine acetic acid derivatives as CRTH2 antagonists. WO2008113965; 2008
   Google Scholar
• Ray NC, Hynd G, Arienzo R, Finch H. 3-Aminoindole compounds as CRTH2 receptor ligands. WO2007045867; 2007
   Google Scholar
• Hynd G, Montana JG, Finch H, Indoles and their therapeutic use. WO2009077728; 2009
   Google Scholar
• Hynd G, Montana JG, Finch H. Indolizine derivatives with CRTH2 receptor affinity for the treatment of inflammatory diseases. WO2009044134; 2009
   Google Scholar
• Hynd G, Montana JG, Finch H, Indolizine derivatives with CRTH2 receptor affinity for the treatment of inflammatory diseases. WO2009044147; 2009
   Google Scholar
• Bartolini W, Cali BM, Chen B, Modulators of CRTH2, COX-2 and FAAH. WO2006036994; 2006
   Google Scholar
• Bartolini W, Cali BM, Chen B, Useful indole compounds. WO2007022501; 2007
   Google Scholar
• Bonafoux DF, Wu X. Thienopyrroles and pyrrolothiazoles as new therapeutic agents. WO2009102462; 2009
   Google Scholar
• Fecher A, Fretz H, Riederer M. 2,3,4,9-Tetrahydro-1H-carbazole derivatives as CRTH2 receptor antagonists. WO2006070325; 2006
   Google Scholar
• Fretz H, Fecher A, Hilpert K, Riederer M. Preparation of (2-sulfanyl-benzimidazol-1-yl)acetic acid derivatives as CRTH2 antagonists. WO2006021418; 2006
   Google Scholar
• Schwarz M, Sebille E, Cleva C, Tricyclic spiro derivatives as CRTH2 modulators. WO2006125784; 2006
   Google Scholar
• Crosignani S, Page P, Missotten M, Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases. J Med Chem 2008;51:2227-43
   PubMed Web of Science ®Google Scholar
• Stearns BA, Truong YP, Hutchinson JH. Antagonists of PGD2 receptors. WO2009061676; 2009
   Google Scholar
• Stearns BA, Hutchinson JH. Antagonists of PGD2 receptors. WO2009061681; 2009
   Google Scholar
• Wang Z. Preparation of indole derivatives as CRTH2 receptor antagonists. WO2007019675; 2007
   Google Scholar
• Yuan WW. Heterocyclic compounds as CRTH2 receptor antagonists. WO2009049021; 2009
   Google Scholar
• Adcock C, Leblanc C, Sandham DA, Pyrrole derivatives having CRTH2 receptor antagonists activity. WO2006063763; 2006
   Google Scholar
• Sandham DA, Leblanc C, Adcock C, Pyrrole derivatives with CRTh2 receptor modulator activity. WO2007144127; 2007
   Google Scholar
• Sandham DA. Organic compounds. WO2007065684; 2007
   Google Scholar
• Brown LN, Leblanc C, Sandham DA, Singh HP. Aryl acetic acid and ester derivatives and their uses as antiinflammatory agents. WO2007065683; 2007
   Google Scholar
• Sandham DA, Leblanc C, Brown LN. Bicyclic heterocyclic compounds as antiinflammatory agents. WO2007065924; 2007
   Google Scholar
• Bonnert R, Brough S, Davies A, Novel compounds. WO2004089885; 2004
   Google Scholar
• Sandham DA, Turner KL, Leblanc C. Preparation of substituted phenoxyacetic acids as CRTh2 receptor antagonists for treating inflammatory or allergic condition. WO2005105727; 2005
   Google Scholar
• Ulven T, Frimurer T, Rist O, CRTH2 receptor ligands for therapeutic use. WO2005115382; 2005
   Google Scholar
• Bonnert RV, Patel A, Thom S. Novel compounds. WO2005018529; 2005
   Google Scholar
• Bonnert RV, Alcaraz L, Mohammed RT, Preparation of phenoxyacetic acids for treatment of respiratory diseases. WO2006056752; 2006
   Google Scholar
• Luker TJ, Mohammed RT, Dickinson M, Thom S. Biphenyloxyacetic acid derivatives for the treatment of respiratory disease. WO2007039741; 2007
   Google Scholar
• Bonnert RV, Luker TJ, Patel A, Rigby A. A biphenyloxypropanoic acid as CRTH2 modulator and intermediates. WO2009004379; 2009
   Google Scholar
• Baettig U, Cox B, Janus D, Organic compounds. WO2006125593; 2006
   Google Scholar
• Axford J, Baettig U, Cox B, Organic compounds for the treatment of inflammatory or allergic conditions. WO2006125596; 2006
   Google Scholar
• Frimurer TM, Ulven T, Hogberg T, Elling CE. A pseudo-sequence method for comparing seven-transmembrane receptors with respect to the physico-chemical properties of their binding sites, and drug discovery uses. WO2004079625; 2004
   Google Scholar
• Frimurer TM, Ulven T, Elling CE, A physicogenetic method to assign ligand-binding relationships between 7TM receptors. Bioorg Med Chem Lett 2005;15:3707-12
   PubMedGoogle Scholar
• Ulven T, Frimurer T, Rist O, CRTH2 receptor ligands for therapeutic use. WO2005115374; 2005
   Google Scholar
• Ulven T, Frimurer T, Rist O, Substituted thiazoleacetic acids as CRTH2 receptor ligands. WO2005116001; 2005
   Google Scholar
• Ulven T, Frimurer T, Rist O, Phenoxyacetic acid derivatives as CRTH2 receptor ligands. WO2007062678; 2007
   Google Scholar
• Receveur J-M, Christensen A, Grimstrup M, Hoegberg T. Oxadiazole derivatives with CRTH2 receptor activity. WO2007062773; 2007
   Google Scholar
• Terasaka T, Zenkoh T, Hayashida H, Polycyclic acid compounds useful as CRTH2 antagonists and antiallergic agents and their preparation and use in the treatment of diseases. WO2008072784; 2008
   Google Scholar
• McGuinness BF, Le TXH, Duo J, Ho K-K. 2-Phenylphenoxyacetic acids useful for treating inflammatory disorders. WO2009089192; 2009
   Google Scholar
• Cramp MC, Arienzo R, Hynd G, Quinolines and their therapeutic use. WO2007036743; 2007
   Google Scholar
• Hynd G, Harris NV, Bull RJ, 2-Oxo-2H-chromene compounds. WO2007144625; 2007
   Google Scholar
• Montana JG, Finch H, Hynd G, Quinolines and their therapeutic use. WO2008122784; 2008
   Google Scholar
• Ray NC, Finch H, Cramp MC, Quinoline derivatives as CRTH2 receptor ligands. WO2008119917; 2008
   Google Scholar
• Hynd G, Montana JG, Finch H, 6,6-Fused bicyclic aromatic compounds and their therapeutic use. WO2009060209; 2009
   Google Scholar
• Grimstrup M, Rist O, Receveur J-M, Amino-substituted aza-heterocyclic compounds for treating inflammatory conditions. WO2007062797; 2007
   Google Scholar
• Ulven T, Frimurer T, Rist O, Thiazolyl- and pyrimidinyl-acetic acids and their use as CRTH2 receptor ligands. WO2007062677; 2007
   Google Scholar
• Grimstrup M, Receveur JM, Rist O, Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. Bioorg Med Chem Lett 2010;20:1638-41
   PubMed Web of Science ®Google Scholar
• Fu Z, Huang XA, Liu J, Asthma and allergic inflammation modulators. WO2004058164; 2004
   Google Scholar
• Jones TR, Labelle M, Belley M, Pharmacology of montelukast sodium (Singulair), a potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol 1995;73:191-201
   PubMed Web of Science ®Google Scholar
• Grillo M, Li A-R, Liu J, Phenylacetic acid derivatives as inflammation modulators. WO2009085177; 2009
   Google Scholar
• Brown M, Johnson MG, Li A-R, Compounds and methods useful for treating asthma and allergic inflammation. WO2008137027; 2008
   Google Scholar
• Wong SG, Fan PW, Subramanian R, Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-Helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction. Drug Metab Dispos 2010;38:841-50
   PubMedGoogle Scholar
• Philip G, van Adelsberg J, Loeys T, Clinical studies of the DP1 antagonist laropiprant in asthma and allergic rhinitis. J Allergy Clin Immunol 2009;124:942-8
   PubMed Web of Science ®Google Scholar
• Available form: http://www.shionogi.co.jp/ir_en/news/detail/e_061027.pdf [Last accessed 9 September 2010]
   Google Scholar
• Wie LT, Koriyama Y, Yoshino T, Pyrimidinylacetic acid derivatives, useful as CRTH2 antagonists. EP1471057; 2004
   Google Scholar
• Ly TW, Koriyama Y, Yoshino T, Pyrimidine derivatives useful for the treatment of diseases mediated by CRTH2. WO2004096777; 2004
   Google Scholar
• Ly T-W, Yoshino T, Takekawa Y, Imidazo[1,2-c]pyrimidinylacetic acid derivatives. WO2005073234; 2005
   Google Scholar
• Ly TW, Raaum ED, Tran MCSY. Alkylthio pyrimidines as CRTH2 antagonists. WO2009042138; 2009
   Google Scholar
• Ly TW, Potter GT, Tran MCSY. 2-S-Benzyl substituted pyrimidines as CRTH2 antagonists. WO2009042139; 2009
   Google Scholar
• Ly TW, Li H-Y. Particulates of a CRTH2 antagonist. WO2008156780; 2008
   Google Scholar
• Ly TW. Amine salts of a CRTH2 antagonist. WO2008156781; 2008
   Google Scholar
• Hutchinson JH, Seiders TJ, Stearns BA, Cyclic diaryl ether compounds as antagonists of prostaglandin D2 receptors. WO2009102893; 2009
   Google Scholar
• Hutchinson JH, Stearns BA, Seiders TJ, Antagonists of prostaglandin D2 receptors. WO2009108720; 2009
   Google Scholar
• Hutchinson JH, Stearns BA, Scott JM, N,N-Disubstituted aminoalkylbiphenyl antagonists of prostaglandin D2 receptors. US2009197959; 2009
   Google Scholar
• Stebbins KJ, Broadhead AR, Correa LD, Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation. Eur J Pharmacol 2010;638:142-9
   PubMed Web of Science ®Google Scholar
• Doherty G, Cook A. 4-Substituted phenoxyphenylacetic acid derivatives. WO2008024746; 2008
   Google Scholar
• Doherty G. 4-Heteroaryl-substituted phenoxyphenylacetic acids. WO2009061730; 2009
   Google Scholar
• Terasaka T, Matsuda H, Ito S, Tasaki M. Polycyclic acid compounds useful as CRTH2 antagonists and antiallergic agents. WO2009096526; 2009
   Google Scholar
• Dudler T, Farouz F, Fowley K, Substituted phenylacetic acids as DP-2 antagonists. WO2007146838; 2007
   Google Scholar
• Page P, Schwarz M, Sebille E, 2,3-Substituted pyrazine sulfonamides. WO2006111560; 2006
   Google Scholar
• Ghosh S, Elder AM, Carson KG, PGD2 receptor antagonists for the treatment of inflammatory diseases. WO2004032848; 2004
   Google Scholar
• Kuhn C, Feru F, Bazin M, A preparation of tetrahydroquinoline derivatives as CRTH2 antagonists. EP1413306; 2004
   Google Scholar
• Kuhn C, Feru F, Bazin M, Quinoline derivatives as CRTH2 antagonists. EP1435356; 2004
   Google Scholar
• Awad MMA, Bazin M, Feru F, Tetrahydroquinoline derivatives as CRTh2 antagonists. WO2004035543; 2004
   Google Scholar
• Inman WD, Liu J, Medina JC, Asthma and allergic inflammation modulators. WO2005007094; 2005
   Google Scholar
• Little JD, Ghosh S, Harrison S, PGD2 receptor antagonists for the treatment of inflammatory diseases. WO2006091674; 2006
   Google Scholar
• Barnes N, Pavord I, Chuchalin A, A randomised, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 on moderate persistent asthma. Euro Res J 2009;34(Suppl. 53):564s-565s
   Google Scholar
• Availabe from: http://www.actelion.com/documents/corporate/fact_sheets/FS_ClinicalDevelopment.pdf [Last visited 20 June 2010]
   Google Scholar
• Available from: http://clinicaltrials.gov/ct2/show/NCT00967356?term=AZD-5985&rank=2 [Last accessed 9 September 2010]
   Google Scholar
• Availabe from: http://clinicaltrials.gov/ct2/show/NCT00787072?term=AZD-8075&rank=2 [Last visited 9 September 2010]
   Google Scholar
• Availabe from: http://clinicaltrials.gov/ct2/show/NCT00690482?term=AZD1981&rank=9 [Last accessed 9 September 2010]
   Google Scholar
• Available from: http://www.amirapharm.com/articles/Amira%20AM461%20Clinical%20Announcement.html [Last accessed 20 June 2010]
   Google Scholar
• Available from: http://www.amirapharm.com/articles/Amira%20AM461%20Press%20Release%20_5-20-2010.pdf [Last accessed 20 June 2010]
   Google Scholar
• Ichinose M. Differences of inflammatory mechanisms in asthma and COPD. Allergol Int 2009;58:307-13
   PubMedGoogle Scholar
• Nantel F, Fong C, Lamontagne S, Expression of prostaglandin D synthase and the prostaglandin D2 receptors DP and CRTH2 in human nasal mucosa. Prostaglandins Other Lipid Mediat 2004;73:87-101
   PubMed Web of Science ®Google Scholar
• Stebbins KJ, Evans JF, Lorrain DS. DP2 Receptor antagonists: novel therapeutic target for COPD. Mol Cell Pharmacol 2010;2:89-96
   Google Scholar
• Shichijo M, Sugimoto H, Nagao K, Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats. J Pharmacol Exp Ther 2003;307:518-25
   PubMedGoogle Scholar
• Ishizuka T, Matsui T, Okamoto Y, Ramatroban (BAY u 3405): A novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D-2 receptor. Cardiovascular Drug Rev 2004;22:71-90
   PubMed Web of Science ®Google Scholar
• Available from: http://astrazeneca.com/research/our-pipeline-summary/ [Last accessed 20 June 2010]
   Google Scholar
• Available from: http://www.oxagen.co.uk/crth2.htm [Last accessed 20 June 2010]
   Google Scholar
• Available from: http://wwwext.amgen.com/science/pipe_amg_853.html [Last visited 20 June 2010]
   Google Scholar
• Available from: http://www.actimis.com/actimisBI6172008.pdf [Last accessed 20 June 2010]
   Google Scholar
• Available from: http://clinicaltrialsfeeds.org/clinical-trials/show/NCT00784732 [Last accessed 20 June 2010]
   Google Scholar
• Bell S, Anderson L, Nugent C, Safety, PK and PD of ARRY-502, a CRTh2 antagonist, in healthy subjects with a history of seasonal allergies. European Respiratory Society Annual Congress, Barcelona 2010, abstract nr. 3954. [https://www.ersnetsecure.org/public/prg_congres.abstract?ww_i_presentation=47267]
   Google Scholar