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Items: 1 to 20 of 111

1.

Zwitterionic CRTh2 antagonists.

Luker T, Bonnert R, Paine SW, Schmidt J, Sargent C, Cook AR, Cook A, Gardiner P, Hill S, Weyman-Jones C, Patel A, Thom S, Thorne P.

J Med Chem. 2011 Mar 24;54(6):1779-88. doi: 10.1021/jm1014549. Epub 2011 Feb 28.

PMID:
21355602
2.

Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.

Sykes DA, Bradley ME, Riddy DM, Willard E, Reilly J, Miah A, Bauer C, Watson SJ, Sandham DA, Dubois G, Charlton SJ.

Mol Pharmacol. 2016 May;89(5):593-605. doi: 10.1124/mol.115.101832. Epub 2016 Feb 25.

3.

Delta12-prostaglandin D2 is a potent and selective CRTH2 receptor agonist and causes activation of human eosinophils and Th2 lymphocytes.

Gazi L, Gyles S, Rose J, Lees S, Allan C, Xue L, Jassal R, Speight G, Gamble V, Pettipher R.

Prostaglandins Other Lipid Mediat. 2005 Jan;75(1-4):153-67.

PMID:
15789622
4.

Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.

Luker T, Bonnert R, Schmidt J, Sargent C, Paine SW, Thom S, Pairaudeau G, Patel A, Mohammed R, Akam E, Dougall I, Davis AM, Abbott P, Brough S, Millichip I, McInally T.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3616-21. doi: 10.1016/j.bmcl.2011.04.101. Epub 2011 Apr 28.

PMID:
21592791
5.

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.

Sandham DA, Arnold N, Aschauer H, Bala K, Barker L, Brown L, Brown Z, Budd D, Cox B, Docx C, Dubois G, Duggan N, England K, Everatt B, Furegati M, Hall E, Kalthoff F, King A, Leblanc CJ, Manini J, Meingassner J, Profit R, Schmidt A, Simmons J, Sohal B, Stringer R, Thomas M, Turner KL, Walker C, Watson SJ, Westwick J, Willis J, Williams G, Wilson C.

Bioorg Med Chem. 2013 Nov 1;21(21):6582-91. doi: 10.1016/j.bmc.2013.08.025. Epub 2013 Aug 22.

PMID:
24021582
6.

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.

Mimura H, Ikemura T, Kotera O, Sawada M, Tashiro S, Fuse E, Ueno K, Manabe H, Ohshima E, Karasawa A, Miyaji H.

J Pharmacol Exp Ther. 2005 Jul;314(1):244-51. Epub 2005 Mar 29.

7.

Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils.

Pettipher R, Vinall SL, Xue L, Speight G, Townsend ER, Gazi L, Whelan CJ, Armer RE, Payton MA, Hunter MG.

J Pharmacol Exp Ther. 2012 Feb;340(2):473-82. doi: 10.1124/jpet.111.187203. Epub 2011 Nov 21.

8.

Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.

Crosignani S, PrĂȘtre A, Jorand-Lebrun C, Fraboulet G, Seenisamy J, Augustine JK, Missotten M, Humbert Y, Cleva C, Abla N, Daff H, Schott O, Schneider M, Burgat-Charvillon F, Rivron D, Hamernig I, Arrighi JF, Gaudet M, Zimmerli SC, Juillard P, Johnson Z.

J Med Chem. 2011 Oct 27;54(20):7299-317. doi: 10.1021/jm200866y. Epub 2011 Oct 3.

PMID:
21916510
9.

Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.

Armer RE, Ashton MR, Boyd EA, Brennan CJ, Brookfield FA, Gazi L, Gyles SL, Hay PA, Hunter MG, Middlemiss D, Whittaker M, Xue L, Pettipher R.

J Med Chem. 2005 Oct 6;48(20):6174-7.

PMID:
16190744
10.

Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.

Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, Thomason J, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E.

J Med Chem. 2012 Jun 14;55(11):5088-109. doi: 10.1021/jm300007n. Epub 2012 May 31.

PMID:
22651823
11.

Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981.

Luker T, Bonnert R, Brough S, Cook AR, Dickinson MR, Dougall I, Logan C, Mohammed RT, Paine S, Sanganee HJ, Sargent C, Schmidt JA, Teague S, Thom S.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6288-92. doi: 10.1016/j.bmcl.2011.08.124. Epub 2011 Sep 5.

PMID:
21944852
12.

4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.

Procopiou PA, Ancliff RA, Bamford MJ, Browning C, Connor H, Davies S, Fogden YC, Hodgson ST, Holmes DS, Looker BE, Morriss KM, Parr CA, Pickup EA, Sehmi SS, White GV, Watts CJ, Wilson DM, Woodrow MD.

J Med Chem. 2007 Dec 27;50(26):6706-17. Epub 2007 Dec 6.

PMID:
18052318
13.

Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.

Crosignani S, Page P, Missotten M, Colovray V, Cleva C, Arrighi JF, Atherall J, Macritchie J, Martin T, Humbert Y, Gaudet M, Pupowicz D, Maio M, Pittet PA, Golzio L, Giachetti C, Rocha C, Bernardinelli G, Filinchuk Y, Scheer A, Schwarz MK, Chollet A.

J Med Chem. 2008 Apr 10;51(7):2227-43. doi: 10.1021/jm701383e. Epub 2008 Mar 5.

PMID:
18318469
14.

Tetrahydroquinoline derivatives as CRTH2 antagonists.

Liu J, Wang Y, Sun Y, Marshall D, Miao S, Tonn G, Anders P, Tocker J, Tang HL, Medina J.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6840-4. doi: 10.1016/j.bmcl.2009.10.094. Epub 2009 Oct 25.

PMID:
19896843
15.

Prostaglandin H2 induces the migration of human eosinophils through the chemoattractant receptor homologous molecule of Th2 cells, CRTH2.

Schuligoi R, Sedej M, Waldhoer M, Vukoja A, Sturm EM, Lippe IT, Peskar BA, Heinemann A.

J Leukoc Biol. 2009 Jan;85(1):136-45. doi: 10.1189/jlb.0608387. Epub 2008 Oct 3.

PMID:
18835884
16.

15R-methyl-prostaglandin D2 is a potent and selective CRTH2/DP2 receptor agonist in human eosinophils.

Monneret G, Cossette C, Gravel S, Rokach J, Powell WS.

J Pharmacol Exp Ther. 2003 Jan;304(1):349-55.

17.

Discovery of novel N-aryl piperazine CXCR4 antagonists.

Zhao H, Prosser AR, Liotta DC, Wilson LJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4950-5. doi: 10.1016/j.bmcl.2015.04.036. Epub 2015 Apr 17.

PMID:
25935642
18.

Discovery of novel and potent CRTH2 antagonists.

Ito S, Terasaka T, Zenkoh T, Matsuda H, Hayashida H, Nagata H, Imamura Y, Kobayashi M, Takeuchi M, Ohta M.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1194-7. doi: 10.1016/j.bmcl.2011.11.079. Epub 2011 Nov 28.

PMID:
22178554
19.

7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.

Sandham DA, Adcock C, Bala K, Barker L, Brown Z, Dubois G, Budd D, Cox B, Fairhurst RA, Furegati M, Leblanc C, Manini J, Profit R, Reilly J, Stringer R, Schmidt A, Turner KL, Watson SJ, Willis J, Williams G, Wilson C.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. doi: 10.1016/j.bmcl.2009.06.042. Epub 2009 Jun 14.

PMID:
19592244
20.

2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.

Sandham DA, Aldcroft C, Baettig U, Barker L, Beer D, Bhalay G, Brown Z, Dubois G, Budd D, Bidlake L, Campbell E, Cox B, Everatt B, Harrison D, Leblanc CJ, Manini J, Profit R, Stringer R, Thompson KS, Turner KL, Tweed MF, Walker C, Watson SJ, Whitebread S, Willis J, Williams G, Wilson C.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.

PMID:
17531480

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