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Page 1
Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.
Scott JM, Baccei C, Bain G, Broadhead A, Evans JF, Fagan P, Hutchinson JH, King C, Lorrain DS, Lee C, Prasit P, Prodanovich P, Santini A, Stearns BA. Scott JM, et al. Among authors: king c. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6608-12. doi: 10.1016/j.bmcl.2011.01.024. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21958540
5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).
Hutchinson JH, Li Y, Arruda JM, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King CD, Lee C, Lorrain D, Prodanovich P, Rong H, Santini A, Stock N, Prasit P, Evans JF. Hutchinson JH, et al. Among authors: king cd. J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d. J Med Chem. 2009. PMID: 19739647
Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.
Stebbins KJ, Broadhead AR, Baccei CS, Scott JM, Truong YP, Coate H, Stock NS, Santini AM, Fagan P, Prodanovich P, Bain G, Stearns BA, King CD, Hutchinson JH, Prasit P, Evans JF, Lorrain DS. Stebbins KJ, et al. J Pharmacol Exp Ther. 2010 Mar;332(3):764-75. doi: 10.1124/jpet.109.161919. Epub 2009 Dec 8. J Pharmacol Exp Ther. 2010. PMID: 19996299
Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.
Bain G, Lorrain DS, Stebbins KJ, Broadhead AR, Santini AM, Prodanovich P, Darlington J, King CD, Lee C, Baccei C, Stearns B, Troung Y, Hutchinson JH, Prasit P, Evans JF. Bain G, et al. Among authors: king cd. J Pharmacol Exp Ther. 2011 Jul;338(1):290-301. doi: 10.1124/jpet.111.180430. Epub 2011 Apr 12. J Pharmacol Exp Ther. 2011. PMID: 21487069
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P. Stock NS, et al. Among authors: king cd. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22059882
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP. Stearns BA, et al. Among authors: king c. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085. Epub 2009 Jun 25. Bioorg Med Chem Lett. 2009. PMID: 19608418
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Stock N, Baccei C, Bain G, Broadhead A, Chapman C, Darlington J, King C, Lee C, Li Y, Lorrain DS, Prodanovich P, Rong H, Santini A, Zunic J, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: king c. Bioorg Med Chem Lett. 2010 Jan 1;20(1):213-7. doi: 10.1016/j.bmcl.2009.10.131. Epub 2009 Oct 31. Bioorg Med Chem Lett. 2010. PMID: 19914828
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
Stock N, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Schaab K, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: king c. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4598-601. doi: 10.1016/j.bmcl.2010.06.011. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20566292
Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Stock N, Volkots D, Stebbins K, Broadhead A, Stearns B, Roppe J, Parr T, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: king c. Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. doi: 10.1016/j.bmcl.2010.12.016. Epub 2010 Dec 9. Bioorg Med Chem Lett. 2011. PMID: 21211969
4,137 results