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Page 1
Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.
Guay D, Beaulieu C, Belley M, Crane SN, DeLuca J, Gareau Y, Hamel M, Henault M, Hyjazie H, Kargman S, Chan CC, Xu L, Gordon R, Li L, Mamane Y, Morin N, Mancini J, Thérien M, Tranmer G, Truong VL, Wang Z, Black WC. Guay D, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2011 May 15;21(10):2832-5. doi: 10.1016/j.bmcl.2011.03.084. Epub 2011 Mar 30. Bioorg Med Chem Lett. 2011. PMID: 21507642
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.
Gauthier JY, Belley M, Deschênes D, Fournier JF, Gagné S, Gareau Y, Hamel M, Hénault M, Hyjazie H, Kargman S, Lavallée G, Levesque JF, Li L, Mamane Y, Mancini J, Morin N, Mulrooney E, Robichaud J, Thérien M, Tranmer G, Wang Z, Wu J, Black WC. Gauthier JY, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2011 May 15;21(10):2836-9. doi: 10.1016/j.bmcl.2011.03.081. Epub 2011 Mar 31. Bioorg Med Chem Lett. 2011. PMID: 21507640
Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14).
Robichaud J, Fournier JF, Gagné S, Gauthier JY, Hamel M, Han Y, Hénault M, Kargman S, Levesque JF, Mamane Y, Mancini J, Morin N, Mulrooney E, Wu J, Black WC. Robichaud J, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4366-8. doi: 10.1016/j.bmcl.2010.12.113. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21689930
Identification of an indole series of prostaglandin D2 receptor antagonists.
Sturino CF, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Brideau C, Cauchon E, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, O'Neill G, Wang Z, Zamboni R, Metters KM, Young RN. Sturino CF, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2006 Jun 1;16(11):3043-8. doi: 10.1016/j.bmcl.2006.02.062. Epub 2006 Mar 10. Bioorg Med Chem Lett. 2006. PMID: 16529930
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
Prasit P, Wang Z, Brideau C, Chan CC, Charleson S, Cromlish W, Ethier D, Evans JF, Ford-Hutchinson AW, Gauthier JY, Gordon R, Guay J, Gresser M, Kargman S, Kennedy B, Leblanc Y, Léger S, Mancini J, O'Neill GP, Ouellet M, Percival MD, Perrier H, Riendeau D, Rodger I, Zamboni R, et al. Prasit P, et al. Among authors: kargman s. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1773-8. doi: 10.1016/s0960-894x(99)00288-7. Bioorg Med Chem Lett. 1999. PMID: 10406640
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Ducharme Y, Blouin M, Carrière MC, Chateauneuf A, Côté B, Denis D, Frenette R, Greig G, Kargman S, Lamontagne S, Martins E, Nantel F, O'Neill G, Sawyer N, Metters KM, Friesen RW. Ducharme Y, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1155-60. doi: 10.1016/j.bmcl.2004.12.005. Bioorg Med Chem Lett. 2005. PMID: 15686932
From indomethacin to a selective COX-2 inhibitor. Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors.
Lau CK, Black WC, Belley M, Chan C, Charleson S, Denis D, Gauthier JY, Gordon R, Guay D, Hamel P, Kargman S, Leblanc Y, Mancini J, Ouellet M, Percival D, Prasit P, Roy P, Skorey K, Tagari P, Vickers P, Wong E. Lau CK, et al. Among authors: kargman s. Adv Exp Med Biol. 1997;407:73-8. Adv Exp Med Biol. 1997. PMID: 9321934 No abstract available.
65 results