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Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA. Boga SB, et al. Among authors: yu y. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18. Bioorg Med Chem Lett. 2017. PMID: 28720503
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, Rokosz LL, Kaiser B, Li G, Wang W, Stauffer T, Ozgur L, Baldwin J, Taveras AG. Dwyer MP, et al. Among authors: yu y. J Med Chem. 2006 Dec 28;49(26):7603-6. doi: 10.1021/jm0609622. J Med Chem. 2006. PMID: 17181143
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
Chao J, Taveras AG, Chao J, Aki C, Dwyer M, Yu Y, Purakkattle B, Rindgen D, Jakway J, Hipkin W, Fosetta J, Fan X, Lundell D, Fine J, Minnicozzi M, Phillips J, Merritt JR. Chao J, et al. Among authors: yu y. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3778-83. doi: 10.1016/j.bmcl.2007.04.016. Epub 2007 Apr 10. Bioorg Med Chem Lett. 2007. PMID: 17459706
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
Biju P, Taveras A, Yu Y, Zheng J, Chao J, Rindgen D, Jakway J, Hipkin RW, Fossetta J, Fan X, Fine J, Qiu H, Merritt JR, Baldwin JJ. Biju P, et al. Among authors: yu y. Bioorg Med Chem Lett. 2008 Jan 1;18(1):228-31. doi: 10.1016/j.bmcl.2007.10.094. Epub 2007 Oct 30. Bioorg Med Chem Lett. 2008. PMID: 18006311
3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.
Biju P, Taveras AG, Yu Y, Zheng J, Hipkin RW, Fossetta J, Fan X, Fine J, Lundell D. Biju P, et al. Among authors: yu y. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1434-7. doi: 10.1016/j.bmcl.2009.01.027. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19200721
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Xiao D, Zhu X, Yu Y, Shao N, Wu J, McCormick KD, Dhondi P, Qin J, Mazzola R, Tang H, Rao A, Siliphaivanh P, Qiu H, Yang X, Rivelli M, Garlisi CG, Eckel S, Mukhopadhyay G, Correll C, Rindgen D, Aslanian R, Palani A. Xiao D, et al. Among authors: yu y. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1615-20. doi: 10.1016/j.bmcl.2014.01.043. Epub 2014 Feb 2. Bioorg Med Chem Lett. 2014. PMID: 24556380
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: yu y. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
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