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Page 1
Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H. Levell J, et al. Among authors: gardyan m. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.
Han Q, Pabba PK, Barbosa J, Mabon R, Healy JP, Gardyan MW, Terranova KM, Brommage R, Thompson AY, Schmidt JM, Wilson AG, Xu X, Tarver JE Jr, Carson KG. Han Q, et al. Among authors: gardyan mw. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1184-7. doi: 10.1016/j.bmcl.2016.01.038. Epub 2016 Jan 18. Bioorg Med Chem Lett. 2016. PMID: 26821819
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.
Harrison BA, Whitlock NA, Voronkov MV, Almstead ZY, Gu KJ, Mabon R, Gardyan M, Hamman BD, Allen J, Gopinathan S, McKnight B, Crist M, Zhang Y, Liu Y, Courtney LF, Key B, Zhou J, Patel N, Yates PW, Liu Q, Wilson AG, Kimball SD, Crosson CE, Rice DS, Rawlins DB. Harrison BA, et al. Among authors: gardyan m. J Med Chem. 2009 Nov 12;52(21):6515-8. doi: 10.1021/jm901226j. J Med Chem. 2009. PMID: 19831390
Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.
Bagdanoff JT, Donoviel MS, Nouraldeen A, Tarver J, Fu Q, Carlsen M, Jessop TC, Zhang H, Hazelwood J, Nguyen H, Baugh SD, Gardyan M, Terranova KM, Barbosa J, Yan J, Bednarz M, Layek S, Courtney LF, Taylor J, Digeorge-Foushee AM, Gopinathan S, Bruce D, Smith T, Moran L, O'Neill E, Kramer J, Lai Z, Kimball SD, Liu Q, Sun W, Yu S, Swaffield J, Wilson A, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. Among authors: gardyan m. J Med Chem. 2009 Jul 9;52(13):3941-53. doi: 10.1021/jm900278w. J Med Chem. 2009. PMID: 19489538
Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.
Harrison BA, Almstead ZY, Burgoon H, Gardyan M, Goodwin NC, Healy J, Liu Y, Mabon R, Marinelli B, Samala L, Zhang Y, Stouch TR, Whitlock NA, Gopinathan S, McKnight B, Wang S, Patel N, Wilson AG, Hamman BD, Rice DS, Rawlins DB. Harrison BA, et al. Among authors: gardyan m. ACS Med Chem Lett. 2014 Nov 24;6(1):84-8. doi: 10.1021/ml500367g. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589936 Free PMC article.