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Page 1
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Azimioara M, et al. Among authors: michellys py. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13. Bioorg Med Chem Lett. 2014. PMID: 25455488
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.
Michellys PY, Ardecky RJ, Chen JH, Crombie DL, Etgen GJ, Faul MM, Faulkner AL, Grese TA, Heyman RA, Karanewsky DS, Klausing K, Leibowitz MD, Liu S, Mais DA, Mapes CM, Marschke KB, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Boehm MF. Michellys PY, et al. J Med Chem. 2003 Jun 19;46(13):2683-96. doi: 10.1021/jm020340q. J Med Chem. 2003. PMID: 12801232
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Michellys PY, Ardecky RJ, Chen JH, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Montrose-Rafizadeh C, Ogilvie KM, Reifel-Miller A, Rungta D, Thompson AW, Tyhonas JS, Boehm MF. Michellys PY, et al. J Med Chem. 2003 Sep 11;46(19):4087-103. doi: 10.1021/jm020401k. J Med Chem. 2003. PMID: 12954061
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Marsilje TH, et al. Among authors: michellys py. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
Syk inhibitors with high potency in presence of blood.
Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H. Thoma G, et al. Among authors: michellys py. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. doi: 10.1016/j.bmcl.2014.03.075. Epub 2014 Apr 3. Bioorg Med Chem Lett. 2014. PMID: 24726806
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Alper P, et al. Among authors: michellys py. Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023. Epub 2014 Mar 27. Bioorg Med Chem Lett. 2014. PMID: 24751443
31 results