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31 results

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Page 1
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Velcicky J, Mathison CJN, Nikulin V, Pflieger D, Epple R, Azimioara M, Cow C, Michellys PY, Rigollier P, Beisner DR, Bodendorf U, Guerini D, Liu B, Wen B, Zaharevitz S, Brandl T. Velcicky J, et al. Among authors: michellys py. ACS Med Chem Lett. 2019 May 23;10(6):887-892. doi: 10.1021/acsmedchemlett.9b00044. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223443 Free PMC article.
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
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
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Michellys PY, Chen B, Jiang T, Jin Y, Lu W, Marsilje TH, Pei W, Uno T, Zhu X, Wu B, Nguyen TN, Bursulaya B, Lee C, Li N, Kim S, Tuntland T, Liu B, Sun F, Steffy A, Hood T. Michellys PY, et al. Bioorg Med Chem Lett. 2016 Feb 1;26(3):1090-1096. doi: 10.1016/j.bmcl.2015.11.049. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26750252
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.
Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeill M, Lu W, Harris J, Bender S, Wong KK, Jänne PA, Eck MJ. Jia Y, et al. Among authors: michellys py. Nature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25. Nature. 2016. PMID: 27251290 Free PMC article.
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Lelais G, et al. Among authors: michellys py. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19. J Med Chem. 2016. PMID: 27433829
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.
He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S, Jia Y, Bursulaya B, Kreusch A, Gao MY, Spraggon G, Baaten J, Clemmer L, Meeusen S, Huang D, Hill R, Nguyen-Tran V, Fathman J, Liu B, Tuntland T, Gordon P, Hollenbeck T, Ng K, Shi J, Bordone L, Liu H. He X, et al. Among authors: michellys py. ACS Med Chem Lett. 2017 Sep 27;8(10):1048-1053. doi: 10.1021/acsmedchemlett.7b00258. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057049 Free PMC article.
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Alper PB, Deane J, Betschart C, Buffet D, Collignon Zipfel G, Gordon P, Hampton J, Hawtin S, Ibanez M, Jiang T, Junt T, Knoepfel T, Liu B, Maginnis J, McKeever U, Michellys PY, Mutnick D, Nayak B, Niwa S, Richmond W, Rush JS, Syka P, Zhang Y, Zhu X. Alper PB, et al. Among authors: michellys py. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127366. doi: 10.1016/j.bmcl.2020.127366. Epub 2020 Jun 24. Bioorg Med Chem Lett. 2020. PMID: 32738975
31 results