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475 related items for PubMed ID: 31368705

  • 1. Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
    Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L.
    J Med Chem; 2019 Sep 12; 62(17):7643-7655. PubMed ID: 31368705
    [Abstract] [Full Text] [Related]

  • 2. Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
    Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z.
    J Med Chem; 2019 Sep 12; 62(17):7923-7940. PubMed ID: 31381333
    [Abstract] [Full Text] [Related]

  • 3. Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models.
    Haselmayer P, Camps M, Liu-Bujalski L, Nguyen N, Morandi F, Head J, O'Mahony A, Zimmerli SC, Bruns L, Bender AT, Schroeder P, Grenningloh R.
    J Immunol; 2019 May 15; 202(10):2888-2906. PubMed ID: 30988116
    [Abstract] [Full Text] [Related]

  • 4. Discovery and biological evaluation of N-(3-(7-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-4-methyl-2-oxo-2H-pyrimido[4,5-d][1,3]oxazin-1(4H)-yl)phenyl)acrylamide as potent Bruton's tyrosine kinase inhibitors.
    Lai MZ, Song PR, Dou D, Diao YY, Tong LJ, Zhang T, Xie H, Li HL, Ding J.
    Acta Pharmacol Sin; 2020 Mar 15; 41(3):415-422. PubMed ID: 31316181
    [Abstract] [Full Text] [Related]

  • 5. Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition.
    Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, Brendza KM, Lutz JD, Keegan KS, Ray AS, Schultz BE, Sakowicz R, Feng JY.
    Biochim Biophys Acta Gen Subj; 2020 Apr 15; 1864(4):129531. PubMed ID: 31953125
    [Abstract] [Full Text] [Related]

  • 6. Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis.
    Montalban X, Arnold DL, Weber MS, Staikov I, Piasecka-Stryczynska K, Willmer J, Martin EC, Dangond F, Syed S, Wolinsky JS, Evobrutinib Phase 2 Study Group.
    N Engl J Med; 2019 Jun 20; 380(25):2406-2417. PubMed ID: 31075187
    [Abstract] [Full Text] [Related]

  • 7. HZ-A-005, a potent, selective, and covalent Bruton's tyrosine kinase inhibitor in preclinical development.
    Huang W, Wang S, Zhang Z, Zhang C, Zeng S, Liang M, Shen Z, Liu X.
    Bioorg Chem; 2020 Dec 20; 105():104377. PubMed ID: 33091668
    [Abstract] [Full Text] [Related]

  • 8. Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
    Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA.
    J Med Chem; 2019 Apr 11; 62(7):3228-3250. PubMed ID: 30893553
    [Abstract] [Full Text] [Related]

  • 9. Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
    Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B.
    Bioorg Med Chem Lett; 2018 Sep 15; 28(17):2939-2944. PubMed ID: 30122225
    [Abstract] [Full Text] [Related]

  • 10. Safety, Tolerability, Pharmacokinetics, Target Occupancy, and Concentration-QT Analysis of the Novel BTK Inhibitor Evobrutinib in Healthy Volunteers.
    Becker A, Martin EC, Mitchell DY, Grenningloh R, Bender AT, Laurent J, Mackenzie H, Johne A.
    Clin Transl Sci; 2020 Mar 15; 13(2):325-336. PubMed ID: 31654487
    [Abstract] [Full Text] [Related]

  • 11. Zanubrutinib (BGB-3111), a Second-Generation Selective Covalent Inhibitor of Bruton's Tyrosine Kinase and Its Utility in Treating Chronic Lymphocytic Leukemia.
    Rhodes JM, Mato AR.
    Drug Des Devel Ther; 2021 Mar 15; 15():919-926. PubMed ID: 33688166
    [Abstract] [Full Text] [Related]

  • 12. Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors.
    Diao Y, Fang X, Song P, Lai M, Tong L, Hao Y, Dou D, Liu Y, Ding J, Zhao Z, Xie H, Li H.
    Bioorg Med Chem; 2019 Aug 01; 27(15):3390-3395. PubMed ID: 31221612
    [Abstract] [Full Text] [Related]

  • 13. Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
    Caldwell R, Liu-Bujalski L, Qiu H, Mochalkin I, Jones R, Neagu C, Goutopoulos A, Grenningloh R, Johnson T, Sherer B, Gardberg A, Follis AV, Morandi F, Head J.
    Bioorg Med Chem Lett; 2018 Nov 15; 28(21):3419-3424. PubMed ID: 30290988
    [Abstract] [Full Text] [Related]

  • 14. Optimizing Platelet GPVI Inhibition versus Haemostatic Impairment by the Btk Inhibitors Ibrutinib, Acalabrutinib, ONO/GS-4059, BGB-3111 and Evobrutinib.
    Denzinger V, Busygina K, Jamasbi J, Pekrul I, Spannagl M, Weber C, Lorenz R, Siess W.
    Thromb Haemost; 2019 Mar 15; 119(3):397-406. PubMed ID: 30685871
    [Abstract] [Full Text] [Related]

  • 15. Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.
    Kawahata W, Asami T, Kiyoi T, Irie T, Kashimoto S, Furuichi H, Sawa M.
    J Med Chem; 2021 Oct 14; 64(19):14129-14141. PubMed ID: 34529443
    [Abstract] [Full Text] [Related]

  • 16. A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant BtkC481S mutation in B-cell malignancies.
    Gui F, Jiang J, He Z, Li L, Li Y, Deng Z, Lu Y, Wu X, Chen G, Su J, Song S, Zhang YM, Yun CH, Huang X, Weisberg E, Zhang J, Deng X.
    Br J Pharmacol; 2019 Dec 14; 176(23):4491-4509. PubMed ID: 31364164
    [Abstract] [Full Text] [Related]

  • 17. Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
    Qiu H, Ali Z, Bender A, Caldwell R, Chen YY, Fang Z, Gardberg A, Glaser N, Goettsche A, Goutopoulos A, Grenningloh R, Hanschke B, Head J, Johnson T, Jones C, Jones R, Kulkarni S, Maurer C, Morandi F, Neagu C, Poetzsch S, Potnick J, Schmidt R, Roe K, Viacava Follis A, Wing C, Zhu X, Sherer B.
    Bioorg Med Chem; 2021 Jun 15; 40():116163. PubMed ID: 33932711
    [Abstract] [Full Text] [Related]

  • 18. Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
    Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B.
    J Med Chem; 2020 May 28; 63(10):5102-5118. PubMed ID: 32083858
    [Abstract] [Full Text] [Related]

  • 19. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
    Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB.
    J Med Chem; 2018 Mar 22; 61(6):2227-2245. PubMed ID: 29457982
    [Abstract] [Full Text] [Related]

  • 20. Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.
    Teng Y, Lu X, Xiao M, Li Z, Zou Y, Ren S, Cheng Y, Luo G, Xiang H.
    Eur J Med Chem; 2020 Aug 01; 199():112339. PubMed ID: 32402933
    [Abstract] [Full Text] [Related]

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