1613413-65-2Relevant articles and documents
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase
Angst, Daniela,Gessier, Fran?ois,Janser, Philipp,Vulpetti, Anna,W?lchli, Rudolf,Beerli, Christian,Littlewood-Evans, Amanda,Dawson, Janet,Nuesslein-Hildesheim, Barbara,Wieczorek, Grazyna,Gutmann, Sascha,Scheufler, Clemens,Hinniger, Alexandra,Zimmerlin, Alfred,Funhoff, Enrico G.,Pulz, Robert,Cenni, Bruno
, p. 5102 - 5118 (2020/06/10)
Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in immunity and is considered an attractive target for treating autoimmune diseases. The use of currently marketed covalent BTK inhibitors is limited to oncology indications based on their suboptimal kinase selectivity. We describe the discovery and preclinical profile of LOU064 (remibrutinib, 25), a potent, highly selective covalent BTK inhibitor. LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases. It demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis. LOU064 is currently being tested in phase 2 clinical studies for chronic spontaneous urticaria and Sjoegren's syndrome.
BTK INHIBITOR
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, (2017/11/16)
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
LABELED AMINO PYRIMIDINE DERIVATIVES
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Page/Page column 35, (2016/06/15)
The present invention describes novel radioactive amino pyrimidine derivatives, their preparation and their use as radiotracers / radiomarkers for imaging techniques and as diagnostic tools in the field of BTK receptor susceptible diseases and/or disorder
