1335490-33-9Relevant academic research and scientific papers
Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer
Lücking, Ulrich,Scholz, Arne,Lienau, Philip,Siemeister, Gerhard,Kosemund, Dirk,Bohlmann, Rolf,Briem, Hans,Terebesi, Ildiko,Meyer, Kirstin,Prelle, Katja,Denner, Karsten,B?mer, Ulf,Sch?fer, Martina,Eis, Knut,Valencia, Ray,Ince, Stuart,von Nussbaum, Franz,Mumberg, Dominik,Ziegelbauer, Karl,Klebl, Bert,Choidas, Axel,Nussbaumer, Peter,Baumann, Matthias,Schultz-Fademrecht, Carsten,Rühter, Gerd,Eickhoff, Jan,Brands, Michael
, p. 1776 - 1793 (2017/10/23)
Selective inhibition of exclusively transcription-regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY-958, lead optimization efforts strictly focusing on kinase selectivity, physicochemical and DMPK properties finally led to the identification of the orally available clinical candidate atuveciclib (BAY 1143572). Structurally characterized by an unusual benzyl sulfoximine group, BAY 1143572 exhibited the best overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats. BAY 1143572 is the first potent and highly selective PTEFb/CDK9 inhibitor to enter clinical trials for the treatment of cancer.
PHARMACEUTICALLY ACTIVE DISUBSTITUTED TRIAZINE DERIVATIVES
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Page/Page column 56, (2011/10/13)
The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase. formula (I) wherein R1 is formula (II), formula (III) or formula (IV).
