219716-49-1Relevant articles and documents
Discovery of highly potent, selective, and brain-penetrant aminopyrazole Leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors
Estrada, Anthony A.,Chan, Bryan K.,Baker-Glenn, Charles,Beresford, Alan,Burdick, Daniel J.,Chambers, Mark,Chen, Huifen,Dominguez, Sara L.,Dotson, Jennafer,Drummond, Jason,Flagella, Michael,Fuji, Reina,Gill, Andrew,Halladay, Jason,Harris, Seth F.,Heffron, Timothy P.,Kleinheinz, Tracy,Lee, Donna W.,Pichon, Claire E. Le,Liu, Xingrong,Lyssikatos, Joseph P.,Medhurst, Andrew D.,Moffat, John G.,Nash, Kevin,Scearce-Levie, Kimberly,Sheng, Zejuan,Shore, Daniel G.,Wong, Susan,Zhang, Shuo,Zhang, Xiaolin,Zhu, Haitao,Sweeney, Zachary K.
, p. 921 - 936 (2014)
Leucine-rich repeat kinase 2 (LRRK2) has drawn significant interest in the neuroscience research community because it is one of the most compelling targets for a potential disease-modifying Parkinson's disease therapy. Herein, we disclose structurally div
CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS
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Page/Page column 291, (2018/02/03)
Fused aromatic bicyclic substituted 5-(2-amino-4-pyrimidinyl)- cyanoindoline derivatives (I) useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
Synthesis and biological activity of 4″-O-acyl derivatives of 14- and 15-membered macrolides linked to ω-quinolone-carboxylic unit
Kugor, Maja Matanovi?,Timac, Vlado,Palej, Ivana,Lugari?, Urdjica,Paljetak, Hana Ipi?,Fili?, Darko,Modri?, Marina,Ilovi?, Ivica,Gembarovski, Dubravka,Mutak, Stjepan,Erakovi? Haber, Vesna,Holmes, David J.,Ivezi?-Schoenfeld, Zrinka,Alihodi?, Sulejman
experimental part, p. 6547 - 6558 (2010/10/03)
The synthesis and antimicrobial activity of a new class of macrolide antibiotics which consist of a macrolide scaffold and a quinolone unit covalently connected by an appropriate linker are described. Optimization of several synthetic steps and structural