219716-49-1Relevant academic research and scientific papers
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
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INIDBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Paragraph 0125; 0126, (2021/02/05)
Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
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.
Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues
Verma, Yogesh Kumar,Reddy, Bonam Srinivasa,Pawar, Mithun S.,Bhunia, Debabrata,Sampath Kumar, Halmuthur M.
, p. 172 - 176 (2016/03/01)
Replacement of the amide moiety in the structure of α-GalCer with a 1,2,3-triazole linker is known to elicit a response skewed toward Th2 immunity, and glycolipids containing an aromatic ring in the terminus of their acyl or phytosphingosine structural component exhibit an enhanced Th1 immune response. In the current study, synthesis and immunological screening of a focused library of benzyloxyalkyl-substituted 1,2,3-triazolyl α-GalCer analogues are reported. The novel α-GalCer analogues activate invariant natural killer T (iNKT) cells via CD1d mediated presentation, which was confirmed by in vitro tests performed on iNKT hybridomas incubated with CD1d proteins. When tested on isolated murine splenocytes, the T1204B and T1206B compounds stimulated higher levels of both IFN-γ and IL-4 cytokine expression in vitro compared to that of α-GalCer.
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
Initial Scale-Up and Process Improvements for the Preparation of a Lead Antibacterial Macrolone Compound
Stimac, Vlado,Matanovic Skugor, Maja,Palej Jakopovic, Ivana,Vinter, Adrijana,Ilijas, Marina,Alihodzc, Sulejman,Mutak, Stjepan
experimental part, p. 1393 - 1401 (2011/09/20)
Macrolones are a novel class of potent antimicrobial agents that consist of a macrolide scaffold to which a quinolone unit is tethered by various linkers to the 4 -O-position of the cladinose sugar. In this paper is described a modified 13-step route to a
MACROLONE COMPOUNDS
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Page/Page column 74, (2008/06/13)
A compound of formula (I) compositions comprising same, processes for their preparation and use of said compounds, particularly in the treatment of microbial infections.
ESTER LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS
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Page/Page column 74, (2008/06/13)
The present invention relates to 14- or 15-membered macrolides substituted at the 4” position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or top
Phase transfer catalysis method of synthesis of benzyl- and benzhydryloxyalkoxyalkynes
Matijoska,Eicher-Lorka,Rastenyte
, p. 160 - 161 (2007/10/03)
The synthesis of benzyl- and benzhydryloxyalkoxyalkynes and the determination of the influence of phase transfer catalyst, solvent and temperature on this nucleophilic substitution reaction is reported.
