52311-36-1Relevant academic research and scientific papers
GSK-3 INHIBITORS
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Page/Page column 103, (2015/05/26)
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.
High colour rendering index and colour stable hybrid white efficient OLEDs with a double emitting layer structure using a single phosphorescence dopant of heteroleptic platinum complexes
Poloek, Anurachw,Lin, Chiao-Wen,Chen, Chin-Ti,Chen, Chao-Tsen
, p. 10343 - 10356 (2015/02/19)
Four heteroleptic platinum complexes (FPtXND) bearing 4-hydroxy-1,5-naphthyridine derivatives functionalized with dimethyl (X = mm), phenoxy (X = OPh), piperidine (X = pp), or carbazole (X = Cz) units as one ligand (XND) and 2-(2,4-difluorophenyl)pyridine as the other common ligand (F) were newly synthesized and characterized. The crystal structures of FPtOPhND and FPtCzND were determined by single-crystal X-ray diffraction crystallography. Although they have a short plane-to-plane packing distance of 3.62 and 3.39 A, respectively, both platinum complexes have different molecular packing patterns, which affect their photoluminescence (PL) in solution and electroluminescence (EL) in the solid state. Due to the contribution from both monomers and excimers/aggregates, all of the platinum complexes exhibited broad and red-shifted PL in concentrated solutions as well as in doped thin films. In the monochromatic organic lighting diode (OLED) testing, FPtXND doped in 4,4′-di(9H-carbazol-9-yl)-1,1′-biphenyl (CBP) exhibited greenish yellow or orange yellow EL, of which FPtOPhND has the highest EL efficiency mainly due to its high solution PL quantum yield of 21%. Hybrid white OLEDs were first achieved with a single emitting layer configuration, of which highly fluorescent blue N,N′-di-1-naphthalenyl-N,N′-diphenyl-[1,1′:4′,1″:4″,1-quaterphenyl]-4,4-diamine (4P-NPD) was used as the host material for all four platinum complexes. To improve the performance of the FPtOPhND-based hybrid white OLEDs, double emitting layer configurations were adopted with CBP and 4P-NPD as the host material. Virtually voltage independent, a white EL having CIEx,y (0.33, 0.31) and a CRI as high as 91 was obtained. The maximum EL efficiency of 11.8%, 25.9 cd A-1, or 11.6 lm W-1 was acquired with FPtOPhND doped in the double emitting layer configuration of an OLED.
Structure guided optimization, in vitro activity, and in vivo activity of pan-PIM kinase inhibitors
Burger, Matthew T.,Han, Wooseok,Lan, Jiong,Nishiguchi, Gisele,Bellamacina, Cornelia,Lindval, Mika,Atallah, Gordana,Ding, Yu,Mathur, Michelle,Mcbride, Chris,Beans, Elizabeth L.,Muller, Kristine,Tamez, Victoriano,Zhang, Yanchen,Huh, Kay,Feucht, Paul,Zavorotinskaya, Tatiana,Dai, Yumin,Holash, Jocelyn,Castillo, Joseph,Langowski, John,Wang, Yingyun,Chen, Min Y.,Garcia, Pablo D.
supporting information, p. 1193 - 1197 (2014/01/06)
Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM Kis 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described.
Heterocyclic Kinase Inhibitors
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Page/Page column 11, (2011/08/22)
New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
Pim kinase inhibitors and methods of their use
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Page/Page column 12-13, (2010/09/05)
The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.
PIM KINASE INHIBITORS AND METHODS OF THEIR USE
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Page/Page column 29, (2009/10/22)
The present invention relates to new compounds of Formulas (I) and (II), their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmac
PIM KINASE INHIBITORS AND METHODS OF THEIR USE
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Page/Page column 62, (2008/12/07)
New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase- mediated disorder, such as cancer.
