84341-13-9Relevant academic research and scientific papers
BICYCLIC ETHER O-GLYCOPROTEIN-2-ACETAMIDO-2-DEOXY-3-D-GLUCOPYRANOSIDASE INHIBITORS
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Paragraph 00247, (2020/08/22)
Described herein are compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R1, R3, R 4, Y1, Y2, n and p are as defined herein.
Substituted Quinazoline and Pyridopyrimidine Derivatives Useful as Anticancer Agents
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, (2019/08/22)
Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
WNT SIGNALING INHIBITOR
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Paragraph 0227-0228, (2016/07/05)
A Wnt signaling inhibitor which comprises, as an active ingredient, a fused-ring heterocyclic compound represented by the following formula (IA) or a pharmaceutically acceptable salt thereof, and the like are provided: (wherein, n1A represents
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
Bavetsias, Vassilios,Lanigan, Rachel M.,Ruda, Gian Filippo,Atrash, Butrus,McLaughlin, Mark G.,Tumber, Anthony,Mok, N. Yi,Le Bihan, Yann-Va?,Dempster, Sally,Boxall, Katherine J.,Jeganathan, Fiona,Hatch, Stephanie B.,Savitsky, Pavel,Velupillai, Srikannathasan,Krojer, Tobias,England, Katherine S.,Sejberg, Jimmy,Thai, Ching,Donovan, Adam,Pal, Akos,Scozzafava, Giuseppe,Bennett, James M.,Kawamura, Akane,Johansson, Catrine,Szykowska, Aleksandra,Gileadi, Carina,Burgess-Brown, Nicola A.,Von Delft, Frank,Oppermann, Udo,Walters, Zoe,Shipley, Janet,Raynaud, Florence I.,Westaway, Susan M.,Prinjha, Rab K.,Fedorov, Oleg,Burke, Rosemary,Schofield, Christopher J.,Westwood, Isaac M.,Bountra, Chas,Müller, Susanne,Van Montfort, Rob L. M.,Brennan, Paul E.,Blagg, Julian
, p. 1388 - 1409 (2016/03/05)
We report the discovery of N-substituted 4-(pyridin-2-yl)thiazole-2-amine derivatives and their subsequent optimization, guided by structure-based design, to give 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysine demethylase (KDM) inhibitors which bind to Fe(II) in the active site. Substitution from C4 of the pyrazole moiety allows access to the histone peptide substrate binding site; incorporation of a conformationally constrained 4-phenylpiperidine linker gives derivatives such as 54j and 54k which demonstrate equipotent activity versus the KDM4 (JMJD2) and KDM5 (JARID1) subfamily demethylases, selectivity over representative exemplars of the KDM2, KDM3, and KDM6 subfamilies, cellular permeability in the Caco-2 assay, and, for 54k, inhibition of H3K9Me3 and H3K4Me3 demethylation in a cell-based assay.
HISTONE DEMETHYLASE INHIBITORS
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Paragraph 00350, (2014/10/04)
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors
Labadie, Sharada,Barrett, Kathy,Blair, Wade S.,Chang, Christine,Deshmukh, Gauri,Eigenbrot, Charles,Gibbons, Paul,Johnson, Adam,Kenny, Jane R.,Kohli, Pawan Bir,Liimatta, Marya,Lupardus, Patrick J.,Shia, Steven,Steffek, Micah,Ubhayakar, Savita,Abbema, Anne Van,Zak, Mark
, p. 5923 - 5930 (2013/10/22)
A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. Structure-based design strategies were applied to significantly improve enzyme potency and the polarity of the molecule was adjusted to gain cellular activity. The crystal structures of two representative inhibitors bound to Jak1 were obtained to enable SAR exploration.
