27063-92-9Relevant academic research and scientific papers
FACTOR XI ACTIVATION INHIBITORS
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Page/Page column 26, (2021/10/11)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.
TRIAZOLOPYRIDINE COMPOUNDS AND USES THEREOF
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Paragraph 00190, (2018/04/11)
A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R6, R7 and R8 are as defined herein.
Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates
Thalhammer, Armin,Mecinovic, Jasmin,Loenarz, Christoph,Tumber, Anthony,Rose, Nathan R.,Heightman, Tom D.,Schofield, Christopher J.
scheme or table, p. 127 - 135 (2011/02/24)
Based on structural analysis of the human 2-oxoglutarate (2OG) dependent JMJD2 histone Nε-methyl lysyl demethylase family, 3-substituted pyridine 2,4-dicarboxylic acids were identified as potential inhibitors with possible selectivity over other human 2OG oxygenases. Microwave-assisted palladium-catalysed cross coupling methodology was developed to install a diverse set of substituents on the sterically demanding C-3 position of a pyridine 2,4-dicarboxylate scaffold. The subsequently prepared di-acids were tested for in vitro inhibition of the histone demethylase JMJD2E and another human 2OG oxygenase, prolyl-hydroxylase domain isoform 2 (PHD2, EGLN1). A subset of substitution patterns yielded inhibitors with selectivity for JMJD2E over PHD2, demonstrating that structure-based inhibitor design can enable selective inhibition of histone demethylases over related human 2OG oxygenases.
HISTONE LYSINE DEMETHYLASE INHIBITORS
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Page/Page column 48; 87-88, (2010/04/30)
The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z1; Z2; Y1; Y2; A; p; X1; X2; m; R4; B; R5; R6; R7; R8; R9; X3; R10; R11 and R12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression.
Substituted pyridine-2,4-dicarboxylic acid derivatives and medicaments based on these compounds
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, (2008/06/13)
The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I STR1 in which R1 and R2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compo
Condensed Heteroaromatic Ring Systems. III. Synthesis of Naphthyridine Derivatives by Cyclization of Ethynylpyridinecarboxamides
Sakamoto, Takao,Kondo, Yoshinori,Yamanaka, Hiroshi
, p. 626 - 633 (2007/10/02)
Four kinds of naphthyridinones, i.e. 1,6-naphthyridin-5-one, 1,7-naphthyridin-8-one, 2,6-naphthyridin-2-one, and 2,7-naphthyridin-1-one derivatives, were commonly synthesized by the intramolecular cyclization of pyridinecarboxamides having an ethynyl group or β,β-dimethoxyethyl group adjacent to the carbamoyl group.The syntheses of the starting pyridine derivatives were easily accomplished by cross-coupling of the corresponding halopyridines with acetylenes.Keywords-intramolecular cyclization; palladium catalyst; trimethylsilylacetylene; naphthyridinone; pyridineacetaldehyde; 1(2H)-isoquinolone
SUBSTITUTED ISOCYTOSINES HAVING HISTAMINE H2-ANTAGONIST ACTIVITY
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, (2008/06/13)
The compounds are substituted isocytosines which are histamine H 2-antagonists. Two specific compounds of the present inventon are 2-2-(5-methyl-4-imidazolylmethylthio)ethylamino!-5-(3-pyridylmethyl)-4-pyrimi done and 2-2-(3-bromo-2-pyridylmethylthio)ethylamino!-5-(4-pyridylmethyl)-4-pyrimidone .
