27063-92-9Relevant articles and documents
FACTOR XI ACTIVATION INHIBITORS
-
, (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.
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.
experimental part, 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.
Substituted pyridine-2,4-dicarboxylic acid derivatives and medicaments based on these compounds
-
, (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