10259-14-0Relevant academic research and scientific papers
ANTAGONIST COMPOUNDS
-
Paragraph 00391, (2022/02/09)
The present invention relates to compounds of formula (I) shown below: wherein R1, R2, R3, R4, R5 and R6 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a and/or A2b receptor activity is implicated, such as, for example, cancer.
1,2,4-TRIAZINE-4-AMINE DERIVATIVES
-
Page/Page column 109, (2011/09/14)
According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1- A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.
Position-specific secondary deuterium isotope effects on basicity of pyridine
Perrin, Charles L.,Karri, Phaneendrasai
experimental part, p. 12145 - 12149 (2010/10/04)
Secondary isotope effects (IEs) on basicities of various deuterated pyridine isotopologues and of 2,6-lutidine-2,6-(CD3)2 have been accurately measured in aqueous solution by an NMR titration method applicable to a mixture. Deuteration at any position of pyridine increases the basicity, but the IE per deuterium is largest for substitution at the 3-position and smallest for the 2-position, which is closest to the site of N-protonation, smaller even than that for 2-CD3 substitution. Computations at the B3LYP/cc-pVTZ level overestimate the magnitude of the measured IEs but largely reproduce the variability with isotopic position. Because the calculated IEs are based on changes in vibrational frequencies on N-protonation, the correspondence between calculated and experimental IEs implies that they arise from zero-point energies, rather than from inductive effects.
Hydrogen-Deuterium Exchange in Dimethylpyridines
Kebede, Naod,Pavlik, James W.
, p. 685 - 686 (2007/10/03)
Dimethylpyridines undergo deuterium-hydrogen exchange when heated in deuterium oxide containing potassium carbonate at ring positions 2 and 6 when these positions are unsubstituted and at methyl groups located at ring positions 2,4, and 6 exclusively.
