22934-24-3Relevant articles and documents
Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz, Richard A.,Ahuja, Vijay T.,Schmitz, William D.,Molski, Thaddeus F.,Mattson, Gail K.,Lodge, Nicholas J.,Bronson, Joanne J.,Macor, John E.
, p. 1890 - 1894 (2010)
A series of N3-pyridylpyrazinones was investigated as corticotropin-releasing factor-1 receptor antagonists. It was observed that the binding affinity of analogues containing a pyridyl group was influenced not only by the substitution pattern on the pyridyl group, but also by the pKa of the pyridyl nitrogen. Analogues containing a novel 6-(difluoromethoxy)-2,5-dimethylpyridin-3-amine group were among the most potent N3-pyridylpyrazinones synthesized. The synthesis and SAR of N3-pyridylpyrazinones is described herein.
OGA INHIBITOR COMPOUNDS
-
Page/Page column 65, (2020/01/11)
The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.