468075-00-5Relevant articles and documents
GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 00582; 00583; 001902; 001903, (2021/01/22)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
Pyrido[4,3- e ][1,2,4]triazolo[4,3- a ]pyrazines as selective, brain penetrant phosphodiesterase 2 (PDE2) inhibitors
Rombouts, Frederik J. R.,Tresadern, Gary,Buijnsters, Peter,Langlois, Xavier,Tovar, Fulgencio,Steinbrecher, Thomas B.,Vanhoof, Greet,Somers, Marijke,Andrés, José-Ignacio,Trabanco, Andrés A.
supporting information, p. 282 - 286 (2015/03/30)
A novel series of pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines is reported as potent PDE2/PDE10 inhibitors with drug-like properties. Selectivity for PDE2 was obtained by introducing a linear, lipophilic moiety on the meta-position of the phenyl ring pending from the triazole. The SAR and protein flexibility were explored with free energy perturbation calculations. Rat pharmacokinetic data and in vivo receptor occupancy data are given for two representative compounds 6 and 12.