87253-79-0Relevant academic research and scientific papers
SUBSTITUTED 5-METHYL-[1, 2, 4] TRIAZOLO [1,5-A) PYRIMIDIN-2-AMINE COMPOUNDS AS PDE2 INHIBITORS
-
Page/Page column 50; 55, (2016/06/01)
The invention provides a chemical entity of Formula (I): (I), wherein R1, R2, R3, and R4, have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma- dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.
Dialkyl bicyclic heterocycles with a bridgehead nitrogen as purine analogs possessing significant cardiac inotropic activity
Okabe,Bhooshan,Novinson,et al.
, p. 735 - 751 (2007/10/02)
A number of 5,7-dialkyl-s-triazolo[1,5-a]pyrimidines and 5,7-dialkylpyrazolo[1,5-a]pyrimidines and related heterocycles containing a bridgehead nitrogen have been prepared and studied as cardiovascular agents in the anesthetized dog. A number of these compounds have exhibited significant inotropic activity with little effct on heart rate. Especially active were 5,7-dialkyl-2-amino or 2-alkylthio-2-triazolo[1,5-a]pyrimidines. In contrast, highly polar purine analogs in these ring systems compounds such as 5,7-di-n-propyl-2-benzylthio-1,3,4-thiadiazolo[3,2-a]pyrimidine bromide 45 containing a charge on the bridgehead nitrogen, were inactive. The detailed structure activity relationship of the dialkyl derivatives of related ring systems are discussed. The presence of certain ring nitrogen atoms are vital to potent in vivo activity, presumably due to specific enzyme binding at these sites. Several of the compounds studied, showed oral activity and are excellent candidates for further evaluation in man.
