VANHOOF, GRETA CONSTANTIA PETER,GUILLEMONT, JERÔME EMILE GEORGES,ROMBOUTS, FREDERIK JAN RITA,BUIJNSTERS, PETER JACOBUS JOHANNES ANTONIUS,ANDRÉS-GIL, JOSÉ IGNACIO,TRABANCO-SUÁREZ, ANDRÉS AVELINO,DE ANG
申请号：
MX2013015201
公开号：
MX2013015201A
申请日:
2012.06.26
申请国别(地区):
MX
年份:
2014
代理人:
摘要：
The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. 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 PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.La presente invención se refiere a derivados novedosos de 1-aril-4-metil-[1 ,2 ,4]triazolo[4,3-a]quinoxalina como inhibidores de la fosfodiesterasa 2 (PDE2) y en menor medida de la fosfodiesterasa 10 (PDEIO), o como inhibidores de tanto la fosfodiesterasa 2 como la 10 la invención también se refiere a composiciones farmacéuticas que comprenden tales compuestos, a procedimientos para preparar tales compuestos y composiciones, y al uso de tales compuestos y composiciones para la prevención y el tratamiento de trastornos en los que interviene PDE2 o trastornos en los que intervienen tanto PDE2 como PDEIO, tales como trastornos neurológicos y psiquiátricos, y enfermedades metabólicas o endocrinológicas la presente invención también se refiere a compuestos radiomarcados que pueden ser útiles para el registro gráfico de imágenes y la cuantificación de la enzima
