GREEN, LUKE,GUBA, WOLFGANG,JAESCHKE, GEORG,JOLIDON, SYNESE,LINDEMANN, LOTHAR,STADLER, HEINZ,VIEIRA, ERIC
申请号:
PE2012000817
公开号:
PE20121443A1
申请日:
2010.12.14
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
1. Refers to the compound extracted from formula (I), where x is n or CR1, wherein R1 is h, low tar, low oxygen, hydrogen Xi, low hydroxide, etc.; and N or CR2, wherein R2 is h, CN, low tar or isocyclic aryl; Z is ch or N; R4 is a six ring aromatic substitute, which contains up to 2 ml of substitutes, mainly replaced by halogen, low tar, etc. The preferred compounds are: 6-phenyl-pyridine-pyridine [1,5-a], 2-methyl-6-phenyl-pyridine-pyrazol [1,5-a], pyridine; 6 - (2-fluoro-phenyl) - 2-methyl-pyrazol [1,5-a] pyridine; 2-tri-butyl-6 - (3-fluoro-phenyl) - pyrazol [1,5-a] - pyridan;There are others He also mentioned a pharmaceutical composer These compounds are the modulators of mGluR5 and can be used in the treatment of schizophrenia.SE REFIERE A COMPUESTOS DERIVADOS DE ETINILO DE FORMULA (I) DONDE X ES N O CR1, EN DONDE R1 ES H, ALQUILO INFERIOR, ALCOXI INFERIOR, HIDROXI, HIDROXIALQUILO INFERIOR, ENTRE OTROS; Y ES N O CR2, EN DONDE R2 ES H, CN, ALQUILO INFERIOR O HETEROCICLOALQUILO; Z ES CH O N; R4 ES UN SUSTITUYENTE AROMATICO DE 6 ESLABONES QUE CONTIENE HASTA 2 N OPCIONALMENTE SUSTITUIDO CON HALOGENO, ALQUILO INFERIOR, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-FENILETINIL-PIRAZOLO[1,5-a]PIRIMIDINA; 2-METIL-6-FENILETINIL-PIRAZOLO[1,5-a]PIRIMIDINA; 6-(2-FLUOR-FENILETINIL)-2-METIL-PIRAZOLO[1,5-a]PIRIMIDINA; 2-TERT-BUTIL-6-(3-FLUOR-FENILETINIL)-PIRAZOLO[1,5-a]-PIRIMIDINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS DEL RECEPTOR DE GLUTAMATO METABOTROPICO DEL SUBTIPO 5 (mGluR5) SIENDO UTILES EN EL TRATAMIENTO DE ESQUIZOFRENIA