PETTERSSON, Martin Youngjin,AM ENDE, Christopher William,JOHNSON, Douglas Scott,KAUFFMAN, Gregory Wayne,STEPAN, Antonia Friederike,VERHOEST, Patrick Robert
申请号:
PE2017001310
公开号:
PE20171318A1
申请日:
2016.01.26
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
It refers to a compound of formula I, where: X is a 5-14 membered heteroaryl containing 1 to 3 heteroatoms; R1 is hydrogen, halogen, among others; R2a and R2b are hydrogen, halogen, cyano, among others; R4a and R4b are hydrogen, halogen, oxo, among others; R5a and R5b are hydrogen, halogen, SF5, among others; R6 and R7 are hydrogen, halogen, among others; R10 is halogen, cyano, among others; R11 is halogen, cyano, among others; y is an integer of 1, 2, 3 or 4. Preferred compounds are: 2 - {[(1aS, 6bR) -4-fluoro-1a-methyl-5- (trifluoromethoxy) -1,1a-dihydro-6bH- cyclopropa [b] [1] benzofuran-6b-yl] methyl} -7- (4-methyl-1H-imidazol-1-yl) -3,4-dihydro-2H-pyrido [1,2-a] pyrazin- 1,6-dione;2 - [(1As, 6br) - 3-fluoro-1a-methyl-5 - (trifluoromethane) - 1, 1a-dihydro-6bh-cyclopapa [b] [1] benzofuran-6b-il] methyl} - 7 - (4-methyl-1h-imidazole-1-il) - 3, 4-dihydro-2h-pyridan [1, 2-A] pyridan-1, 6-dioxin, etc. He also mentioned a pharmaceutical composer These compounds are gamma Secretariat modulators that can be used to treat neurodegenerative and neurological diseases such as Alzheimer's and Down's syndrome.Se refiere a un compuesto de formula I, donde: X es un heteroarilo de 5 a 14 miembros que contiene 1 a 3 heteroatomos; R1 es hidrogeno, halogeno, entre otros; R2a y R2b son hidrogeno, halogeno, ciano, entre otros; R4a y R4b son hidrogeno, halogeno, oxo, entre otros; R5a y R5b son hidrogeno, halogeno, SF5, entre otros; R6 y R7 son hidrogeno, halogeno, entre otros; R10 es halogeno, ciano, entre otros; R11 es halogeno, ciano, entre otros; y es un numero entero de 1, 2, 3 o 4. Son compuestos preferidos: 2-{[(1aS, 6bR)-4-fluoro-1a-metil-5-(trifluorometoxi)-1,1a-dihidro-6bH-ciclopropa[b][1]benzofuran-6b-il]metil}-7-(4-metil-1H-imidazol-1-il)-3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona; 2-{[(1aS, 6bR)-3-fluoro-1a-metil-5-(trifluorometoxi)-1,1a-dihidro-6bH-ciclopropa[b][1]benzofuran-6b-il]metil}-7-(4-metil-1H-imidazol-1-il)-3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona; entre