PETTERSSON, Martin Youngjin,AM ENDE, Christopher William,JOHNSON, Douglas Scott,KAUFFMAN, Gregory Wayne,STEPAN, Antonia Friederike,VERHOEST, Patrick Robert
申请号:
PE0013102017
公开号:
PE13182017A1
申请日:
2016.01.26
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
Refers to a compound of formula I, where X is a heteroaryl 5 to 14 members that contains 1 to 3 heteroatoms r1 is Hydrogen, halogen, among others 2a and R2B is Hydrogen, halogeno, cyano, among others and R4A r4b are Hydrogen, halogen, Oxo, among others and r5a r5b are Hydrogen, halogen Or, sedan, among others R6 and R7 are Hydrogen, halogen, among others, R10 is halogeno, cyano,Among others, R11 is halogeno, cyano, among others and it is an integer of 1, 2, 3 or 4.Preferred compounds are: {[2 - (1ST, 6BR) - 4 - methyl - 5 - fluoro - 1a - (trifluoromethoxy) - dihydro - - 1,1a 6Bh cyclopropa [b] [1] benzofuran - 6B - il] methyl} - 7 - (4 - methyl - 1 - il - 1H imidazole) - 3,4-dihydro - 2H - pirido [1,2-a] 1.6 - dione 2 - {[(1ST, 6BR) - 3 - methyl - 5 - fluoro - 1a - (trifluoromethoxy) - dihydro - - 1,1a 6Bh cyclopropa [b] [1] Benzofuran - 6B - il] methyl} - 7 - (4 - methyl - 1H imidazol-1-yl) - 3,4-dihydro - 2H - pirido [1,2-a] 16 - dione among others. It also relates to a Pharmaceutical composition. These compounds are gamma secretase modulators, being useful in the treatment of Neurological and neurodegenerative Disorders such as Alzheimers disease and Down 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