BANNER, DAVID,GUBA, WOLFGANG,HILPERT, HANS,MAUSER, HARALD,MAYWEG, ALEXANDER V.,NARQUIZIAN, ROBERT,PINARD, EMMANUEL,POWER, EOIN,ROGERS-EVANS, MARK,WOLTERING, THOMAS,WOSTL, WOLFGANG
申请号：
PE0008032012
公开号：
PE15002012A1
申请日:
2010.12.06
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to a compound of formula (i) wherein: R1 is aryl, heteroaryl, Lower alkyl, cycloalkyl, among others R2 is H, alkyl and Halogen less R3 is lower alkyl R4 and R5 are independently H and Lower alkyl n is 0, 1, or 2.Preferred compounds are: [3 - ((R) - 2 - amino - 4 - methyl - 5.5 - difluor 5,6 dihydro - 4H - [1,3] - oxazin - 4-yl) - 4 - Fluorine phenyl amide acid] - 5 - Chloro - pyridine - 2 - [3 - carboxylic acid ((R) - 2 - amino - 4 - methyl - 5.5 - difluor 5,6 dihydro - 4H - [1,3] - oxazin - 4-yl) - 4 - Fluorine phenyl amide acid] - 5 - fluoro pyridine carboxylic acid - 2 - [3 - ((R 5.5) - 2 - amino - 4 - methyl - - difluor 5,6 dihydro - 4H - [1,Oxazin] - 3 - 4 - 4 - fluoro - il) - phenyl] - 3 - Chloro - amide acid - 2 - pyridine carboxylic acid among others. It also relates to a Pharmaceutical Composition and a process for obtaining. This Compound is an inhibitor of BACE1 and BACE2, being useful in the treatment of Alzheimers disease and Metabolic DisordersSE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: R1 ES ARILO, HETEROARILO, ALQUILO INFERIOR, CICLOALQUILO, ENTRE OTROS R2 ES H, HALOGENO Y ALQUILO INFERIOR R3 ES ALQUILO INFERIOR R4 Y R5 SON INDEPENDIENTEMENTE H Y ALQUILO INFERIOR n ES 0, 1, O 2. SON COMPUESTOS PREFERIDOS: [3-((R)-2-AMINO-5,5-DIFLUOR-4-METIL-5,6-DIHIDRO-4H-[1,3]-OXAZIN-4-IL)-4-FLUOR-FENIL]-AMIDA DEL ACIDO 5-CLORO-PIRIDINA-2-CARBOXILICO [3-((R)-2-AMINO-5,5-DIFLUOR-4-METIL-5,6-DIHIDRO-4H-[1,3]-OXAZIN-4-IL)-4-FLUOR-FENIL]-AMIDA DEL ACIDO 5-FLUOR-PIRIDINA-2-CARBOXILICO [3-((R)-2-AMINO-5,5-DIFLUOR-4-METIL-5,6-DIHIDRO-4H-[1,3]-OXAZIN-4-IL)-4-FLUOR-FENIL]-AMIDA DEL ACIDO 3-CLORO-PIRIDINA-2-CARBOXILICO ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y UN PROCESO DE OBTENCION. DICHO COMPUESTO ES INHIBIDOR DE LA BACE1 Y BACE2, SIENDO UTIL EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER Y TRANSTORNOS METABOLICOS
