HEMBRE, Erik James,LOPEZ, Jose Eduardo,MCMAHON, Jennifer Anne,RICHARDS, Simon James,WINNEROSKI, JR., Leonard Larry,WOODS, Timothy Andrew
申请号：
PE0012562017
公开号：
PE13372017A1
申请日:
2016.02.17
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to a compound of formula II or its pharmaceutically acceptable Salt, where r is Methyl or Ethyl ciclopropilo.Preferred compounds are: N - [3 - [(4aS, 5S, 7aS) - 2 - amino - 5 - (1.1 - difluoroetil) - 4,4a 5.7 - tetrahidrofuro [3,4-d] [1,3] tiazin - 7a - yl] - 4 - fluoro phenyl] - 5 - (1,2,4 - triazole - 1 - il) pyrazine-2-carboxamide malonate n - [3 - [(4aS, 5S, 7aS) - 2 - amino - 5 - (1.1 - difluoroetil) - 4,4a 5.7 - tetrahidrofuro [3,4-d] [1,3] tiazin - 7a - yl] - 4 - fluoro phenyl] - 5 - (1,2,4 - triazole - 1 - il) pyrazine-2-carboxamide, among others.It also relates to a Pharmaceutical Composition and a method for obtaining. These compounds are Selective inhibitors of the Enzyme cleavage of the beta site amyloid precursor protein - 1 (BACE1), being useful in the treatment of Alzheimers diseaseSe refiere a un compuesto de formula II o a su sal farmaceuticamente aceptable, donde R es metilo, etilo o ciclopropilo. Son compuestos preferidos: N-[3-[(4aS, 5S, 7aS)-2-amino-5-(1,1-difluoroetil)-4,4a,5,7-tetrahidrofuro[3,4-d][1,3]tiazin-7a-il]-4-fluoro-fenil]-5-(1,2,4-triazol-1-il)pirazina-2-carboxamida malonato de N-[3-[(4aS, 5S, 7aS)-2-amino-5-(1,1-difluoroetil)-4,4a,5,7-tetrahidrofuro[3,4-d][1,3]tiazin-7a-il]-4-fluoro-fenil]-5-(1,2,4-triazol-1-il)pirazina-2-carboxamida, entre otros. Tambien se refiere a una composicion farmaceutica y a un procedimiento de obtencion. Dichos compuestos son inhibidores selectivos de la enzima de escision de la proteina precursora amiloide de beta-sitio-1 (BACE1), siendo utiles en el tratamiento de la enfermedad de Alzheimer
