LUEOEND, RAINER MARTIN,MACHAUER, RAINER,RUEEGER, HEINRICH,VEENSTRA, SIEM JACOB
申请号:
PE0002562014
公开号:
PE15402014A1
申请日:
2012.08.23
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Relates to compounds of formula (i), wherein: R1 and R2 are independently H or Halogen R3 and R4 are independently H or c1-3 alkyl or taken together are ciclopropilo R3 and R4, R1 and R4 are H and R2 and R3 are taken together - CH2 - or - CH2 R5 is c1-3 alkyl, Halo alkyl or alkoxyl C1 C1 - 3 - 3 - Lquilo c1-3 phenyl or heteroaryl monociclico R6 is a 5 or 6 members comprising 1.23 or 4 heteroatoms selected irrespective of N, o and S, where the phenyl or heteroaryl is optionally substituted.Preferred compounds are: [6 - ((R) - 2 - amino - 4 - methyl - 5.5 - difluoro - 5.6 - dihydro - 4H - [1,3] oxazin - 4 - 5 - fluoro - il) pyridin-2-yl] - amide acid 5 - cyano - 3 - methyl - pyridin - 2 - [6 - (carboxylic acid (R) - 2 - amino - 4 - methyl - 5.5 - difluoro - 5.6 - dihydro - 4H - [1,3] oxazin - 4 - 5 - fluoro - il) pyridin-2-yl] - amide acid 3-amino-5 - (1.1 - Difluoro ethyl) - 2 - pirazin - carboxylic acid among others.It also relates to a Pharmaceutical Composition and a combination. These compounds are useful for the treatment of Alzheimers disease or diabetesSE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE: R1 Y R2 SON INDEPENDIENTEMENTE H O HALOGENO R3 Y R4 SON INDEPENDIENTEMENTE H O ALQUILO C1-3, O R3 Y R4 TOMADOS JUNTOS SON CICLOPROPILO, O R1 Y R4 SON H Y R2 Y R3 TOMADOS JUNTOS SON -CH2-O-CH2 R5 ES ALQUILO C1-3, HALO-ALQUILO C1-3 O ALCOXILO C1-3-ALQUILO C1-3 R6 ES FENILO O UN HETEROARILO MONOCICLICO DE 5 O 6 MIEMBROS QUE COMPRENDE 1,2,3 O 4 HETEROATOMOS SELECCIONADOS INDEPENDIENTEMENTE DE N, O Y S, EN DONDE EL FENILO O HETEROARILO ESTA OPCIONALMENTE SUSTITUIDO. SON COMPUESTOS PREFERIDOS: [6-((R)-2-AMINO-5,5-DIFLUORO-4-METIL-5,6-DIHIDRO-4H-[1,3]OXAZIN-4-IL)-5-FLUORO-PIRIDIN-2-IL]-AMIDA DEL ACIDO 5-CIANO-3-METIL-PIRIDIN-2-CARBOXILICO [6-((R)-2-AMINO-5,5-DIFLUORO-4-METIL-5,6-DIHIDRO-4H-[1,3]OXAZIN-4-IL)-5-FLUORO-PIRIDIN-2-IL]-AMIDA DEL ACIDO 3-AMINO-5-(1,1-DIFLUORO-ETIL)-PIRAZIN-2-CARBOXILICO ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UNA COM