HILPERT, HANS,NARQUIZIAN, ROBERT,PINARD, EMMANUEL,POLARA, ALESSANDRA,ROGERS-EVANS, MARK,WOLTERING, THOMAS,WOSTL, WOLFGANG
申请号：
PE0024972013
公开号：
PE10052014A1
申请日:
2012.05.11
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Refers to - 1.3 oxazine derivative compounds of formula (i) where X is aryl, heteroaryl or cycloalkyl (C3 and C6) is optionally substituted c = or - NH -, - CH2 -, - NH -, among others Z is aryl, heteroaryl, cycloalkyl (C3, C6) among others, R2 is h, alkyl or Halogen (C1 - C6) alkyl (C1 - C3, R3) and R4 are each h, halogen or alkyl (C1 - C6) R5 and R6 are each H or alkyl (C1 - C6).Preferred compounds are: (S) - 4 - (5 - [(1 - 4 - chlorine - difluormetil - 1H pyrazole - 3 - methyl) amino] - 2 - phenyl Fluorine} - 4 - methyl - 5.6 - dihydro - oxazin 4H - [1,3] - 2 - (4R, ilamina 5R) - 5 - fluoro - 4 - [2 - (2 - 5 - fluoro methoxy phenylamino) - phenyl] - 4 - methyl - 5.6 - dihydro - 4H - [1,3] - 2 - ilamina oxazin among others. It also refers to a process of obtaining and to a Pharmaceutical composition.These compounds are inhibitors of BACE1 and BACE2 being useful in the treatment of Alzheimers disease, Type 2 diabetesSE REFIERE A COMPUESTOS DERIVADOS DE 1,3-OXAZINA DE FORMULA (I) DONDE X ES ARILO, HETEROARILO O CICLOALQUILO(C3-C6) OPCIONALMENTE SUSTITUIDOS Y ES -C=O-NH-, -CH2-, -NH-, ENTRE OTROS Z ES ARILO, HETEROARILO, CICLOALQUILO(C3-C6), ENTRE OTROS R2 ES H, ALQUILO(C1-C6) O HALOGENO-ALQUILO(C1-C3) R3 Y R4 SON CADA UNO H, HALOGENO O ALQUILO(C1-C6) R5 Y R6 SON CADA UNO H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: (S)-4-{5-[(4-CLORO-1-DIFLUORMETIL-1H-PIRAZOL-3-ILMETIL)-AMINO]-2-FLUOR-FENIL}-4-METIL-5,6-DIHIDRO-4H-[1,3]OXAZIN-2-ILAMINA (4R,5R)-5-FLUOR-4-[2-FLUOR-5-(2-METOXI-FENILAMINO)-FENIL]-4-METIL-5,6-DIHIDRO-4H-[1,3]OXAZIN-2-ILAMINA ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE OBTENCION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE BACE1 Y BACE2 SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, DIABETES TIPO 2
