VAN BRANDT, SVEN FRANCISCUS ANNA,DE CLEYN, MICHEL ANNA JOZEF,GIJSEN, HENRICUS JABOBUS MARIA,BERTHELOT, DIDIER JEAN-CLAUDE,SURKYN, MICHEL
申请号：
PE0009922012
公开号：
PE15122012A1
申请日:
2011.01.12
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to a compound of formula (i) wherein: het1 is a heterocycle of formula (1), (2), among others, is to extend or A1, A2, A3 and A4 are independently CH o n maximum whenever two of them are n L1 is, or carbonyl NH (c = o), among others r1 is cycloalkyl alquenilo C2 - C3 - 7, 6 or alkyl C 1 - 6 optionally replaced, among others L2 is a direct link, carbonyl, o, S,Among others R2 is morfolinilo, piperidinilo, piperazinilo, among others R9 is H, or C1 - alquiloxi Halo 4 R3 is c1-4 alkyl R4, R5 and R6 are independently H or c1-4 alkyl n is CH or Xa, XB is o or S.Preferred compounds are: 5 - (2-chlorophenoxy) - N - [3 - (4 - (4 - methoxy Methyl 1h imidazol-1-yl) phenyl] - 1 - (1-methylethyl) - 1h-1,2,4-triazole - 3 - Amine n - [3 - (4 - methoxy (2 - methyl - 4 - piridinil) phenyl] - 1 - (1-methylethyl) - 5 - [3 - (trifluoromethyl) - piperidinyl] - 1H - 1,2, 4-triazol-3-amina.2.2hcl.2.7h2o among others. In addition to such a Pharmaceutical Composition and a preparation method.The Compound of the Enzyme gamma secretase Modulator is useful for the treatment of Alzheimers disease, traumatic brain injurySE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: HET1 ES UN HETEROCICLO DE FORMULA (a-1), (a-2), ENTRE OTROS A1 ES CR9 O N A2, A3 Y A4 SON INDEPENDIENTEMENTE CH O N SIEMPRE QUE MAXIMO DOS DE ELLOS SEAN N L1 ES O, CARBONILO, NH(C=O), ENTRE OTROS R1 ES CICLOALQUILO C3-7, ALQUENILO C2-6 O ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO, ENTRE OTROS L2 ES UN ENLACE DIRECTO, CARBONILO, O, S, ENTRE OTROS R2 ES MORFOLINILO, PIPERIDINILO, PIPERAZINILO, ENTRE OTROS R9 ES H, HALO O ALQUILOXI C1-4 R3 ES ALQUILO C1-4 R4, R5, Y R6 SON INDEPENDIENTEMENTE H, O ALQUILO C1-4 Xa ES CH O N Xb ES O O S. SON COMPUESTOS PREFERIDOS: 5-(2-CLOROFENOXI)-N-[3-METOXI-4-(4-METIL-1H-IMIDAZOL-1-IL)FENIL]-1-(1-METILETIL)-1H-1,2,4-TRIAZOL-3-AMINA N-[3-METOXI-4-(2-METIL-4-PIRIDINIL)FENIL]-1-(1-METILETIL)-5-[3-(TRIFLUORMETIL)-1-PIPERIDINIL]-1H-1,2,4-TRIAZOL-3-AMINA.2.2HCL.2.7H2O ENTRE OTROS. REFERIDA ADEMAS A UNA COMP
