DE CLEYN, MICHEL ANNA JOZEF,VAN BRANDT, SVEN FRANCISCUS ANNA,GIJSEN, HENRICUS JABOBUS MARIA,BERTHELOT, DIDIER JEAN-CLAUDE,OEHLRICH, DANIEL
申请号：
PE0009912012
公开号：
PE15112012A1
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 each L1 is n or CH, NH, or carbonyl (c = o) among others R1 and R2 - L2 - together form a Bivalent radical Formula - ch = CH - ch = N -, - ch = CH - ch = CH - ch = CH - ch = n Among others, XA is CH or N R3 is c1-4 alkyl R4R5 and R6 are each H or c1-4 alkyl, optionally substituted XB is o or s R9 is H, or C1 - alkoxy Halo 4. Preferred compounds are 5,6,7,8-tetrahydro - N - [4 - (2 - methyl - 4 - piridinil) phenyl] - 2 - [2 - (trifluoromethyl) phenyl] - [1,2,4] triazolo [1,5-a] pyridin - 2 - Amine 8 - (2-chlorophenyl) - 5,6,7,8-tetrahydro - N - [4 - (2 - methyl - 4 - piridinil) phenyl] - [1,2,4] triazolo [1,5-a] pyridin - 2 - Amine among others.It also relates to a Pharmaceutical composition. This Compound is a Modulator of the Enzyme gamma secretase is useful for the treatment of Alzheimers disease, Parkinsons 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 CADA UNO CH O N L1 ES O, CARBONILO, NH-(C=O), ENTRE OTROS R1 Y -L2-R2 JUNTOS FORMAN UN RADICAL BIVALENTE DE FORMULA -CH=CH-N=CH-, -CH=CH-CH=CH-, -CH=N-CH=CH-, ENTRE OTROS Xa ES CH O N R3 ES ALQUILO C1-4 R4, R5 Y R6 SON CADA UNO H O ALQUILO C1-4 OPCIONALMENTE SUSTITUIDO Xb ES O O S R9 ES H, HALO O ALCOXI C1-4. SON COMPUESTOS PREFERIDOS 5,6,7,8-TETRAHIDRO-N-[4-(2-METIL-4-PIRIDINIL)FENIL]-8-[2-(TRIFLUOROMETIL)FENIL]-[1,2,4]TRIAZOLO[1,5-a]PIRIDIN-2-AMINA 8-(2-CLOROFENIL)-5,6,7,8-TETRAHIDRO-N-[4-(2-METIL-4-PIRIDINIL)FENIL]-[1,2,4]TRIAZOLO[1,5-a]PIRIDIN-2-AMINA ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES MODULADOR DE LA ENZIMA GAMMA SECRETASA SIENDO UTIL PARA EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, PARKINSON, LESION CEREBRAL TRAUMATICA
