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Novel substituted bicyclic triazole derivatives as gamma-secretase modulators
专利权人:
JANSSEN PHARMACEUTICALS, INC.;CELLZOME LIMITED
发明人:
DE CLEYN, MICHEL ANNA JOZEF,VAN BRANDT, SVEN FRANCISCUS ANNA,GIJSEN, HENRICUS JACOBUS MARIA,BERTHELOT, DIDIER JEAN-CLAUDE,OEHLRICH, DANIEL
申请号:
ES11700171
公开号:
ES2512840T3
申请日:
2011.01.12
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Compound of formula (I) or a stereoisomeric form thereof, in which: Het1 is a heterocycle, having the formula (a-1), (a-2), (a-3) or (a-4) R3 it is C1-4 alkyl; R4, R5, R6 and R8 are each independently hydrogen or C1-4 alkyl optionally substituted with one or more halo substituents; R7a is hydrogen, halo or C1-4 alkyl; R7b and R7c are each independently hydrogen, halo, cyano, C1-4 alkyloxy, C3-7 cycloalkyl or C1-4 alkyl optionally substituted with one or more halo substituents; Xa is CH or N; Xb is O or S; A1 is CR9 or N; wherein R9 is hydrogen, halo or C1-4 alkyloxy; A2, A3 and A4 are each independently CH or N; provided that at most two of A1, A2, A3 and A4 are N; L1 is O, carbonyl, NR10, NH- (C>; = O) or (C>; = O) -NH; wherein R10 is hydrogen or C1-4 alkyl; R1 and --L2-R2 are taken together to form a bivalent radical --R1-R2-L2-- having the formula (b-1), (b-2), (b-3), (b-4 ), (b-5), (b-6) or (b-7) - (CH2) mnY- (CH2) n-- (b-1); - (CH2) n-Y- (CH2) m-n-- (b-2); --CH>; = CH-CH>; = CH-- (b-3); --CH>; = CH-N>; = CH-- (b-4); --CH>; = N-CH>; = CH-- (b-5); - (CH2) q-r-Y- (CH2) r-1,2-benzenediyl-- (b-6); - (CH2) rY- (CH2) q-r-1,2-benzenediyl-- (b-7); in which (b-1) or (b-2) may contain an unsaturated bond;Compuesto de fórmula (I) o una forma estereoisomérica del mismo, en la que: Het1 es un heterociclo, que tiene la fórmula (a-1), (a-2), (a-3) o (a-4) R3 es alquilo C1-4; R4, R5, R6 y R8 son cada uno independientemente hidrógeno o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes halo; R7a es hidrógeno, halo o alquilo C1-4; R7b y R7c son cada uno independientemente hidrógeno, halo, ciano, alquiloxilo C1-4, cicloalquilo C3-7 o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes halo; Xa es CH o N; Xb es O o S; A1 es CR9 o N; en el que R9 es hidrógeno, halo o alquiloxilo C1-4; A2, A3 y A4 son cada uno independientemente CH o N; siempre que como máximo dos de A1, A2, A3 y A4 sean N; L1 es O, carbonilo, NR10, NH-(C>;=O) o (C>;=O
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