N - ((1H-indole-3-yl) -alkyl) -4-benzyl) benzamide and derivatives of N - ((1H-pyrrolo [2,3-b] pyridin-3-yl) -alkyl) -4- benzyl) benzamide as inhibitors of alpha-synuclein aggregation for the treatment of neurodegenerative disorders
GRIFFIOEN, Gerard,VAN DOOREN, Tom,ROJAS DE LA PARRA, Verónica,ALLASIA, Sara,MARCHAND, Arnaud,KILONDA, Amuri,CHALTIN, Patrick
申请号:
ES11805450
公开号:
ES2637288T3
申请日:
2011.12.13
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula (A1) or a stereoisomer, enantiomer or tautomer thereof, ** Formula ** in which - E is independently selected from CR3; and N; - each R1, R3, R4 and R6 is independently selected from hydrogen; halogen; -OH; -OR10; -SH; -SR10; -S (O) R11; -S (O) 2R11; -SO2NR12R13; trifluoromethyl; trifluoromethoxy; nitro; -NHC (O) R10; -NHS (O) 2R10; - NHC (O) NR12R13; -NR10C (O) R10; -NR10S (O) 2R10; -NR10C (O) NR12R13; -NR12R13; -ciano -COOH; -COOR10; - C (O) NR12R13; -C (O) R11; I rent; alkenyl; alkynyl; aryl; heterocycle; arylalkylene; arylalkenylene; arylalkylene; heterocycle-alkylene; heterocycle-alkenylene; and heterocycloalkynylene; * and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkylene, heterocycle-alkylene, heterocyclo-alkenylene or heterocyclo-alkynylene optionally includes one or more heteroatoms in the alkyl (eno) moiety, alkenyl (eno ) or alkynyl (eno), said heteroatoms being selected from the atoms O, S and N; * and in which said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkylene, heterocycle-alkylene, heterocyclo-alkenylene or heterocyclo-alkynylene may be unsubstituted or substituted with one or more Z; * and in which a carbon atom or hetero atom of said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkylene, heterocycle-alkylene, heterocyclo-alkenylene or heterocyclo20 alkynylene may be oxidized to form a C>; = O, C >; = S, N>; = O, N>; = S, S>; = O or S (O) 2; - R2 is selected from hydrogen; I rent; alkenyl; and alkynyl; - R5 is independently selected from halogen; -OH; -OR10; -SH; -SR10; -S (O) R11; -S (O) 2R11; - SO2NR12R13; trifluoromethyl; trifluoromethoxy; nitro; -NHC (O) R10; -NHS (O) 2R10; -NHC (O) NR12R13; -NR10C (O) R10; - NR10S (O) 2R10; -NR10C (O) NR12R13; -NR12R13; -ciano -COOH; -COOR10; -C (O) NR12R13; -C (O) R11; I rent; alkenyl; alkynyl; aryl; heterocycle; arylalkylene; arylalkenylene; arylalkylene; het