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ENT1 Nucleoside Balancing Conveyor Inhibitors
专利权人:
JANSSEN PHARMACEUTICA; N.V.
发明人:
BOSMANS, Jean-Paul René Marie André,BERTHELOT, Didier Jean-Claude,PIETERS, Serge Maria Aloysius,VERBIST, Bie Maria Pieter,DE CLEYN, Michel Anna Jozef
申请号:
ES08849500
公开号:
ES2569511T3
申请日:
2008.11.13
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compound of formula (1) ** Formula ** including any stereochemically isomeric form thereof, in which -A-B- represents ** Formula ** in which n is an integer 0 or 1; R13 represents hydroxy or halo; R14 represents hydrogen or C1-6 alkyl; in the bivalent radicals (a-4), (a-5) and (a-6), any of the hydrogen atoms in the same or in a different carbon atom may be substituted by halo; R1 and R2 are each independently selected from hydrogen, halo or C1-6 alkyl; R3, R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6 alkyl, polyhalo-C1-6 alkyl, C3-6 cycloalkyl, NO2, Cycle1, Cycle2, or X-R8, in the that X represents O or NR9, in which R9 is hydrogen, C1-6 alkyl or C1-6 alkyl-oxy C1-6 alkyl, and in which R8 is hydrogen, C1-6 alkyl, C2 alkenyl -6, C3-6 cycloalkyl, polyhalo-C1-6 alkyl, C1-6 alkyl oxycarbonyl, C1-6 alkylcarbonyl, polyhalo-C1-6 alkylcarbonyl, Cycle2, - (C>; = O) - (CH2) m-Cycle2, - (C>; = O) - (CH2) m-CH2-OH, - (C>; = O) - (CH2) m-CH2-O-C1-4 alkyl or C1 alkyl -6 substituted with halo, hydroxy, cyano, C3-6 cycloalkyl, C1-6-oxy alkyl, aminocarbonyl, phenyl, Cycle1, or Cycle2, or NR11R12, wherein R11 and R12 are each independently selected from hydrogen, alkyl C1-6, C1-6 alkylcarbonyl, or C1-6 alkyl oxycarbonyl; m is an integer of 0, 1 or 2; Cycle 1 is selected from ** Formula ** in which R 10 is hydrogen, C 1-6 alkyl, C 1-6 alkylcarbonyl, or C 1-6 alkyl oxycarbonyl; and Cycle2 is selected from where R10 is hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkylcarboxylic or C1-6alkyl substituted by halo or hydroxy; or a pharmaceutically acceptable acid addition salt thereof, or a solvate thereof, or an N-oxide form thereof.Compuesto de fórmula (1) **Fórmula** incluyendo cualquier forma estereoquímicamente isomérica del mismo, en el que -A-B- representa **Fórmula** en los que n es un número entero 0 o 1; R13 representa hidroxi o halo; R14 representa hidrógeno o alquilo de C1-6; en los radicales bivalentes (a-4), (a-5) y (a-6), cualquiera de los
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