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Prodrugs of multifunctional nitroxide derivatives and their uses
专利权人:
Salzman Group; Ltd
发明人:
SALZMAN, Andrew Lurie,JAGTAP, Prakash,SOUTHAN, Garry John
申请号:
ES14713588
公开号:
ES2663477T3
申请日:
2014.03.05
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of the general formula I: ** (See formula) ** or an enantiomer, diastereomer, racemate or a pharmaceutically acceptable salt thereof, wherein R1 is each independently selected from H, -OH, -COR4, -COOR4 , -OCOOR4, -OCON (R4) 2, -C1-C16 alkylene -CO4, -CN, -NO2, -SH, -SR4, -C1-C16 alkyl, -O-C1-C16 alkyl , -N (R4) 2, -CON (R4) 2, -SO2R4, - SO2NHR4, -S (>; = O) R4, or a nitric oxide donor group of formula -X1-X2-X3, where X1 is absent or selected from -O-, -S- or -NH-; X2 is absent or is (C1-C20) alkylene optionally substituted with one or more -ONO2 groups; and X3 is -NO or -ONO2, with the proviso that at least one R1 group is a nitric oxide donor group; R2 is each independently selected from (C1-C16) alkyl, (C2-C16) alkenyl or (C2-C16) alkynyl; R3 is selected from (C1-C10) alkyl, cycloalkyl (C3-C10), aryl (C6-C14) or 4 to 12 membered heterocyclyl, each of which may be optionally substituted with -OH, -COR5, -COOR5 , -C1-C8 alkylene -COOR5, -CN, -NO2, -C1-C8 alkyl, -O-C1-C8 alkyl, -N (R5) 2, -CON (R5) 2, - SO2R5, -SO2NHR5, or -S (>; = O) R5; R4 is each independently selected from H, (C1-C8) alkyl, (C3-C10) cycloalkyl, (C6-C14) aryl or 4-12 membered heterocyclyl, each of which other than H may be optionally substituted with - OH, -COR5, -COOR5, -OCOOR5, -OCON (R5) 2, -alkylene (C1-C8) -COOR5, -CN, -NO2, -SH, -SR5, -alkyl (C1-C8), - O-(C1-C8) alkyl, -N (R5) 2, -CON (R5) 2, -SO2R5, -SO2NHR5 or -S (>; = O) R5; R5 is each independently selected from H, (C1-C8) alkyl, (C3-C10) cycloalkyl, (C6-C14) aryl or 4-12 membered heterocyclyl; and n is an integer from 1 to 3.Un compuesto de la fórmula general I: **(Ver fórmula)** o un enantiómero, diastereómero, racemato o una sal farmacéuticamente aceptable del mismo, en donde R1 se selecciona cada uno independientemente entre H, -OH, -COR4, -COOR4, -OCOOR4, -OCON(R4)2, -alquileno (C1-C16)-COOR4, -CN, -NO2, -SH, -SR4, -alquilo (C1-C16), -O-alquilo ( C1-C16), -N(R4)2, -CON(R4)2, -SO2R4, - SO2NHR4, -S(>;=O)R4, o un g
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