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Multifunctional nitroxide derivatives and uses thereof
专利权人:
Radikal Therapeutics Inc.
发明人:
JAGTAP, Prakash,SALZMAN, Andrew Lurie
申请号:
ES11808945
公开号:
ES2580104T3
申请日:
2011.12.08
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of the general formula I: ** Formula ** wherein Y is N, CH or N (→ O), or an enantiomer, diastereomer, racemate, or a pharmaceutically acceptable salt or solvate thereof, wherein A is a structural unit of the general formula II linked through its terminal -NH group to any carbon atom of the pyridine, phenyl, or pyridine oxide ring: ** Formula ** X is absent or is - (CR2R2) n-; R1 is absent or has 1 to 5 substituents each independently selected from halogen, -CN, -OH, -NO2, - N (R6) 2, -OCF3, -CF3, -OR6, -COR6, -COOR6, -CON ( R6) 2, - OCOOR6, -OCON (R6) 2, -alkyl (C1-C8), -alkylene (C1-C8) - COOR6, -SR6, -SO2R6, - SO2N (R6) 2, or -S (>; = O) R6, wherein said -C1-C8 alkyl and -C1-C8 alkylene -COOR6 can optionally be substituted with -OH, -OR3, -OCF3, -CF3, -COR3, -COOR3, - OCOOR3 . -OCON (R3) 2, -C1-C8 alkylene-COOR3, -CN, -NH2, -NO2, -SH, -SR3, - (C1-C8) alkyl, -O-(C1-C8) alkyl, -N (R3) 2, -CON (R3) 2, -SO2R3, or -S (>; = O) R3, or two adjacent R1 groups and the carbon atoms to which they adhere form a carbocyclic or heterocyclic ring of 5 or 6 members, aryl (C6-C10), or 6 to 10 member heteroaryl; provided that when Y is N (→ O), then the maximum number of groups R1 is 4; R2 each is independently selected from H, halogen, -OCF3, -CF3, -OR7, -COR7, -COOR7, -OCOOR7, - OCON (R7) 2, -alkylene (C1-C8) -COOR7, -CN, - NO2, -SH, -SR7, -C1-C8 alkyl, -N (R7) 2, -CON (R7) 2, -SO2R7, SO2N (R7) 2, or -S (>; = O) R7; or two R2 groups and the carbon atom to which they adhere form a 5- or 6-membered carbocyclic or heterocyclic ring; R3 each is independently selected from (C1-C8) alkyl, (C2-C8) alkenyl, or (C2-C8) alkynyl; R4 is selected from H, -COOR7, -C1-C8 alkylene -COOR7, -CN, -C1-C8 alkyl, or -CON (R7) 2; R5 is selected from H, -OH, -O-(C1-C8) alkyl, -CO-(C1-C8) alkyl, -COO-(C1-C8) alkyl, -CN, or -NH2; R6 each is independently selected from H, (C1-C8) alkyl, (C3-C10) cycloalkyl, 4-12 membered heterocyclyl, (C6-C14) aryl, or (C1-C8) -NH2 alkylene; R7 each is ind
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