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    • 4. 发明授权
    • Heterocyclic NF-κB inhibitors
    • 杂环NF-κB抑制剂
    • US07812041B2
    • 2010-10-12
    • US11192009
    • 2005-07-29
    • Johann LebanHarald SchmittKristina WolfStefano PegoraroAndreas Wuzik
    • Johann LebanHarald SchmittKristina WolfStefano PegoraroAndreas Wuzik
    • A01N43/78A01N43/50A01N43/76A01N43/36A61K31/425A61K31/415A61K31/42C07D277/04C07D277/08C07D263/02C07D413/00C07D233/00C07D233/02C07D207/00C07D295/00
    • C07D401/14C07D263/48C07D413/12C07D417/04C07D417/12C07D417/14C07D487/04C07D495/04
    • The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, or SO2.
    • 本发明涉及通式(I)的化合物及其盐和生理功能衍生物,其中R 1独立地是氢; 烷基,环烷基,羟基烷基,卤代烷基,卤代烷氧基,芳基,取代的芳基,杂芳基,取代的杂芳基,芳基烷基或取代的芳基烷基; R2独立地是-NR3R4,R3独立地是烷基,环烷基,烷氧基,烷基胺,-OH,-SH,烷硫基,羟基烷基,卤代烷基,卤代烷氧基,芳基或杂芳基,R4独立地是烷基,环烷基,烷氧基,烷基胺,烷硫基, 卤代烷基,卤代烷氧基,芳基或杂芳基; R5独立地是H,COR6,CO2R6,SOR6,SO3R6,烷基,环烷基,烷氧基,-NH2,烷基胺,-NR7COR6,卤素,-OH,-SH,烷硫基,羟基烷基,卤代烷基,卤代烷氧基,芳基或杂芳基; R6独立地为H,烷基,环烷基,-NH2,烷基胺,芳基或杂芳基; R 7独立地是H,烷基,环烷基,烷氧基,-OH,-SH,烷硫基,羟基烷基,芳基或杂芳基; p为0或1; q为0或1; X是CO或SO2。
    • 9. 发明授权
    • Heterocyclic NF-κB inhibitors
    • 杂环NF-κB抑制剂
    • US08106048B2
    • 2012-01-31
    • US11575647
    • 2005-07-29
    • Johann LebanHarald SchmittKristina WolfStefano PegoraroAndreas Wuzík
    • Johann LebanHarald SchmittKristina WolfStefano PegoraroAndreas Wuzík
    • A61K31/535A61K31/53A61K31/497A61K31/4965A61K31/445A61K31/425C07D403/10C07D401/10
    • C07D263/48C07D277/56C07D401/14C07D413/06C07D413/12C07D413/14C07D417/04C07D417/06C07D417/12C07D417/14C07D487/04C07D491/04C07D495/04
    • The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, or SO2.
    • 本发明涉及通式(I)的化合物及其盐和生理功能衍生物,其中R 1独立地为氢,烷基,环烷基,羟基烷基,卤代烷基,卤代烷氧基,芳基,取代的芳基,杂芳基,取代的杂芳基, 芳基烷基或取代的芳基烷基; R 2独立地是-NR 3 R 4,(II)或(III)R 3独立地是烷基,环烷基,烷氧基,烷基胺,-OH,-SH,烷硫基,羟基烷基,卤代烷基,卤代烷氧基,芳基或杂芳基,R 4独立地是烷基,环烷基,烷氧基 烷基胺,烷硫基,羟基烷基,卤代烷基,卤代烷氧基,芳基或杂芳基; R5独立地是H,COR6,CO2R6,SOR6,SO2R6,SO3R6,烷基,环烷基,烷氧基,-NH2,烷基胺,-NR7COR6,卤素,-OH,-SH,烷硫基,羟基烷基,卤代烷基,卤代烷氧基,芳基或杂芳基; R6独立地为H,烷基,环烷基,-NH2,烷基胺,芳基或杂芳基; R 7独立地是H,烷基,环烷基,烷氧基,-OH,-SH,烷硫基,羟基烷基,芳基或杂芳基; p为0或1; q为0或1; X是CO或SO2。