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16 条记录 (耗时 0.026 秒)

    Novel heterocyclic NF-kB inhibitors
    5.
    发明申请
    Novel heterocyclic NF-kB inhibitors 失效
    新型杂环NF-kB抑制剂

    公开(公告)号：US20060069102A1

    公开(公告)日：2006-03-30

    申请号：US11192009

    申请日：2005-07-29

    申请人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    发明人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    IPC分类号： A61K31/496 ,  A61K31/4545 ,  C07D417/14

    CPC分类号： C07D401/14 ,  C07D263/48 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

    摘要： The present invention relates to compounds of the general formula (1) 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.

    摘要翻译： 本发明涉及通式（1）的化合物及其盐和生理功能衍生物，

    Novel heterocyclic NF-kB inhibitors
    6.
    发明申请
    Novel heterocyclic NF-kB inhibitors 失效
    新型杂环NF-kB抑制剂

    公开(公告)号：US20060247253A1

    公开(公告)日：2006-11-02

    申请号：US11375259

    申请日：2006-03-15

    申请人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    发明人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    IPC分类号： A61K31/496 ,  A61K31/4545 ,  A61K31/454 ,  C07D417/14 ,  C07D417/04

    CPC分类号： C07D277/56 ,  C07D263/48 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

    摘要： The present invention relates to compounds of the general formula (III) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4′OR5′, NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N═CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hyodroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N═CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.

    摘要翻译： 本发明涉及通式（III）的化合物或其药学上可接受的盐与酸或碱，或其药学上可接受的前药或立体异构体，其中R 3是H，-C（ 卤素，烷基，卤代烷基，芳基，杂芳基，OH，SH，NR 4'或O 5 NH 2，胺，烷基胺，烷氧基，环烷基，杂环烷基，羟基烷基或卤代烷氧基; R 4是H，卤素，烷基，-C（NR 7）NR 7 R 8， - （ CH 2芳基， - （CH 2 CH 2）n NR 7 R 12 8，-C（O）NR 7 R 8，-N-CR 7 R 8 C 0（O）R 8，环烷基，杂环烷基，卤代烷基，羟基烷基，羟基烷基氨基，烷基氨基，杂芳基或芳基; R 5是卤素，烷基，-C（NR 7）NR 7 R 8， - （CH 3） （CH 2）n，NR 2，R 2，R 2，R 3， > 8，-C（O）NR 7 R 8，-N-CR 7 R 8， （O）R 8，环烷基，杂环烷基，卤代烷基，羟基烷基，羟基烷基氨基，烷基氨基，杂芳基或芳基。

    Heterocyclic NF-κB inhibitors
    8.
    发明授权
    Heterocyclic NF-κB inhibitors 失效
    杂环NF-κB抑制剂

    公开(公告)号：US08106048B2

    公开(公告)日：2012-01-31

    申请号：US11575647

    申请日：2005-07-29

    申请人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzík

    发明人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzík

    IPC分类号： A61K31/535 ,  A61K31/53 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/445 ,  A61K31/425 ,  C07D403/10 ,  C07D401/10

    CPC分类号： C07D263/48 ,  C07D277/56 ,  C07D401/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： 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.

    摘要翻译： 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。