Novel heterocyclic NF-kB inhibitors
    1.
    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

    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,

    Heterocyclic NF-kB inhibitors
    2.
    发明授权
    Heterocyclic NF-kB inhibitors 失效
    杂环NF-kB抑制剂

    公开(公告)号:US07601745B2

    公开(公告)日:2009-10-13

    申请号:US11375259

    申请日:2006-03-15

    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(O)NR a R b,卤素,烷基, 卤代烷基,芳基,杂芳基,OH,SH,NR4'OR5',NH2,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)paryl, - (CH 2)p NR 17 R 8,-C(O)NR 7 R 8,-N-CR 7 R 8,-NR 7 C(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; R5是卤素,烷基,-C(NR7)NR7R8, - (CH2)paryl, - (CH2)pNR7R8,-C(O)NR7R8,-N-CR7R8,-NR7C(O)R8,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。

    Novel Heterocyclic Nf-Kb Inhibitors
    3.
    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:US20080261971A1

    公开(公告)日:2008-10-23

    申请号:US11575647

    申请日:2005-07-29

    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独立地为烷基,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; R 5独立地为H,COR 6,CO 2,R 6,SOR 6, SO 2 SO 2,SO 3 R 6,烷基,环烷基,烷氧基,-NH

    Heterocyclic NF-κB inhibitors
    5.
    发明授权
    Heterocyclic NF-κB inhibitors 失效
    杂环NF-κB抑制剂

    公开(公告)号:US07812041B2

    公开(公告)日:2010-10-12

    申请号:US11192009

    申请日:2005-07-29

    摘要: 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.

    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。

    Novel compounds as inhibitors of cell proliferation and viral infections
    7.
    发明申请
    Novel compounds as inhibitors of cell proliferation and viral infections 失效
    新型化合物作为细胞增殖和病毒感染的抑制剂

    公开(公告)号:US20050197368A1

    公开(公告)日:2005-09-08

    申请号:US11066265

    申请日:2005-02-28

    IPC分类号: A61K31/422 C07D413/02

    摘要: The present invention relates to novel compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Z is NH, or CH2 if Y is SO2 Y is C═O, C═S, or SO2 if Z is CH2; A is phenyl or indolyl, N-methyl-indolyl R1 is —CN, wherein the bond between CR3 and CR7 is a single or double bond; m is 0 or 1; n is 0 or 1; p is 0 or 1; and to their use as medicaments.

    摘要翻译: 本发明涉及通式(I)的新化合物及其盐和生理功能衍生物,其中如果Y是SO 2 Y,Z是NH或CH 2 如果Z是CH 2,则为CO,CS或SO 2; A是苯基或吲哚基,N-甲基 - 吲哚基R 1是-CN,其中CR 3和CR 7之间的键是单个 或双键; m为0或1; n为0或1; p为0或1; 并用作药物。

    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

    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。

    Compounds as inhibitors of cell proliferation and viral infections
    10.
    发明授权
    Compounds as inhibitors of cell proliferation and viral infections 失效
    化合物作为细胞增殖和病毒感染的抑制剂

    公开(公告)号:US07317030B2

    公开(公告)日:2008-01-08

    申请号:US11066265

    申请日:2005-02-28

    IPC分类号: A61K31/421 C07D263/34

    摘要: The present invention relates to novel compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Z is NH, or CH2 if Y is SO2 Y is C═O, C═S, or SO2 if Z is CH2; A is phenyl or indolyl, N-methyl-indolyl R1 is —CN, wherein the bond between CR3 and CR7 is a single or double bond; m is 0 or 1; n is 0 or 1; p is 0 or 1; and to their use as medicaments.

    摘要翻译: 本发明涉及通式(I)的新化合物及其盐和生理功能衍生物,其中如果Y是SO 2 Y,Z是NH或CH 2 如果Z是CH 2,则为CO,CS或SO 2; A是苯基或吲哚基,N-甲基 - 吲哚基R 1是-CN,其中CR 3和CR 7之间的键是单个 或双键; m为0或1; n为0或1; p为0或1; 并用作药物。