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1. 发明申请

US20060069102A1 Novel heterocyclic NF-kB inhibitors 失效
标题翻译：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，

2. 发明申请

US20060247253A1 Novel heterocyclic NF-kB inhibitors 失效
标题翻译：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。

3. 发明申请

US20100267717A1 Novel Heterocyclic NF-kB Inhibitors 审中-公开
标题翻译：新型杂环NF-kB抑制剂
公开(公告)号：US20100267717A1
公开(公告)日：2010-10-21
申请号：US11686301
申请日：2007-03-14
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： A61K31/5377 , C07D401/14 , A61K31/497 , A61K31/496 , C07D487/04 , A61K31/53 , C07D417/14 , A61P9/10 , A61P25/16 , A61P25/28 , A61P25/08 , A61P17/06 , A61P17/00 , A61P17/02 , A61P31/14 , A61P31/18 , A61P31/16 , A61P19/10
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 in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2′, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7′R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N═CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4′OR5′, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2′, O, or S; Z is N or CR2′.
摘要翻译：本发明在一个实施方案中涉及式（Ih）化合物和/或其药学上可接受的盐与酸或碱，和/或其药学上可接受的前药和/或立体异构体，其中A是NR 2'，S 或O; R3a是H，OH，SH，NH2，-C（NR7）NR7'R8， - （CH2）paryl， - （CH2）pNR7R8，-C（O）NR7R8，-N = CR7R8，-NR7C（O）烷基，环烷基，羟基烷基，卤代烷基，卤代烷氧基，烷氧基，烷基氨基，羟基烷基氨基，卤素，芳基或杂芳基; R3是H，-C（O）NRaRb，卤素，烷基，卤代烷基，芳基，杂芳基，OH，SH，NR4'OR5'，NH2，羟烷基氨基，烷基氨基，烷氧基，环烷基，杂环烷基，羟基烷基或卤代烷氧基。 X是NR2'，O或S; Z是N或CR2'。

4. 发明申请

US20120022068A1 NOVEL HETEROCYCLIC NF-kB INHIBITORS 审中-公开
标题翻译：新型杂环NF-kB抑制剂
公开(公告)号：US20120022068A1
公开(公告)日：2012-01-26
申请号：US13225144
申请日：2011-09-02
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： A61K31/5377 , C07D417/14 , C07D403/02 , A61K31/454 , A61K31/53 , A61P19/10 , A61P37/00 , A61P31/12 , A61P9/10 , A61P35/00 , A61P25/28 , A61P1/00 , C07D401/04 , A61K31/506
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 in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2′, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7′R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N═CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4′OR5′, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2′, O, or S; Z is N or CR2′.
摘要翻译：本发明在一个实施方案中涉及式（Ih）化合物和/或其药学上可接受的盐与酸或碱，和/或其药学上可接受的前药和/或立体异构体，其中A是NR 2'，S 或O; R3a是H，OH，SH，NH2，-C（NR7）NR7'R8， - （CH2）paryl， - （CH2）pNR7R8，-C（O）NR7R8，-N = CR7R8，-NR7C（O）烷基，环烷基，羟基烷基，卤代烷基，卤代烷氧基，烷氧基，烷基氨基，羟基烷基氨基，卤素，芳基或杂芳基; R3是H，-C（O）NRaRb，卤素，烷基，卤代烷基，芳基，杂芳基，OH，SH，NR4'OR5'，NH2，羟烷基氨基，烷基氨基，烷氧基，环烷基，杂环烷基，羟烷基或卤代烷氧基。 X是NR2'，O或S; Z是N或CR2'。

5. 发明授权

US07812041B2 Heterocyclic NF-κB inhibitors 失效
标题翻译：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
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： A01N43/78 , A01N43/50 , A01N43/76 , A01N43/36 , A61K31/425 , A61K31/415 , A61K31/42 , C07D277/04 , C07D277/08 , C07D263/02 , C07D413/00 , C07D233/00 , C07D233/02 , C07D207/00 , C07D295/00
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 (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。

6. 发明申请

US20100048583A1 Novel Heterocyclic NF-kB Inhibitors 审中-公开
标题翻译：新型杂环NF-kB抑制剂
公开(公告)号：US20100048583A1
公开(公告)日：2010-02-25
申请号：US12546505
申请日：2009-08-24
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： A61K31/497 , C07D401/14 , A61K31/445 , A61P25/28 , A61P31/04 , A61P31/12
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 (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, 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R1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，芳烷基或取代的芳烷基 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，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。

7. 发明申请

US20100048574A1 NOVEL HETEROCYCLIC NF-kB INHIBITORS 审中-公开
标题翻译：新型杂环NF-kB抑制剂
公开(公告)号：US20100048574A1
公开(公告)日：2010-02-25
申请号：US12576475
申请日：2009-10-09
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： A61K31/53 , C07D401/14 , C07D409/14 , C07D253/06 , A61K31/497 , A61P25/28 , A61P9/10
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 (II): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.
摘要翻译：本发明涉及通式（II）的化合物或其与酸或碱的药学上可接受的盐，或其药学上可接受的前药或立体异构体。

8. 发明授权

US07601745B2 Heterocyclic NF-kB inhibitors 失效
标题翻译：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
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： A01N43/52 , A01N43/78 , A61K31/415 , A61K31/425 , C07D235/04 , C07D263/58 , C07D263/60 , C07D277/82 , C07D403/02 , C07D413/00 , C07D498/00
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（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。

9. 发明申请

US20080261971A1 Novel Heterocyclic Nf-Kb Inhibitors 失效
标题翻译：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
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： A61K31/5377 , A61P35/00 , A61P25/00 , A61P31/00 , A61P19/00 , C07D417/14 , A61K31/427 , A61K31/53 , A61K31/4545 , A61K31/496 , A61K31/497
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

10. 发明授权

US08106048B2 Heterocyclic NF-κB inhibitors 失效
标题翻译：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。

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