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1. 发明申请

US20070149523A1 Thiazole Analogues and Uses Thereof 审中-公开
标题翻译：噻唑类似物及其用途
公开(公告)号：US20070149523A1
公开(公告)日：2007-06-28
申请号：US11559662
申请日：2006-11-14
申请人： Jan Ehlert , Thomas Herz , Rolf Krauss , Micheal Kubbutat , Martin Lang , Stefano Pegoraro , Christoph Schachtele , Frank Totzke , Ute Zirrgiebel
发明人： Jan Ehlert , Thomas Herz , Rolf Krauss , Micheal Kubbutat , Martin Lang , Stefano Pegoraro , Christoph Schachtele , Frank Totzke , Ute Zirrgiebel
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/52 , A61K31/519 , A61K31/506 , A61K31/4745 , A61K31/4439 , C07D473/02 , C07D487/02 , C07D417/02
CPC分类号： C07D417/12
摘要： Compounds of formula (I) and salts and physiologically functional derivatives thereof, wherein R2 is attached at the 4- or 5-position of the thiazole ring and is hydrogen, alkyl, halogen, cyano, alkoxy, haloalkoxy, or alkylamino; X independently represents a divalent linkage group selected from S, O, NR4, SO, or SO2; R4 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, or heterocyclyl; R1 is attached at the 4- or 5-position of the thiazole ring and independently represents a group of formula (II): wherein the dotted line represents a single or double bond; * indicates the point of attachment to the thiazole ring; and n is 1, 2, or 3. Also disclosed are pharmaceutical compositions comprising the above compounds and method of treatments for cancer and other diseases.
摘要翻译：式（I）化合物及其盐和生理功能衍生物，其中R 2连接在噻唑环的4-或5-位，并且是氢，烷基，卤素，氰基，烷氧基，卤代烷氧基或烷基氨基; X独立地表示选自S，O，NR 4，SO或SO 2的二价键合基团。 R 4是氢，烷基，环烷基，环烷基烷基或杂环基; R 1连接在噻唑环的4-或5-位，独立地表示式（II）的基团：其中虚线表示单键或双键; *表示与噻唑环的连接点; 并且n为1,2或3.还公开了包含上述化合物的药物组合物和用于癌症和其它疾病的治疗方法。

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. 发明授权

US06949567B2 Compounds for the treatment of protozoal diseases 失效
标题翻译：用于治疗原生动物疾病的化合物
公开(公告)号：US06949567B2
公开(公告)日：2005-09-27
申请号：US10083008
申请日：2002-02-26
申请人： Andrea Aschenbrenner , Katharina Aulinger Fuchs , Matthias Dormeyer , Gabriel Garcia , Bernd Kramer , Jürgen Kraus , Rolf Krauss , Johan Leban , Stefano Pegoraro , Wael Saeb , Kristina Wolf
发明人： Andrea Aschenbrenner , Katharina Aulinger Fuchs , Matthias Dormeyer , Gabriel Garcia , Bernd Kramer , Jürgen Kraus , Rolf Krauss , Johan Leban , Stefano Pegoraro , Wael Saeb , Kristina Wolf
IPC分类号： A61P33/02 , A61P35/00 , C07C275/40 , C07C275/42 , C07C311/21 , C07C311/37 , C07C311/38 , C07C311/46 , C07C311/47 , C07C317/50 , C07C323/44 , C07C335/22 , C07D209/48 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/24 , C07D261/18 , C07D277/82 , C07D295/13 , C07D307/14 , C07D333/38 , C07D333/54 , C07D413/12 , A61K31/17 , C07C275/28 , C07C275/30
CPC分类号： C07D209/48 , C07C275/40 , C07C275/42 , C07C311/21 , C07C311/37 , C07C311/38 , C07C311/46 , C07C311/47 , C07C317/50 , C07C323/44 , C07C335/22 , C07C2603/74 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/24 , C07D261/18 , C07D277/82 , C07D295/13 , C07D307/14 , C07D333/38 , C07D333/54
摘要： The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C═O, C═S, C═NH, (C═O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.
摘要翻译：本发明涉及具有式（I）的新的二苯脲或其盐，其中Y是C-O，C-S，C-NH，（C-O）2或SO 2。以及这些化合物的制备方法及其在治疗原生动物疾病中的用途以及细胞内蛋白质降解途径的抑制是有益的疾病。

4. 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，

5. 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'。

6. 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。

7. 发明申请

US20100216772A1 Novel Phenantridine Analogues and Uses Thereof 审中-公开
标题翻译：新型苯那啶类似物及其用途
公开(公告)号：US20100216772A1
公开(公告)日：2010-08-26
申请号：US11568500
申请日：2004-10-05
申请人： Stefano Pegoraro , Martin Lang , Juliane Feurle , Jürgen Krauss
发明人： Stefano Pegoraro , Martin Lang , Juliane Feurle , Jürgen Krauss
IPC分类号： A61K31/5513 , A61P17/06 , A61P17/14 , A61P37/06 , C07D221/12 , A61K31/473 , C07D401/04 , C07D413/10 , A61K31/5377 , C07D223/18
CPC分类号： C07D221/12 , C07D233/18 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of the general formula (IV) and (II) and salts and physiologically functional derivatives thereof, wherein X is C—R8 or N; and Z is independently one of the following groups:
摘要翻译：本发明涉及通式（IV）和（II）的化合物及其盐和生理功能衍生物，其中X为C-R8或N; Z独立地为以下组之一：

8. 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。

9. 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。

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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