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。

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。

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。

公开(公告)号：US08343963B2

公开(公告)日：2013-01-01

申请号：US12696479

申请日：2010-01-29

申请人： Stefano Pegoraro

发明人： Stefano Pegoraro

IPC分类号： A61K31/5375 ,  A61K31/541 ,  A61K31/495 ,  A61K31/17 ,  C07C311/47 ,  C07D207/09 ,  C07D211/22 ,  C07D211/62 ,  C07D213/36 ,  C07D215/42 ,  C07D277/04 ,  C07D279/12

CPC分类号： C07D295/13 ,  C07C311/47 ,  C07C317/42 ,  C07D207/09 ,  C07D207/14 ,  C07D209/44 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D211/74 ,  C07D213/36 ,  C07D215/42 ,  C07D241/08 ,  C07D277/04 ,  C07D279/12 ,  C07D295/15 ,  C07D295/205 ,  C07D295/26 ,  C07D307/14 ,  C07D307/64 ,  C07D317/28

摘要： The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.

摘要翻译： 本发明涉及具有式（I）的新型氨磺酰基 - 苯基 - 脲基化合物或其生理上可接受的盐或衍生物，其适于治疗由原生动物引起的感染，特别是由疟原虫引起的不复杂或严重的疟疾。

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。

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