公开(公告)号：US08329689B2

公开(公告)日：2012-12-11

申请号：US12600251

申请日：2007-05-17

申请人： Andrey Alexandrovich Ivashchenko ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Oleg Dmitrievich Mitkin ,  Ilya Matusovich Okun ,  Alexandr Sergeevich Kyselvev ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivachtchenko

发明人： Andrey Alexandrovich Ivashchenko ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Oleg Dmitrievich Mitkin ,  Ilya Matusovich Okun ,  Alexandr Sergeevich Kyselvev ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivachtchenko

IPC分类号： A61K31/404 ,  A61K31/407 ,  C07D209/12 ,  C07D498/04

CPC分类号： C07D401/14 ,  C07D209/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D498/04

摘要： The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu. The invention proposes novel substituted indoles of general formula (1) or the racemates or the optical isomers or the pharmaceutically acceptable salts and/or hydrates thereof, wherein R1, R14 and R24 independently of each other are an aminogroup substituent selected for hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, or R14 and R24 together with a nitrogen atom, with which they are bound, form through R14 and R24 optionally substituted azaheterocyclyl or guanidyl; R2 is analkyl substituent selected from hydrogen, an optionally substituted mercaptogroup, optionally substituted aminogroup and optionally substituted hydroxyl; R3 is lower alkyl, R5 is an hydrogen atom or R5 together with an oxygen atom with which it is linked or R24 together with a nitrogen atom with which it is linked close, via R5 and R24 an oxazine cycle; R6 is a cyclic system substituent selected for hydrogen, a halogen atom, cyanogroup, optionally substituted aryl or substituted heterocyclyl.

摘要翻译： 本发明涉及以药物组合物物质形式使用的新型取代的吲哚，以及所述组合物用于制备用于预防和治疗病毒性疾病，特别是感染性肝炎（HCV，HBV）病毒引起的药物制剂的用途， ，人类免疫缺陷（HIV），非典型肺炎（SARS）和禽流感。 本发明提出了通式（1）的新型取代吲哚或其外消旋物或光学异构体或其药学上可接受的盐和/或水合物，其中R1，R14和R24彼此独立地是选自氢的氨基取代基， 烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂环基，或R 14和R 24与它们所连接的氮原子一起通过R 14和R 24任选取代的杂环基或胍基形成; R2是选自氢，任选取代的巯基，任选取代的氨基和任选取代的羟基的烷基取代基; R 3是低级烷基，R 5是氢原子或R 5与连接的氧原子连在一起，或者R 24与其连接的氮原子一起通过R5和R24进行恶嗪循环; R6是选择用于氢，卤素原子，氰基，任选取代的芳基或取代的杂环基的环系取代基。

公开(公告)号：US20110160197A1

公开(公告)日：2011-06-30

申请号：US12600251

申请日：2007-05-17

申请人： Andrey Alexandrovich Ivashchenko ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Oleg Dmitrievich Mitkin ,  Ilya Matusovich Okun ,  Alexandr Sergeevich Kyselvev ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivachtchenko

发明人： Andrey Alexandrovich Ivashchenko ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Oleg Dmitrievich Mitkin ,  Ilya Matusovich Okun ,  Alexandr Sergeevich Kyselvev ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivachtchenko

IPC分类号： A61K31/404 ,  C07D209/42 ,  C07D403/10 ,  C07D401/10 ,  A61K31/4725 ,  A61K31/454 ,  A61K31/496 ,  C07D498/04 ,  A61K31/5365 ,  A61K31/5377 ,  A61P31/16 ,  A61P31/18 ,  A61P31/20 ,  A61P31/14

CPC分类号： C07D401/14 ,  C07D209/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D498/04

摘要： The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu. The invention proposes novel substituted indoles of general formula (1) or the racemates or the optical isomers or the pharmaceutically acceptable salts and/or hydrates thereof, wherein R1, R14 and R24 independently of each other are an aminogroup substituent selected for hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, or R14 and R24 together with a nitrogen atom, with which they are bound, form through R14 and R24 optionally substituted azaheterocyclyl or guanidyl; R2 is analkyl substituent selected from hydrogen, an optionally substituted mercaptogroup, optionally substituted aminogroup and optionally substituted hydroxyl; R3 is lower alkyl, R5 is an hydrogen atom or R5 together with an oxygen atom with which it is linked or R24 together with a nitrogen atom with which it is linked close, via R5 and R24 an oxazine cycle; R6 is a cyclic system substituent selected for hydrogen, a halogen atom, cyanogroup, optionally substituted aryl or substituted heterocyclyl.

摘要翻译： 本发明涉及以药物组合物物质形式使用的新型取代的吲哚，以及所述组合物用于制备用于预防和治疗病毒性疾病的药物制剂的用途，特别是由感染性肝炎（HCV，HBV）病毒引起的病毒性疾病， ，人类免疫缺陷（HIV），非典型肺炎（SARS）和禽流感。 本发明提出了通式（1）的新型取代吲哚或其外消旋体或光学异构体或其药学上可接受的盐和/或水合物，其中R1，R14和R24彼此独立地是选自氢的氨基取代基， 烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂环基，或R 14和R 24与它们所连接的氮原子一起通过R 14和R 24任选取代的杂环基或胍基形成; R2是选自氢，任选取代的巯基，任选取代的氨基和任选取代的羟基的烷基取代基; R 3是低级烷基，R 5是氢原子或R 5与连接的氧原子连在一起，或者R 24与其连接的氮原子一起通过R5和R24进行恶嗪循环; R6是选择用于氢，卤素原子，氰基，任选取代的芳基或取代的杂环基的环系取代基。