公开(公告)号：US20110230524A1

公开(公告)日：2011-09-22

申请号：US13130311

申请日：2009-11-27

申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Pavel Mikhailovich Yamanushkin ,  Oleg Dmitrievich Mitkin ,  Vladimir Yurievich Vvedensky ,  Vadim Vasilievich Bichko

发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Pavel Mikhailovich Yamanushkin ,  Oleg Dmitrievich Mitkin ,  Vladimir Yurievich Vvedensky ,  Vadim Vasilievich Bichko

IPC分类号： A61K31/4439 ,  C07D209/18 ,  C07D209/20 ,  C07D209/26 ,  C07D401/12 ,  C07D209/24 ,  C07D401/06 ,  C07D401/10 ,  A61K31/405 ,  A61P31/12 ,  A61P31/16 ,  A61P31/14

CPC分类号： C07F1/005 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/4858 ,  A61K47/10 ,  C07D209/32 ,  C07D209/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12

摘要： The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.Novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, their esters of the general formula 1 and pharmaceutically acceptable salts and/or hydrates thereof have been disclosed wherein: R1 represents amino group substituent selected from hydrogen, optionally substituted C1-C5 alkyl, acyl or sulfonyl; R2 and R4 independently of each other represent alkyl substituent selected from hydrogen, halogen, optionally substituted C1-C3 alkyl, optionally substituted hydroxyl, optionally substituted amino group, optionally substituted aminomethyl, substituted mercapto group; R3 represents hydrogen, optionally substituted lower C1-C5 alkyl; R5 represents cyclic system substituent selected from hydrogen, fluorine, trifluoromethyl, carboxy group, alkyloxycarbonyl, possibly substituted aryl, heterocyclyl, optionally substituted aminomethyl, cyano group; R6 represents hydroxyl group substituent selected from hydrogen, optionally substituted C1-C5 alkyl, acyl.

摘要翻译： 本发明涉及新的取代的2-（5-羟基-2-甲基-1H-吲哚-3-基）乙酸，新颖的抗病毒活性成分，药物组合物，抗病毒药物，预防和治疗病毒性疾病的方法，特别是 由流感病毒和感染性肝炎C（HCV）病毒引起。 已经公开了新的取代的2-（5-羟基-2-甲基-1H-吲哚-3-基）乙酸，它们的通式1的酯及其药学上可接受的盐和/或水合物，其中：R1代表氨基取代基 选自氢，任选取代的C 1 -C 5烷基，酰基或磺酰基; R 2和R 4彼此独立地表示选自氢，卤素，任选取代的C 1 -C 3烷基，任选取代的羟基，任选取代的氨基，任选取代的氨基甲基，取代的巯基的烷基取代基; R3表示氢，任选取代的低级C 1 -C 5烷基; R5表示选自氢，氟，三氟甲基，羧基，烷氧基羰基，可能取代的芳基，杂环基，任选取代的氨基甲基，氰基的环状体系取代基。 R 6表示选自氢，任选取代的C 1 -C 5烷基，酰基的羟基取代基。

公开(公告)号：US08481587B2

公开(公告)日：2013-07-09

申请号：US13130311

申请日：2009-11-27

申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Pavel Mikhailovich Yamanushkin ,  Oleg Dmitrievich Mitkin ,  Vladimir Yurievich Vvedensky ,  Vadim Vasilievich Bichko

发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Pavel Mikhailovich Yamanushkin ,  Oleg Dmitrievich Mitkin ,  Vladimir Yurievich Vvedensky ,  Vadim Vasilievich Bichko

IPC分类号： A61K31/405 ,  C07D209/12

CPC分类号： C07F1/005 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/4858 ,  A61K47/10 ,  C07D209/32 ,  C07D209/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12

摘要： The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.Novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, their esters of the general formula 1 and pharmaceutically acceptable salts and/or hydrates thereof have been disclosed wherein: R1 represents amino group substituent selected from hydrogen, optionally substituted C1-C5 alkyl, acyl or sulfonyl; R2 and R4 independently of each other represent alkyl substituent selected from hydrogen, halogen, optionally substituted C1-C3 alkyl, optionally substituted hydroxyl, optionally substituted amino group, optionally substituted aminomethyl, substituted mercapto group; R3 represents hydrogen, optionally substituted lower C1-C5 alkyl; R5 represents cyclic system substituent selected from hydrogen, fluorine, trifluoromethyl, carboxy group, alkyloxycarbonyl, possibly substituted aryl, heterocyclyl, optionally substituted aminomethyl, cyano group; R6 represents hydroxyl group substituent selected from hydrogen, optionally substituted C1-C5 alkyl, acyl.

摘要翻译： 本发明涉及新的取代的2-（5-羟基-2-甲基-1H-吲哚-3-基）乙酸，新颖的抗病毒活性成分，药物组合物，抗病毒药物，预防和治疗病毒性疾病的方法，特别是 由流感病毒和感染性肝炎C（HCV）病毒引起。 已经公开了新的取代的2-（5-羟基-2-甲基-1H-吲哚-3-基）乙酸，它们的通式1的酯及其药学上可接受的盐和/或水合物，其中：R1代表氨基取代基 选自氢，任选取代的C 1 -C 5烷基，酰基或磺酰基; R 2和R 4彼此独立地表示选自氢，卤素，任选取代的C 1 -C 3烷基，任选取代的羟基，任选取代的氨基，任选取代的氨基甲基，取代的巯基的烷基取代基; R3表示氢，任选取代的低级C 1 -C 5烷基; R5表示选自氢，氟，三氟甲基，羧基，烷氧基羰基，可能取代的芳基，杂环基，任选取代的氨基甲基，氰基的环状体系取代基。 R 6表示选自氢，任选取代的C 1 -C 5烷基，酰基的羟基取代基。