公开(公告)号：US08618114B2

公开(公告)日：2013-12-31

申请号：US13122152

申请日：2009-10-06

申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC分类号： C07D487/04

摘要： The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.In the general formula 1: wherein: X=S, SO or NH; R1 represents hydrogen, optionally substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R2 represents hydrogen, halogen, optionally substituted C1-C3alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R3 represents hydrogen, optionally substituted C1-C3alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X=S or X=NH, at least one of R1, R2 or R3 represent substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R1, R2 or R3 represent hydrogen; R4 represents C1-C3alkyl; R5 represents hydrogen, one or two halogens, C1-C3alkyl or optionally substituted hydroxyl.

摘要翻译： 本发明涉及通式1的新的取代的3-芳基磺酰基 - 吡唑并[1,5-a]嘧啶，其药学上可接受的盐和/或水合物，5-羟色胺5-HT 6受体拮抗剂和药物组合物，还涉及 预防和治疗人类和温血动物的各种中枢神经系统疾病，其发病机制与血清素5-HT6受体，特别是阿尔茨海默病，帕金森病，亨廷顿病，精神分裂症和其他神经变性疾病，认知障碍 和肥胖。 在通式1中：其中：X = S，SO或NH; R 1表示氢，任选取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基或杂环基; R 2表示氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，芳基二氮烯基或任选取代的氨基; R 3表示氢，任选取代的C 1 -C 3烷基，取代的羟基，吡啶基或任选取代的氨基，此外，在X = S或X = NH的情况下，R 1，R 2或R 3中的至少一个表示取代的C 1 -C 3烷基，环烷基， 金刚烷基，芳基，杂环基，卤素，取代的羟基，任选取代的氨基，芳基二氮烯基或R 1，R 2或R 3中的至少两个表示氢; R4代表C1-C3烷基; R5表示氢，一个或两个卤素，C1-C3烷基或任选取代的羟基。

公开(公告)号：US20110178078A1

公开(公告)日：2011-07-21

申请号：US13122152

申请日：2009-10-06

申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

IPC分类号： A61K31/5377 ,  A61K31/497 ,  A61K31/519 ,  C07D487/04 ,  A61P3/04 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P3/10

CPC分类号： C07D487/04

摘要： The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.In the general formula 1: wherein: X═S, SO or NH; R1 represents hydrogen, optionally substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R2 represents hydrogen, halogen, optionally substituted C1-C3alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R3 represents hydrogen, optionally substituted C1-C3alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X═S or X═NH, at least one of R1, R2 or R3 represent substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R1, R2 or R3 represent hydrogen; R4 represents C1-C3alkyl; R5 represents hydrogen, one or two halogens, C1-C3alkyl or optionally substituted hydroxyl.

摘要翻译： 本发明涉及通式1的新的取代的3-芳基磺酰基 - 吡唑并[1,5-a]嘧啶，其药学上可接受的盐和/或水合物，5-羟色胺5-HT 6受体拮抗剂和药物组合物，还涉及 预防和治疗人类和温血动物的各种中枢神经系统疾病，其发病机制与血清素5-HT6受体，特别是阿尔茨海默病，帕金森病，亨廷顿病，精神分裂症和其他神经变性疾病，认知障碍 和肥胖。 在通式1中：其中：X = S，SO或NH; R 1表示氢，任选取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基或杂环基; R 2表示氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，芳基二氮烯基或任选取代的氨基; R 3表示氢，任选取代的C 1 -C 3烷基，取代的羟基，吡啶基或任选取代的氨基，此外，在X = S或X = NH的情况下，R 1，R 2或R 3中的至少一个表示取代的C 1 -C 3烷基，环烷基， 金刚烷基，芳基，杂环基，卤素，取代的羟基，任选取代的氨基，芳基二氮烯基或R 1，R 2或R 3中的至少两个表示氢; R4代表C1-C3烷基; R5表示氢，一个或两个卤素，C1-C3烷基或任选取代的羟基。

公开(公告)号：US20120071493A1

公开(公告)日：2012-03-22

申请号：US13320911

申请日：2010-04-30

申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Oleg Dmitrievich Mitkin ,  Volodymyr Mikhailovich Kysil

发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Oleg Dmitrievich Mitkin ,  Volodymyr Mikhailovich Kysil

IPC分类号： A61K31/437 ,  A61K31/497 ,  A61P25/24 ,  A61P25/22 ,  A61P25/28 ,  A61P25/18 ,  C07D471/04 ,  A61P25/00

CPC分类号： A61K31/437 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/4858 ,  A61K47/10 ,  C07D471/04

摘要： The invention relates to novel substituted 8-sulfonyl-2,3,4,5-tetrahydro-1H-γ-carbolines of the general formula 1 and their pharmaceutically acceptable salt—ligands exhibiting biological activity simultaneously towards alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepinefrine receptors, serotonin receptors, to active components, pharmaceutical compositions, comprising as an active component novel ligands, to novel medicaments intended for treatment of conditions and diseases of central nervous system. In the general formula 1 R1 represents a substituent selected from hydrogen, optionally substituted C1-C3 alkyl or C1-C4 alkyloxycarbonyl; R2 represents a cyclic system substituent selected from hydrogen, optionally substituted C1-C3 alkyl, optionally substituted C2-C3 alkenyl or substituted sulfonyl; R3 represents optionally substituted aryl or substituted amino group.

摘要翻译： 本发明涉及通式1的新的取代的8-磺酰基-2,3,4,5-四氢-1H-γ-咔啉及其药学上可接受的盐配体，其表现出与α-肾上腺素能受体，多巴胺受体，组胺 受体，咪唑啉受体，西格玛受体，诺诺福瑞汀受体，5-羟色胺受体，活性组分，药物组合物，作为活性成分的新型配体，用于治疗中枢神经系统病症和疾病的新型药物。 在通式1中，R 1表示选自氢，任选取代的C 1 -C 3烷基或C 1 -C 4烷氧基羰基的取代基; R2表示选自氢，任选取代的C 1 -C 3烷基，任选取代的C 2 -C 3烯基或取代的磺酰基的环状体系取代基; R3表示任选取代的芳基或取代的氨基。

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。

公开(公告)号：US20100120792A1

公开(公告)日：2010-05-13

申请号：US12594453

申请日：2008-04-01

申请人： Andrey Alexandrovich Ivashchenko ,  Alexandre Vasilievich Ivachtchenko ,  Sergey Yevgenievich Tkachenko ,  Evgueni Borisovich Frolov ,  Oleg Dmitrievich Mitkin ,  llya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Yan Lavrovsky

发明人： Andrey Alexandrovich Ivashchenko ,  Alexandre Vasilievich Ivachtchenko ,  Sergey Yevgenievich Tkachenko ,  Evgueni Borisovich Frolov ,  Oleg Dmitrievich Mitkin ,  llya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Yan Lavrovsky

IPC分类号： A61K31/4427 ,  A61K31/4745 ,  C07D471/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/28 ,  A61P25/24 ,  A61P25/22 ,  A61P9/10

CPC分类号： A61K31/437 ,  A61K31/444 ,  C07D471/04

摘要： The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2, is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH═CH—, or ethynyl group —C≡C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.

摘要翻译： 本发明涉及同时调节细胞中Ca 2+离子的体内平衡的5-羟色胺5-HT6受体的拮抗剂，代表通式1的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚 ，其药学上可接受的盐和/或水合物。 在通式1中：R 1表示选自任选取代的C 1 -C 5烷基的氨基取代基; R2是选自氢，卤素，C1-C3烷基，CF3，OCF3中的一个或多个取代基; Ar是任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，取代的氨基或CF 3取代的苯基; 或在该循环中任选取代的包含1-2个氮原子的芳族6-元杂环; W表示亚乙基-CH 2 -CH 2 - ，乙烯基-CH = CH-或乙炔基-C≡C-。 本发明还涉及选自通式1的化合物，其制备方法，药物组合物及其用途的新化合物。

公开(公告)号：US08541437B2

公开(公告)日：2013-09-24

申请号：US12594453

申请日：2008-04-01

申请人： Andrey Alexandrovich Ivashchenko ,  Alexandre Vasilievich Ivachtchenko ,  Sergey Yevgenievich Tkachenko ,  Evgueni Borisovich Frolov ,  Oleg Dmitrievich Mitkin ,  Dmitri Vladimirovich Kravchenko ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Yan Lavrovsky

发明人： Andrey Alexandrovich Ivashchenko ,  Alexandre Vasilievich Ivachtchenko ,  Sergey Yevgenievich Tkachenko ,  Evgueni Borisovich Frolov ,  Oleg Dmitrievich Mitkin ,  Dmitri Vladimirovich Kravchenko ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Yan Lavrovsky

IPC分类号： C07D471/04 ,  A61K31/437

CPC分类号： A61K31/437 ,  A61K31/444 ,  C07D471/04

摘要： The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2i is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH═CH—, or ethynyl group —C≡C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.

摘要翻译： 本发明涉及同时调节细胞中Ca 2+离子的体内平衡的5-羟色胺5-HT6受体的拮抗剂，代表通式1的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚 ，其药学上可接受的盐和/或水合物。 在通式1中：R 1表示选自任选取代的C 1 -C 5烷基的氨基取代基; R2i是一个或多个选自氢，卤素，C1-C3烷基，CF3，OCF3的取代基; Ar是任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，取代的氨基或CF 3取代的苯基; 或在该循环中任选取代的包含1-2个氮原子的芳族6-元杂环; W表示亚乙基-CH 2 -CH 2 - ，乙烯基-CH = CH-或乙炔基-C = C-。 本发明还涉及选自通式1的化合物，其制备方法，药物组合物及其用途的新化合物。

公开(公告)号：US20110039825A1

公开(公告)日：2011-02-17

申请号：US12810013

申请日：2008-12-19

申请人： Andrey Alexandrovich Ivashchenko ,  Vasilievich Ivashchenko ,  Yan Vadimovich Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Ilya Matusovich Okun

发明人： Andrey Alexandrovich Ivashchenko ,  Vasilievich Ivashchenko ,  Yan Vadimovich Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Ilya Matusovich Okun

IPC分类号： A61K31/55 ,  C07D471/04 ,  A61K31/437 ,  A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  A61P25/28 ,  A61P25/24

CPC分类号： C07D471/04 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/4858 ,  A61K31/407 ,  A61K31/437 ,  A61K31/55 ,  C07D487/04

摘要： The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously α-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates, wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C1-C4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH2)m group, optionally substituted CH═CH group, optionally substituted CH2—CH═CH group, C≡C group, SO2 group; n=1, 2; m=1, 2, 3; solid line accompanied by dotted line, i.e. may represent single or double bond. The invention also relates to active ingredients, pharmaceutical compositions comprising the said ligands as active ingredients; to novel medicaments useful for treatment of diseases and conditions of central nervous system (CNS) of humans and warm-blooded animals.

摘要翻译： 本发明涉及其具有广谱生物活性的新配体，其包括同时α-肾上腺素受体，多巴胺受体，组胺受体，咪唑啉受体和5-羟色胺受体，其中5-羟色胺5-HT 7受体是通式1的化合物，其形式为 游离碱，几何异构体，外消旋混合物或单独的光学异构体，药学上可接受的盐和/或水合物，其中：R1是氨基的取代基，其选自氢，任选取代的C 1 -C 4烷基，酰基，杂环基，烷氧基羰基，取代的 磺酰基 R2是选自氢，卤素，任选取代的C 1 -C 4烷基，CF 3，CN，烷氧基，烷氧基羰基，羧基，杂环基或取代的磺酰基的环状体系的取代基。 Ar是任选取代的芳基，不一定与杂环基或任选取代的芳族杂环基取代; W是任选取代的（CH 2）m基团，任选取代的CH = CH基团，任选取代的CH 2 -CH = CH基团，C≡C基团，SO 2基团; n = 1,2; m = 1,2,3。 伴有虚线的实线即可表示单键或双键。 本发明还涉及活性成分，包含所述配体作为活性成分的药物组合物; 用于治疗人类和温血动物的中枢神经系统（CNS）的疾病和病症的新型药物。

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：US20180030080A1

公开(公告)日：2018-02-01

申请号：US15221613

申请日：2016-07-28

申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  ASAVI, LLC

发明人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  Andrey Alexandrovich Ivashchenko ,  Alena Alexandrovna Ivachtchenko ,  Nikolay Filippovich Savchuk

IPC分类号： C07H19/16 ,  C07H19/06 ,  C07F9/6558 ,  C07F9/6561

CPC分类号： C07H19/16 ,  A61P31/12 ,  A61P35/00 ,  C07F9/65586 ,  C07F9/65616 ,  C07H19/06 ,  C07H19/10 ,  C07H19/20

摘要： The present invention pertains to chemotherapeutic agents and their use for treating viral and cancerous diseases. These compounds are inhibitors of HCV NS5B polymerase, HBV DNA polymerase and, HIV-1 reverse transcriptase (RT) inhibitor, and for treatment of hepatitis B and C infection in mammals. These compounds are also of interest for the treatment of cancer.The phosphoramidate nucleoside prodrug of the general formula 1, a stereoisomer, isotope-enriched analogue, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: Ar is aryl or hetaryl; R1 is H or CH3; R2 is the substituent selected from OCH2CH═CH2, OCH2CH≡CH, OCH2CH2CH2OCH3, R3 is H or CH3; R4 is OH, OR5, NR6R7; R5 is C1-C4-alkyl; R6 and R7 are not necessarily the same substituents selected from H or CH3; Z═O, or NH; an arrow (→) indicates the place of substituent connection; Nuc is R8 and R9 are not necessarily the same substituents selected from H, F, Cl, CH3 or OH provided when continuous line and its accompanying dotted line () together are the single carbon-carbon (C—C) bond or R8 and R9 are hydrogen provided when continuous line and its accompanying dotted line () together are the double carbon-carbon bond (C═C); R10 is the substituent selected from R10.1-R10.5; R11 is the substituent selected from H, F, Cl, CH3, or CF3; R12 is hydrogen, C1-C4-alkyl or C3-C6-cycloalkyl; X is oxygen or ethanediyl-1,1 (C═CH2); Y is O, S, CH2, or HO—CH group provided when continuous line and its accompanying dotted line () together are the single carbon-carbon (C—C) bond or Y is CH group provided when continuous line and its accompanying dotted line () together are the double carbon-carbon bond (C═C), and compound of the general formula 1, stereoisomers, isotope-enriched analogues, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, wherein: Ar is aryl or hetaryl; R1 is H or CH3; R is isopropyl; Nuc is