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1. 发明申请

US20110039870A1 TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：四氢吡喃并[1,5-A]吡啶并吡啶作为丝氨酸5-HT6受体的拮抗剂，其生产和使用方法
公开(公告)号：US20110039870A1
公开(公告)日：2011-02-17
申请号：US12937720
申请日：2009-04-30
申请人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Evashchenko
发明人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Evashchenko
IPC分类号： A61K31/519 , C07D471/14 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/22 , A61P3/10 , A61P3/04 , C12N5/02
CPC分类号： C07D471/14 , A61K31/519
摘要： The present invention relates to serotonin 5-HT6 receptor antagonists-novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors.In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 is hydrogen, optionally substituted lower C1-C3 alkyl, substituted hydroxyl group, substituted sulfanyl group; R2 is hydrogen or optionally substituted C1-C3 alkyl; R3 is hydrogen, optionally substituted C1-C3 alkyl or tert.-butyloxycarbonyl.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型取代的3-磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的3-磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，包含上述化合物的药物的药物和药物组合物，以及各种条件的预防和治疗方法人类的中枢神经系统疾病和温血动物，其发病机制与血清素5-HT6受体有关。在式1和2中Ar是任选取代的芳基或任选取代的杂环基; R1是氢，任选取代的低级C 1 -C 3烷基，取代的羟基，取代的硫烷基; R2是氢或任选取代的C 1 -C 3烷基; R3是氢，任选取代的C 1 -C 3烷基或叔丁氧基羰基。

2. 发明授权

US08552017B2 2-amino-3-sulphonyl-tetrahydro-pyrazolo[1,5-A]pyrido-pyrimidine antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof 有权
标题翻译： 5-羟色胺5-HT6受体的2-氨基-3-磺酰基 - 四氢 - 吡唑并[1,5-A]吡啶并 - 嘧啶拮抗剂，其制备方法和用途
公开(公告)号：US08552017B2
公开(公告)日：2013-10-08
申请号：US12937718
申请日：2009-04-30
申请人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
发明人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00
CPC分类号： C07D471/14 , A61K31/519
摘要： The invention relates to serotonin 5-HT6 receptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT6 receptors including cognitive and neurodegenerative diseases.Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is hydrogen, optionally substituted C1-C3 alkyl, C1-C4 alkyloxycarbonyl; R2 is hydrogen, halogen or optionally substituted C1-C3 alkyl; R13 and R23 represent optionally alike: hydrogen, optionally substituted C1-C3 alkyl or R13 and R23 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基 -3-芳基磺酰基-5,6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，药物物质和药物组合物，其包含作为所述化合物的所述药物物质，预防和治疗人类和动物的中枢神经系统的各种疾病，其发病机制与血清素5-HT6受体（包括认知和神经变性疾病）相关。通式1的取代的2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基-3-芳基磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，及其药学上可接受的盐和/或水合物。其中：Ar是任选取代的芳基或任选取代的杂芳基; R 1是氢，任选取代的C 1 -C 3烷基，C 1 -C 4烷氧基羰基; R2是氢，卤素或任选取代的C 1 -C 3烷基; R 13和R 23任选地相似：氢，任选取代的C 1 -C 3烷基或R 13和R 23与它们所连接的氮原子一起形成任选取代的杂环。

3. 发明授权

US08569318B2 Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof 有权
标题翻译：四氢吡唑并[1,5-a]吡啶并嘧啶作为5-羟色胺5-HT 6受体的拮抗剂，其生产和使用方法
公开(公告)号：US08569318B2
公开(公告)日：2013-10-29
申请号：US12937720
申请日：2009-04-30
申请人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
发明人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00
CPC分类号： C07D471/14 , A61K31/519
摘要： The present invention relates to serotonin 5-HT6 receptor antagonists-novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors.In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 is hydrogen, optionally substituted lower C1-C3 alkyl, substituted hydroxyl group, substituted sulfanyl group; R2 is hydrogen or optionally substituted C1-C3 alkyl; R3 is hydrogen, optionally substituted C1-C3 alkyl or tert.-butyloxycarbonyl.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型取代的3-磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的3-磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，包含上述化合物的药物的药物和药物组合物，以及各种条件的预防和治疗方法人类的中枢神经系统疾病和温血动物，其发病机制与血清素5-HT6受体有关。在式1和2中Ar是任选取代的芳基或任选取代的杂环基; R1是氢，任选取代的低级C 1 -C 3烷基，取代的羟基，取代的硫烷基; R2是氢或任选取代的C 1 -C 3烷基; R3是氢，任选取代的C 1 -C 3烷基或叔丁氧基羰基。

4. 发明授权

US08329689B2 Substituted indoles and a method for the production and use thereof 失效
标题翻译：取代的吲哚及其制备和使用方法
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。

5. 发明申请

US20120071493A1 SUBSTITUTED 8-SULFONYL-2,3,4,5-TETRAHYDRO-1H-GAMMA-CARBOLINES, LIGANDS AND PHARMACEUTICAL COMPOSITION; METHOD FOR THE PRODUCTION AND USE OF SAME 审中-公开
标题翻译：取代的8-磺基-2,3,4,5-四氢-1H-咪唑碳水化合物，配体和药物组合物; 生产和使用相同方法
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。

6. 发明申请

US20110160197A1 Substituted Indoles and a Method for the Production and Use Thereof 失效
标题翻译：取代的吲哚及其生产和使用方法
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。

7. 发明申请

US20110046149A1 2-AMINO-3-SULPHONYL-TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINE ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：丝氨酸5-HT6受体的2-氨基-3-磺酰基 - 四氢吡喃并[1,5-A]吡啶并 - 吡咯烷酮拮抗剂，其生产方法及其用途
公开(公告)号：US20110046149A1
公开(公告)日：2011-02-24
申请号：US12937718
申请日：2009-04-30
申请人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
发明人： Andrey Alexandrovich Ivashchenko , Volodymyr Mikhailovich Kysil , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
IPC分类号： A61K31/519 , C07D471/14 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/22 , A61P3/04 , C12N5/02
CPC分类号： C07D471/14 , A61K31/519
摘要： The invention relates to serotonin 5-HT6 receptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT6 receptors including cognitive and neurodegenerative diseases.Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is hydrogen, optionally substituted C1-C3 alkyl, C1-C4 alkyloxycarbonyl; R2 is hydrogen, halogen or optionally substituted C1-C3 alkyl; R13 and R23 represent optionally alike: hydrogen, optionally substituted C1-C3 alkyl or R13 and R23 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基 -3-芳基磺酰基-5,6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，药物物质和药物组合物，其包含作为所述化合物的所述药物物质，预防和治疗人类和动物的中枢神经系统的各种疾病，其发病机制与血清素5-HT6受体（包括认知和神经变性疾病）相关。通式1的取代的2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基-3-芳基磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，及其药学上可接受的盐和/或水合物。其中：Ar是任选取代的芳基或任选取代的杂芳基; R 1是氢，任选取代的C 1 -C 3烷基，C 1 -C 4烷氧基羰基; R2是氢，卤素或任选取代的C 1 -C 3烷基; R 13和R 23任选地相似：氢，任选取代的C 1 -C 3烷基或R 13和R 23与它们所连接的氮原子一起形成任选取代的杂环。

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