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1. 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。

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。

4. 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。

5. 发明授权

US08629154B2 Substituted cycloalcano[e and d] pyrazolo [1,5-a]pyrimidines/antagonists of serotonin 5-HT6 receptors and methods for production and the use thereof 失效
标题翻译： 5-羟色胺5-HT 6受体的取代的环硫烷并[e和d]吡唑并[1,5-a]嘧啶/拮抗剂及其制备方法及用途
公开(公告)号：US08629154B2
公开(公告)日：2014-01-14
申请号：US12863192
申请日：2009-01-23
申请人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Nikolay Filippovich Savchuk
发明人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Nikolay Filippovich Savchuk
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D487/00
CPC分类号： C07D487/04
摘要： The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors.In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂的取代的2-烷基硫基-3-（芳基磺酰基） - 环烷基[e和d]吡唑并[1,5-a]嘧啶，用于新药物和药物组合物，作为活性成分，用于治疗和预防人类CNS疾病的新型药物和方法，以及与5-HT6受体有关的温血动物的发病机制。在通式1和2中，R 1表示氢或C 1 -C 3烷基; R2代表C1-C3烷基; R 3表示氢，一个或多个任选相同的卤素，任选被C 1 -C 3烷基取代的C 1 -C 3烷基或羟基; n表示整数1,2或3。

6. 发明授权

US08552005B2 (EN) 3-sulfonyl-pyrazolo[1,5-a] pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof 有权
标题翻译：（EN）3-磺酰基 - 吡唑并[1,5-a]嘧啶/ 5-羟色胺5-HT 6受体的拮抗剂，生产方法及其用途
公开(公告)号：US08552005B2
公开(公告)日：2013-10-08
申请号：US12812728
申请日：2009-01-23
申请人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Nikolay Filippovich Savchuk
发明人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Nikolay Filippovich Savchuk
IPC分类号： A01N43/90 , A01N43/00 , A61K31/519 , A61K31/33 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel substituted 3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HT6 receptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HT6 receptor activation.In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R1, R2 and R3 independently of each other represent hydrogen, C1-C3 alkyl or phenyl; R4 represents hydrogen, optionally substituted C1-C5 alkyl, substituted hydroxyl group or substituted sulfanyl group.
摘要翻译：本发明涉及通式1的药学上可接受的盐和/或水合物的新的取代的3-（芳基磺酰基）吡唑并[1,5-a]嘧啶新颖的5-羟色胺5-HT 6受体拮抗剂，新药物，药物组合物，药物及其制备方法，用于治疗和预防CNS的病理状态和疾病，其发病机制与血清素5-HT6受体激活的干扰有关。在通式1的化合物中Ar表示任选取代的芳基或杂环基; R 1，R 2和R 3彼此独立地表示氢，C 1 -C 3烷基或苯基; R 4表示氢，任选取代的C 1 -C 5烷基，取代的羟基或取代的硫烷基。

7. 发明授权

US08481587B2 Substituted 2-(5-hydroxy-2-methyl-1H-indole-3-yl)acetic acids and ethers thereof and the use of same to treat viral diseases 失效
标题翻译：取代的2-（5-羟基-2-甲基-1H-吲哚-3-基）乙酸及其醚及其用途来治疗病毒性疾病
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。

8. 发明授权

US08471009B2 (EN) 2-alkylamino-3-arylsulfonyl-cycloalcano [e OR d] pyrazolo [1,5-A]pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof 有权
标题翻译：（EN）2-烷基氨基-3-芳基磺酰基 - 环硫烷基[e OR d]吡唑并[1,5-A]嘧啶/ 5-羟色胺5-HT 6受体的拮抗剂，其制备方法及用途
公开(公告)号：US08471009B2
公开(公告)日：2013-06-25
申请号：US12812734
申请日：2009-01-23
申请人： Andrey Alexandrovich Ivashchenko , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
发明人： Andrey Alexandrovich Ivashchenko , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases.2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: R1 is hydrogen or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is hydrogen, one or more optionally identical halogen atoms, C1-C3 alkyl or hydroxyl group optionally substituted with C1-C3 alkyl; n is the whole numbers 1, 2 or 3.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂的取代的2-烷基氨基-3-（芳基磺酰基）环烷基[e或d]吡唑并[1,5-a]嘧啶，用于新药物和包含所述化合物的药物组合物活性成分，以及用于治疗和预防各种CNS疾病的新药物和方法。通式1的2-烷基氨基-3-芳基磺酰基环烷基[e]吡唑并[1,5-a]嘧啶和2-烷基氨基-3-芳基磺酰基环烷基[d]吡唑并[1,5-a]嘧啶，其中： R1是氢或C1-C3烷基; R2是C1-C3烷基; R 3是氢，一个或多个任选相同的卤原子，任选被C 1 -C 3烷基取代的C 1 -C 3烷基或羟基; n是整数1,2或3。

9. 发明申请

US20110059997A1 SUBSTITUTED CYCLOALCANO[e AND d] PYRAZOLO [1,5-a]PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND METHODS FOR PRODUCTION AND THE USE THEREOF 失效
标题翻译：取代的环己烷基[e和d]吡唑并[1,5-a]嘧啶/硒酸5-HT6受体的拮抗剂及其生产方法及其用途
公开(公告)号：US20110059997A1
公开(公告)日：2011-03-10
申请号：US12863192
申请日：2009-01-23
申请人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Nikolay Filippovich Savchuk
发明人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Nikolay Filippovich Savchuk
IPC分类号： A61K31/519 , C07D471/04 , A61P3/04 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/14 , B65D85/00
CPC分类号： C07D487/04
摘要： The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors.In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.
摘要翻译：本发明涉及5-羟色胺5-HT 6受体拮抗剂的取代的2-烷基硫烷基-3-（芳基磺酰基） - 环烷基[e和d]吡唑并[1,5-a]嘧啶，用于新药物和药物组合物，作为活性成分，用于治疗和预防人类CNS疾病的新型药物和方法，以及与5-HT6受体有关的温血动物的发病机制。在通式1和2中，R 1表示氢或C 1 -C 3烷基; R2代表C1-C3烷基; R 3表示氢，一个或多个任选相同的卤素，任选被C 1 -C 3烷基取代的C 1 -C 3烷基或羟基; n表示整数1,2或3。

10. 发明申请

US20110046368A1 LIGANDS OF 5-HT6 RECEPTORS, A PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译： 5-HT6受体的配体，药物组合物，其生产和使用方法
公开(公告)号：US20110046368A1
公开(公告)日：2011-02-24
申请号：US12741006
申请日：2007-11-15
申请人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Sergey Yevgenievich Tkachenko , Ilya Matusovich Okun , Nikolay Filippovich Savchuk
发明人： Andrey Alexandrovich Ivashchenko , Alexander Vasilievich Ivashchenko , Sergey Yevgenievich Tkachenko , Ilya Matusovich Okun , Nikolay Filippovich Savchuk
IPC分类号： C07D487/04 , C07D471/04 , C07D473/04
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The invention relates to novel ligands of 5-HT6 receptor, to a pharmaceutical composition containing said novel ligands of 5-HT6 receptor as active component and to novel medicaments used for humans and warm-blooded animals for treating diseases and conditions of central nervous system, in pathogenesis of which neuromediator systems induced by 5-HT6 receptors are playing an essential role.Azaheterocyclic compounds of the general formula 1 or racemates, or optical or geometrical isomers, or pharmaceutically acceptable salts and/or hydrates thereof are used as 5-HT6 ligands. Wherein R2 and R3 independently of each other represent an amino group substituent selected from hydrogen; substituted carbonyl; substituted aminocarbonyl; substituted aminothiocarbonyl; substituted sulphonyl; C1-C5-alkyl optionally substituted by: C6-C10-arylaminocarbonyl, heterocyclyl, C6-C10-arylaminocarbonyl, C6-C10-arylaminothiocarbonyl, C5-C10-azaheteroaryl, optionally substituted carboxyl, nitryl group, optionally substituted aryl; R1k represents from 1 to 3 substituents of cyclic system, independent of each other and selected from hydrogen, optionally substituted C1-C5-alkyl, C1-C5-alkoxy, C1-C5-alkenyl, C1-C5-alkynyl, halogen, trifluoromethyl, CN-group, carboxyl, optionally substituted aryl, optionally substituted heterocyclyl, substituted sulfonyl, optionally substituted carboxyl; the solid line accompanied by the dotted line represents a single or a double bond; n=1, 2 or 3.
摘要翻译：本发明涉及含有5-HT 6受体作为活性成分的所述新型配体的药物组合物和用于人和用于治疗中枢神经系统疾病和病症的温血动物的新型药物的5-HT 6受体的新配体，在5-HT6受体诱导的神经调节因子的发病机理中起着重要的作用。通式1的氮杂环化合物或其外消旋体或光学或几何异构体或其药学上可接受的盐和/或水合物用作5-HT 6配体。其中R2和R3彼此独立地表示选自氢的氨基取代基; 取代羰基; 取代的氨基羰基; 取代的氨基硫代羰基; 取代磺酰基; 任选被C 6 -C 10芳基氨基羰基，杂环基，C 6 -C 10 - 芳基氨基羰基，C 6 -C 10 - 芳基氨基硫代羰基，C 5 -C 10 - 氮杂杂芳基，任选取代的羧基，硝基，任选取代的芳基取代的C 1 -C 5 - 任选取代的C 1 -C 5 - 烷基，C 1 -C 5 - 烷氧基，C 1 -C 5 - 烯基，C 1 -C 5 - 炔基，卤素，三氟甲基， CN-基团，羧基，任选取代的芳基，任选取代的杂环基，取代的磺酰基，任选取代的羧基; 伴随虚线的实线表示单键或双键; n = 1,2或3。

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