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。

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：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：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。

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：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。

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。

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。

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。