公开(公告)号：US20190054109A1

公开(公告)日：2019-02-21

申请号：US15745152

申请日：2017-04-07

申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko ,  Alexandre Vasilievich IVACHTCHENKO ,  ALLA CHEM, LLC

发明人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin

IPC分类号： A61K31/7072 ,  A61P31/14 ,  A61K45/06 ,  A61K31/403 ,  A61K31/4709

摘要： The present invention relates to an antiviral composition and a method for application thereof in the treatment of hepatitis C virus.Said antiviral composition comprises the HCV NS5B inhibitor of general formula 1, or a stereoisomer, an isotopically enriched analog, or crystalline or polycrystalline forms thereof.

公开(公告)号：US20140100216A1

公开(公告)日：2014-04-10

申请号：US14118895

申请日：2012-05-12

申请人： Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Denis Yevgenievich Nazarenkov

发明人： Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Denis Yevgenievich Nazarenkov

IPC分类号： C07D267/14 ,  C07D413/14 ,  C07D498/04 ,  C07D413/12 ,  A61K31/553 ,  A61K45/06

CPC分类号： C07D267/14 ,  A61K31/553 ,  A61K45/06 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D498/04

摘要： The invention relates to the area of medicinal chemistry, pharmacology and medicine and includes description of pharmaceutical compositions and combined medicaments on the base of secretion stimulators and protectors of incretin hormones for treatment of metabolic diseases (among them, diabetes, obesity, metabolic syndrome and the like). The invention consists in that that pharmaceutical composition or combined medicament comprises a derivative of tetrahydrobenzo[f][1,4]oxazepine—either nonsteroidal agonist of bile aids receptor TGR5, or one of endogenous bile acids which stimulate incretin hormones secretion, and also one of the known inhibitors of DPP-IV proteinase. In this case administration of TGR5 agonists is carried out peroral, and administration of endogenous bile acids is exercised rectal in the form of suppository or gel. As proteinase DPP-IV inhibitors could be used Vildagliptin, Saxagliptin, Sitagliptin, Teneligliptin, Linagliptin, Dutogliptin, Alogliptin, Gemigliptin, Carmegliptin and the like. Besides, the invention includes description of novel tetrahydrobenzo[f][1,4]oxazepine derivatives—nonsteroidal agonist of bile aids receptors TGR5, and also methods for their preparation. The invention provides enhancement of therapy effectiveness owing to synergetic action of the components, thus making possible simultaneous treatment of diabetes, and obesity, other metabolic diseases and their cardiovascular and renal complications.

摘要翻译： 本发明涉及药物化学，药理学和药物领域，包括在分泌刺激剂的基础上的药物组合物和组合药物的描述，以及用于治疗代谢疾病的肠激素激素的保护剂（其中，糖尿病，肥胖症，代谢综合征和 喜欢）。 本发明包括：药物组合物或组合药物包含四氢苯并[f] [1,4]氧氮杂-胆汁辅助受体TGR5的非甾体激动剂或刺激肠降血糖素激素分泌的内源性胆汁酸之一的衍生物，以及一种 已知的DPP-IV蛋白酶抑制剂。 在这种情况下，通过口服施用TGR5激动剂，并以栓剂或凝胶的形式施用内源性胆汁酸。 由于蛋白酶DPP-IV抑制剂可以使用维格列汀，沙格列汀，西他列汀，替奈米汀，利那格列汀，杜曲列汀，阿格列汀，吉格列汀，卡米利宁等。 此外，本发明还包括描述新型四氢苯并[f] [1,4]恶唑嘌呤衍生物 - 胆汁辅助受体TGR5的非甾体激动剂及其制备方法。 本发明由于组分的协同作用提高了治疗效果，从而使糖尿病和肥胖，其他代谢疾病及其心血管和肾脏并发症成为可能的同时治疗。

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。

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：US20110053915A1

公开(公告)日：2011-03-03

申请号：US12808152

申请日：2008-12-12

申请人： Andrey Alexandrovich Ivaschenko ,  Yan Vadimovich Lavrovsky ,  Sergey Viktorovich Malyarchuk ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Alexander Vasilievich Ivaschenko

发明人： Andrey Alexandrovich Ivaschenko ,  Yan Vadimovich Lavrovsky ,  Sergey Viktorovich Malyarchuk ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Alexander Vasilievich Ivaschenko

IPC分类号： A61K31/55 ,  A61K31/5025 ,  C07D487/04 ,  A61K31/5377 ,  A61K31/542 ,  C07D513/04 ,  A61P35/00 ,  A61K31/437 ,  C07D471/04 ,  A61K31/519 ,  C07D495/04 ,  A61K31/454 ,  A61K31/496 ,  A61K31/438 ,  A61K31/4545 ,  C07D401/04 ,  C07D215/58 ,  A61K31/47 ,  A61K31/4365

CPC分类号： C07D487/04 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2059 ,  A61K9/4858 ,  C07D215/58 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c] N-acidylated 3-azole derivatives.

摘要翻译： 本发明涉及新颖的杂环化合物及其用途，含有所述化合物作为活性成分的药物组合物及其用于生产用于治疗由异常活性引起的疾病的人和温血动物的药物制剂的用途 刺猬（Hh） - 信号系统，特别是肿瘤疾病。 本发明还涉及以“分子药理学工具”形式的上述化合物用于检查（体外和体内）Hh信号系统的生物化学特征的用途，特别是Hh蛋白和 跨膜蛋白，即抑制剂Patched（Ptc）和原癌蛋白。 所要求保护的八个化合物组包括2,6-二氢-7H-吡唑并[3,4-d]哒嗪-7-酮和1,4-二氢吡唑并[3,4-b] [1,4] 噻嗪-5-酮; N-酸化的4-咪唑并[1,2-a]嘧啶-2-基]苯胺; （[4H-噻吩并[3,2-b]吡咯-5-基）羰基]哌啶-4-碳酸酰胺; 2-（4-氰基吡啶-1-基） - 异烟酰胺; N-磺酰基-1,2,3,4-四氢喹啉-6-碳酸酰胺; 和吡啶2-氨基-4,5,6,7-四氢噻吩并[2,3-c] N-酸化的3-唑衍生物。

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

公开(公告)号：US20170000773A1

公开(公告)日：2017-01-05

申请号：US14791280

申请日：2015-07-03

申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich lvashchenko ,  Nikolay Filippovich Savchuk

发明人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich lvashchenko ,  Nikolay Filippovich Savchuk

IPC分类号： A61K31/437 ,  A61K31/444

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

摘要： The present invention relates to a method of antagonizing a 5-HT6 serotonin receptor, comprising administering to the cell a compound of formula 1.2, or a pharmaceutically acceptable salt thereof, wherein: R1 is a C1-C5 alkyl; R2i is independently hydrogen, halogen, a C1-C3 alkyl, CF3, OCF3 or OCH3; i is 1, 2, 3 or 4; Ar is an unsubstituted phenyl or a substituted phenyl substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle with one or two nitrogen atoms in the heterocycle. The invention also relates to pharmaceutical compositions and method for treating a cognitive disorder or neurodegenerative disease in a subject in need thereof comprising administering an effective dose to the subject of a compound of formula 1.2 according to claim 1, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明还涉及用于治疗有需要的受试者的认知障碍或神经变性疾病的药物组合物和方法，其包括向所述受试者施用根据权利要求1的式1.2化合物或其药学上可接受的盐的有效剂量。

公开(公告)号：US20160031859A1

公开(公告)日：2016-02-04

申请号：US14798541

申请日：2014-02-04

申请人： Andrey Alexandrovich IVASHCHENKO ,  Nikolay Filippovich SAVCHUK ,  Alexandre Vasilievich IVACHTCHENKO

发明人： Alexandre Vasilievich Ivachtchenko

IPC分类号： C07D403/14

CPC分类号： C07D403/14 ,  A61K31/4178

摘要： The present invention relates to NS5A inhibitors, to novel pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, in particular caused by hepatitis C (HCV) virus and hepatitis GBV-C virus.Alkyl [(S)-1-((S)-2-{5-[4-(4-{2-[(S)-1-((S)-2-methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-3 H-imidazol-4-yl}-buta-1,3-diynyl)-phenyl]-1H-imidazol-2-yl}-pyrrolidine-1-carbonyl)-2-methyl-propyl]-carbamate naphthaline-1,5-disulfonate of the general formula 1, possibly in crystalline or polycrystalline form, have been proposed, wherein: R is C1-C3 alkyl.

摘要翻译： 本发明涉及NS5A抑制剂，新型药物组合物，抗病毒药物，预防和治疗病毒性疾病的方法，特别是由丙型肝炎（HCV）病毒和乙型肝炎病毒乙型肝炎病毒引起的。 烷基[（S）-1 - （（S）-2- {5- [4-（4- {2 - [（S）-1 - （（S）-2-甲氧基羰基氨基-3-甲基 - 丁酰基） 吡咯烷-2-基] -3H-咪唑-4-基} - 丁-1,3-二炔基） - 苯基] -1H-咪唑-2-基} - 吡咯烷-1-羰基）-2-甲基 - 丙基 已经提出了通式1的萘胺-1,5-二磺酸盐，可能是结晶或多晶形式，其中：R是C 1 -C 3烷基。

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。