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1. 发明公开

EP3331354A1 PHOSPHORAMIDATE NUCLEOSIDE PRODRUG FOR TREATING VIRAL DISEASES AND CANCER, PROCESSES FOR THEIR PREPARATION AND THEIR USE 审中-公开
公开(公告)号：EP3331354A1
公开(公告)日：2018-06-13
申请号：EP17834922.1
申请日：2017-06-21
申请人： Asavi, LLC , Ivashchenko, Andrey Alexandrovich , Savchuk, Nikolay Filippovich , Mitkin, Oleg Dmitrievich , Ivachtchenko, Alexandre Vasilievich , Ivachtchenko, Alena Alexandrovna
发明人： IVACHTCHENKO, Alexandre Vasilievich , IVASHCHENKO, Andrey Alexandrovich , SAVCHUK, Nikolay Filippovich , MITKIN, Oleg Dmitrievich , IVACHTCHENKO, Alena Alexandrovna
IPC分类号： A01K43/04 , A61K31/70
CPC分类号： C07H19/16 , C07F9/65586 , C07F9/65616 , C07H19/06
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, formula (1) wherein: Ar is aryl or hetaryl; R1 is H or CH3, R2 is the substituent selected from OCH2CH=CH2, OCH2CH≡CH, OCH2CH2CH2OCH3, formula (2), formula (3) or formula (4), 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 formula (5) or (6); 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; R10.1 R10.2 R10.4 R10.5 ; R11 is the substituent selected from H, F, CI, 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 (formula 7) together are the single carbon-carbon (C-C) bond or Y is CH group provided when continuous line and its accompanying dotted line (formula 7) 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; R2 is isopropyl; Nuc is formula (8), (9) or (10).

2. 发明公开

EP3650015A1 COMBINED MEDICINAL PREPARATION FOR TREATING VIRAL INFECTIONS 无效
公开(公告)号：EP3650015A1
公开(公告)日：2020-05-13
申请号：EP18828227.1
申请日：2018-02-14
申请人： Ivachtchenko, Alexandre Vasilievich , Ivashchenko, Andrey Alexandrovich , Savchuk, Nikolay Filippovich , Alla Chem, LLC , Ivachtchenko, Alena Alexandrovna
发明人： IVACHTCHENKO, Alexandre Vasilievich , IVASHCHENKO, Andrey Alexandrovich , SAVCHUK, Nikolay Filippovich
IPC分类号： A61K9/20 , A61K9/48 , A61K9/14 , A61K9/68 , A61P31/18 , A61P31/12 , A61P31/20 , C07D411/04 , C07C311/46 , C07F9/6553 , C07F9/6568 , C07F9/6561
摘要： The present invention relates to a novel combination drug in a solid oral dosage form comprising, as one of the three active ingredients, elsulfavirine sodium that may be suitable for medical use when treating viral infections including HIV and HBV.
An antiviral combination drug in a solid oral dosage form comprising, as one of the three active ingredients, a therapeutically effective amount of elsulfavirine sodium of formula 1a in a crystalline or polycrystalline form optionally in combination with auxiliary agents:

3. 发明公开

EP3988539A1 ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, AND MEDICINAL PREPARATION FOR THERAPY OF HIV AND AIDS 审中-实审
公开(公告)号：EP3988539A1
公开(公告)日：2022-04-27
申请号：EP20798528.4
申请日：2020-03-05
申请人： Alla Chem, LLC , Savchuk, Nikolay Filippovich , Ivashchenko, Andrey Alexandrovich , Ivachtchenko, Alena Alexandrovna , Ivachtchenko, Alexandre Vasilievich
发明人： IVACHTCHENKO, Alexandre Vasilievich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Andrey Alexandrovich , IVACHTCHENKO, Alena Alexandrovna
IPC分类号： C07C311/51 , A61K31/18 , A61K9/14 , A61K47/26 , A61K47/38 , A61K47/06 , A61P31/18
摘要： This invention relates to the active ingredient of a pharmaceutical composition consisting of micronized monoclinic symmetry crystals (MMSCs) of sodium {[4-({[4-bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl] acetyl }amino)-3-chlorophenyl] - sulfonyl}(propanoyl)azanide with an average particle diameter ≤130 µm and methods of use thereof in the treatment of Human Immunodeficiency Virus (HIV) and Acquired Immune Deficiency Syndrome (AIDS).

4. 发明公开

EP3978503A1 ANNELATED 9-HYDROXY-1,8-DIOXO-1,3,4,8-TETRAHYDRO-2H-PYRIDO[1,2-a]PYRAZINE-7-CARBOXAMIDES AS HIV INTEGRASE INHIBITORS 无效
公开(公告)号：EP3978503A1
公开(公告)日：2022-04-06
申请号：EP20818731.0
申请日：2020-03-05
申请人： Ivachtchenko, Alena Alexandrovna , Alla Chem, LLC , Ivachtchenko, Alexandre Vasilievich , Savchuk, Nikolay Filippovich , Ivashchenko, Andrey Alexandrovich
发明人： MITKIN, Oleg Dmitrievich , IVACHTCHENKO, Alexandre Vasilievich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Andrey Alexandrovich
IPC分类号： C07D498/14 , C07D498/18 , A61K31/5365 , A61K31/537 , A61K31/553 , A61K31/4985 , A61P31/18
摘要： The present invention relates to a novel compound that has antiviral activity, in particular, inhibitory activity against the integrase of the human immunodeficiency virus (HIV).
The subject of this invention is a novel annelated 9-hydroxy-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxamide of general formula 1 or 2, or any stereoisomer, any pharmaceutically acceptable salt, any solvate, or any crystalline or polycrystalline form thereof

wherein
ring A 1 is an optionally methyl-substituted 5-7 membered saturated heterocycle or heterobicycle;
ring A 2 is a 5-6 membered optionally methyl-substituted saturated or partially saturated monocyclic heterocycle;
ring A 3 is a 5-6 membered monocyclic saturated cycloalkane or tetrahydro-2H-pyran;
R is a 5-7 membered optionally substituted with one, two, or three optionally identical substituents monocyclic or bicyclic heterocyclic radical comprising 1-4 heteroatoms selected from the series O, S, and N except (2 S ,5 R ,13a S )-8-hydroxy-7,9-dioxo- N -{[3-(trifluoromethyl)-pyridin-2-yl]methyl}-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopurido[1',2':4,5]pyrazino[2,1- b ][1,3]oxazepine-10-carboxamide (formula A4) and (1 R ,4 S ,12a R )- N -[(3,5-difluoropyridin-2-yl)methyl]-7-hydroxy-6,8-dioxo-1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2- a :1',2'- d ]pyrazine-9-carboxamide (formula A5).

5. 发明授权

EP2287163B1 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：血清素5-HT6受体的2-氨基-3-磺酰基 - 四氢 - 吡唑并[1,5-A]吡啶 - 嘧啶拮抗剂，其生产方法和用途
公开(公告)号：EP2287163B1
公开(公告)日：2014-08-06
申请号：EP09742910.4
申请日：2009-04-30
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich , IVASHCHENKO, Andrey Alexandrovich
IPC分类号： C07D471/14 , A61P25/22 , A61K31/519 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/08 , A61P3/08 , A61P25/26 , A61P9/10 , A61P25/16 , A61P3/04
CPC分类号： C07D471/14 , A61K31/519

6. 发明公开

EP2327703A1 LIGAND WITH A BROAD SPECTRUM OF PHARMACOLOGICAL ACTIVITY, A PHARMACEUTICAL COMPOSITION, A MEDICINAL AGENT AND A METHOD OF TREATMENT 审中-公开
标题翻译：具有广泛的活动范围药理，药物组合物，药物和治疗方法的配体
公开(公告)号：EP2327703A1
公开(公告)日：2011-06-01
申请号：EP09810284.1
申请日：2009-08-03
申请人： IVASHCHENKO, Andrey Alexandrovich , Alla Chem, LLC.
发明人： IVASHCHENKO, Alexander Vasilievich , SAVCHUK, Nikolay Filippovich
IPC分类号： C07D471/02 , A61K31/437 , A61P25/28
CPC分类号： A61K31/437 , C07D471/04
摘要： The present invention is directed to the novel ligand with wide range of pharmacological activity including activity to GPCR receptors, ion channels and monoamine transporters representing 3-methyl-9-benzyl-1,2,3,4-tetrahydrocarboline naphthalene-1,5-disulfonate of formula 1

The invention is also directed to the novel drug substance, Pharmaceutical formulation comprising the novel drug substance, and to the method for its preparation, to the novel medicaments, and method for treatment of CNS diseases including neurodegenerative diseases and cognitive disorders at humans and warm blooded animals.
摘要翻译：本发明是针对新颖的配体与广泛的药理学活性，包括活性GPCR受体，离子通道和单胺转运蛋白代表3-甲基9-苄基-1,2,3,4-四氢萘-1,5-二咔啉因此式1的本发明的二磺酸被引导到新的药物物质，药物制剂，包括新颖的药物物质，和其制备的方法中，对新颖的药物，以及用于治疗CNS疾病的方法，包括神经变性疾病和在认知障碍人和温血动物。

7. 发明公开

EP2036889A2 SUBSTITUTED INDOLES AND A METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：维多利亚独立电力公司
公开(公告)号：EP2036889A2
公开(公告)日：2009-03-18
申请号：EP07747937.6
申请日：2007-05-17
申请人： Alla Chem, LLC. , Ivashchenko, Andrey, Alexandrovich
发明人： IVASCHENKO, Andrey Alexandrovich , TKACHENKO, Sergey Yevgenievich , KHVAT, Alexander Viktorovich , MITKIN, Oleg Dmitrievich , OKUN, Ilya Matusovich , KYSELVEV, Alexandr Sergeevich , KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich
IPC分类号： C07D209/42 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/14 , C07D498/04 , A61K31/405 , A61K31/407 , A61K31/416 , A61K31/4439 , A61K31/4465 , A61K31/454 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/55
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 compositions for the manufacture of 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 (I) or racemates, optical isomers, pharmaceutically acceptable salts and/or hydrates thereof, wherein R 1 , R 1 4 and R 2 4 independently are an aminogroup substituent selected from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, or R 1 4 and R 2 4 together with the nitrogen atom to which they are attached, form via R 1 4 and R 2 4 an optionally substituted azaheterocyclyl or guanidyl; R 2 is an alkyl substituent selected from hydrogen, an optionally substituted mercaptogroup, optionally substituted aminogroup and optionally substituted hydroxyl; R 3 is lower alkyl, R 5 is an hydrogen atom or R 5 together with the oxygen atom to which it is attached and R 2 4 together with the nitrogen atom to which it is attached close, via R 5 and R 2 4 an oxazine ring; R 6 is a cyclic system substituent selected from hydrogen, 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），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（I）的新型取代的吲哚或其外消旋物，旋光异构体，药学上可接受的盐和/或水合物，其中R 1，R 14和R 24独立地是选自氢，任选取代的烷基，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经由R 14和R 24经任意取代的杂环基或胍基形成; R 2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为低级烷基，R 5为氢原子或R 5与连接的氧原子一起形成，R 2与其所连接的氮原子一起通过R 5和R 24接近恶嗪环; R 6是选自氢，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。

8. 发明公开

EP2248814A2 SUBSTITUTED CYCLOALCANO[e AND d] PYRAZOLO [1,5-a] PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND METHODS FOR PRODUCTION AND THE USE THEREOF 审中-公开
标题翻译：替代环己烷酮[E UND D]吡唑并[1,5-A]吡咯烷酮ALS ANTAGONISTEN VON SEROTONIN-5-HT6-REZEPTOREN
公开(公告)号：EP2248814A2
公开(公告)日：2010-11-10
申请号：EP09703618.0
申请日：2009-01-23
申请人： Alla Chem, LLC. , Ivashchenko, Andrey Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , IVASHCHENKO, Alexander Vasilievich , SAVCHUK, Nikolay Filippovich
IPC分类号： C07D487/04 , A61P25/26 , A61P25/18 , A61P9/10 , A61P25/08 , A61P25/28 , A61P3/08 , A61P25/16 , A61K31/519 , A61P3/04
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-HT 6 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-HT 6 receptors.
In general formulas 1 and 2

R 1 represents hydrogen or C 1 -C 3 alkyl; R 2 represents C 1 -C 3 alkyl; R 3 represents hydrogen, one or more optionally identical halogens, C 1 -C 3 alkyl or hydroxyl optionally substituted with C 1 -C 3 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，称为活性成分，用于治疗和预防人类CNS疾病的新型药物和方法以及与5-HT 6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; R 2表示C 1 -C 3烷基; R 3表示氢，一个或多个任选相同的卤素，C 1 -C 3烷基或任选被C 1 -C 3烷基取代的羟基; n表示整数1,2或3。

9. 发明公开

EP2236511A2 LIGANDS OF ALPHA-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF 审中-公开
标题翻译： ALPHA-肾上腺素和多巴胺，组胺，咪唑啉和血清素受体及其使用配体
公开(公告)号：EP2236511A2
公开(公告)日：2010-10-06
申请号：EP08864305.1
申请日：2008-12-19
申请人： Alla Chem, LLC. , Ivashchenko, Andrey Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , IVASHCHENKO, Alexander Vasilievich , LAVROVSKY, Yan Vadimovich , MITKIN, Oleg Dmitrievich , SAVCHUK, Nikolay Filippovich , TKACHENKO, Sergey Yevgenievich , OKUN, Ilya Matusovich
IPC分类号： C07D471/04 , C07D487/04 , A61K31/43 , A61K31/519 , A61P25/00
CPC分类号： C07D471/04 , 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-HT 7 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 C 1 -C 4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C 1 -C 4 alkyl, CF 3 , 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 (CH 2 ) m group, optionally substituted CH=CH group, optionally substituted CH 2 -CH=CH group, C≡C group, SO 2 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：本发明涉及新的配体的生物学活性的广谱都包括同时±肾上腺素能受体，多巴胺受体，组胺受体，咪唑啉受体和血清素受体，其中血清素5-HT 7种受体，它们是在通式1的化合物的游离碱，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，形式worin：R 1是氨基，选自氢，任选取代的C 1 -C 4烷基，酰基，杂环基的取代基，烷氧基羰基，取代的磺酰基; R2是环体系，选自氢，卤素，任选取代的C 1个-C 4烷基，CF 3中选择的取代基，CN，烷氧基，烷氧基羰基，羧基，杂环基或取代的磺酰基; Ar是芳基OPTIONALLY substituiertem不一定安娜迟来与杂环基，或任选取代的芳族杂环基; W是任选substituiertem（CH 2）M基，任选substituiertem CH = CH基团，任选substituiertem CH 2 -CH = CH基团，C‰¡C组，SO 2基团; n = 1时，2; M = 1，2，3; solidLine陪同下虚线，即（---）可以代表单键或双键。因此，本发明涉及活性成分，药物组合物包含所述的配位体作为活性成分; 用于治疗的疾病和人类和温血动物的中枢神经系统（CNS）的条件下有用的新的药物。

10. 发明公开

EP2184064A2 LIGANDS OF 5-HT6 RECEPTORS, A PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：配体的5-HT 6受体，药物组合物，方法和用途
公开(公告)号：EP2184064A2
公开(公告)日：2010-05-12
申请号：EP07861047.4
申请日：2007-11-15
申请人： Alla Chem, LLC. , IVASHCHENKO, Andrey Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , IVASHCHENKO, Alexandr Vasilievich , TKACHENKO, Sergey Yevgenievich , OKUN, Ilya Matusovich , SAVCHUK, Nikolay Filippovich
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4748 , A61K31/497 , A61K31/4985 , A61K31/52 , A61K31/522 , A61K31/529 , A61K31/5513 , A61K31/55 , C07D209/14 , C07D209/18 , C07C209/22
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The invention relates to novel ligands of 5-HT 6 receptor, to a pharmaceutical composition containing said novel ligands of 5-HT 6 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-HT 6 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-HT 6 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; C 1 -C 5 -alkyl optionally substituted by: C 6 -C 10 -arylaminocarbonyl, heterocyclyl, C 6 -C 10 -arylaminocarbonyl, C 6 -C 10 -arylaminothiocarbonyl, C 5 -C 10 -azaheteroaryl, optionally substituted carboxyl, nitryl group, optionally substituted aryl; R 1 k represents from 1 to 3 substituents of cyclic system, independent of each other and selected from hydrogen, optionally substituted C 1 -C 5 -alkyl, C 1 -C 5 -alkoxy, C 1 -C 5 -alkenyl, C 1 -C 5 -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5-HT 6受体的新配体，含有5-HT 6受体作为活性组分并用于人和温血动物用于治疗疾病和中枢神经的条件新颖药物的所述新的配体的药物组合物系统由5-HT引起的神经其中调解制度的发病6个受体打出了至关重要的作用。通式1或种族匹配，或光学或几何异构体，或药学上可接受的盐和/或水合物的氮杂杂环化合物及其作为5-HT 6个配体。其中海誓山盟的R2和R3表示unabhängig在选自氢氨基取代基; 取代羰基; 取代羰基; 取代氨基硫; 取代磺酰基; C 1 -C 5烷基任选被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 -arylaminothiocarbonyl，C 5 -C 10 -azaheteroaryl，任选取代的羧基，硝基基，任选取代的芳基; 的R 1为1〜3个取代基的环状体系，相互独立的k个darstellt并选自氢，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; 由虚线（---）的陪同下，实线代表单键或双键; N = 1,2或第三

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