公开(公告)号：US20230181704A1

公开(公告)日：2023-06-15

申请号：US17045538

申请日：2020-07-03

申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko ,  Vladimir Grigorievich Loginov ,  Mikhail Topr

发明人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko ,  Vladimir Grigorievich Loginov ,  Mikhail Topr

IPC分类号： A61K38/57 ,  A61K47/02 ,  A61K47/10 ,  A61K47/44 ,  A61P31/14

CPC分类号： A61K38/57 ,  A61K47/02 ,  A61K47/10 ,  A61K47/44 ,  A61P31/14

摘要： This invention relates to a novel anti-SARS-CoV-2 virus agent Antiprovir to be used for the prevention and treatment of coronavirus disease COVID-19.
The use of a pharmaceutical composition, including Aprotex®, Gordox® and Aerus®, with aprotinin as the active ingredient and excipients, said pharmaceutical composition being anti-SARS-CoV-2 virus drug Antiprovir to be used for the prevention and treatment of coronavirus disease COVID-19.
The drug Antiprovir for the prevention and treatment of coronavirus disease COVID-19, which is a pharmaceutical composition containing 0.1% wt. ÷ 0.2% wt. aprotinin, optionally 0.2 %wt. ÷ 1.0% wt. excipients, and the rest is water for injection.

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：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：US20220096421A1

公开(公告)日：2022-03-31

申请号：US17418249

申请日：2020-03-05

申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko

发明人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko

IPC分类号： A61K31/277

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).

公开(公告)号：US20190233409A1

公开(公告)日：2019-08-01

申请号：US15485269

申请日：2017-04-12

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

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

IPC分类号： C07D471/04 ,  A61P3/14

CPC分类号： C07D471/04 ,  A61P3/14

摘要： The present invention relates to compound of the formula 1.2, or a pharmaceutically acceptable salt, or hydrate thereof wherein R1 is C1-C5 alkyl; R2, is independently hydrogen, halogen, C1-C3 alkyl, CF3, OCF3 or OCH3; i is 1, 2,3, or 4; Ar is unsubstituted phenyl or substituted phenyl substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, a substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle one or, with two nitrogen atoms in the heterocycle; excluding the compounds of the formulas A1-A4 The invention relates to the novel chemical compounds, methods for their preparation and use as antagonists of 5-HT6 receptors, simultaneously regulating homeostasis of calcium ions in cells. The invention relates to the novel annelated azaheterocycles—2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles, to methods for their preparation, to pharmaceutical compositions, including these compounds as active substances, and to methods of treatment and profylaxis of various diseases.

公开(公告)号：US20230020329A1

公开(公告)日：2023-01-19

申请号：US17432115

申请日：2020-03-05

申请人： Alexandrovna Alena Ivachtchenko ,  Alexandre Vasilievich Ivachtchenko ,  Nikolay Filippovich Savchuk ,  Andrey Alexandrovich Ivashchenko

发明人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Oleg Dmitrievich Mitkin

IPC分类号： C07D498/14

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 A1 is an optionally methyl-substituted 5-7 membered saturated heterocycle or heterobicycle; ring A2 is a 5-6 membered optionally methyl-substituted saturated or partially saturated monocyclic heterocycle; ring A3 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 (2S,5R,13aS)-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 (1R,4S,12aR)-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).

公开(公告)号：US09655886B2

公开(公告)日：2017-05-23

申请号：US14791280

申请日：2015-07-03

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

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

IPC分类号： A61K31/44 ,  A61K31/437 ,  C07D471/04 ,  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.

公开(公告)号：US10266558B2

公开(公告)日：2019-04-23

申请号：US15287805

申请日：2016-10-07

申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  ASAVI, LLC ,  Alena Alexandrovna Ivachtchenko ,  Oleg Dmitrievich Mitkin

发明人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  Andrey Alexandrovich Ivashchenko ,  Alena Alexandrovna Ivachtchenko ,  Nikolay Filippovich Savchuk

IPC分类号： A61K31/70 ,  A01N43/04 ,  C07H19/10 ,  A61K31/7072 ,  A61K45/06 ,  A61K31/7068 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7064 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7084 ,  A61K31/7052

摘要： Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2′-deoxy-L-uridine (CAS 31501-19-6), 2′-deoxy-D-uridine (CAS 951-78-0), telbivudine (CAS 3424-98-4), zidovudine (AZT, CAS 30516-87-1), trifluridine (CAS 70-00-8), clevudine (CAS 163252-36-6), PSI-6206 (CAS 863329-66-2), 2′-(S)-2′-chloro-2′-deoxy-2′-fluorouridine (CAS 1673560-41-2), ND06954 (CAS 114248-23-6), stavudine (CAS 3056-17-5), 5-ethynyltavudine (Festinavir, CAS 634907-30-5), torcitabine (CAS 40093-94-5), (−)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4(1H,3H)-pyrimidinedione, CAS No. 127658-07-5), 2-(6-amino-purin-9-yl)-ethanol (CAS 707-99-3), 2′-C-methylcytidine (CAS 20724-73-6), PSI-6130 (CAS 817204-33-4), gemcitabine (CAS 95058-81-4), 2′-chloro-2′-deoxy-2′-fluorocytidine (CAS 1786426-19-4), 2′,2′-dichloro-2′-deoxycytidine (CAS 1703785-65-2), 2′-C-methylcytidine (CAS 20724-73-6), PSI-6130 (CAS 817204-33-4), lamivudine (3TC, CAS 134678-17-4), emtricitabine (CAS 143491-57-0), 2′-deoxyadenosine (CAS 958-09-8), 2′-deoxy-β-L-adenosine (CAS 14365-45-8), 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (CAS 865363-93-5), didanosine (CAS 69655-05-6), entecavir (CAS 209216-23-9), FMCA (CAS 1307273-70-6), dioxolane-G (DOG, CAS 145514-01-8), β-D-2′-deoxy-2′-(R)-fluoro-2′-β-C-methylguanosine (CAS No 817204-45-8), abacavir (ABC, CAS 136470-78-5), dioxolane-A (DOA, CAS #145514-02-9), [(2R,4R)-4-(6-cyclopropylamino-purin-9-yl)-[1,3]dioxolan-2-yl]-methanol (CAS 1446751-04-7), amdoxovir (AMDX, CAS 145514-04-1), (R)-1-(6-amino-purin-9-yl)-propan-2-ol (CAS 14047-28-0), and [(2S,5R)-5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yl]-methanol.Macroheterocyclic nucleoside derivative and its analog of the general formula 1 or general formula 2, a stereoisomer, isotope-enriched analog, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: Ar is aryl or hetaryl; R1 and R2 are not necessarily the same substituents selected from H, F, Cl, CH3, OH; R3 is H or CH3; X is oxygen or ethanediyl-1,1 (C═CH2); Y is CH(R4)(CH2)k, CH(R4)(CH2)mC(O)O(CH2)n; R4 is H or CH3; k has a value from zero to six; m has a value from zero to two; n has a value of one to four; Q is a radical selected from Q1-Q4; wherein: R5 is the substituent selected from H, F, Cl, CH3, OH; the arrow (→) indicates the location, joined by Q1-Q4.

公开(公告)号：US20180099989A1

公开(公告)日：2018-04-12

申请号：US15287805

申请日：2016-10-07

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： C07H19/10 ,  A61K45/06 ,  A61K31/7072

CPC分类号： C07H19/10 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K45/06 ,  A61K2300/00

摘要： Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2′-deoxy-L-uridine (CAS No 31501-19-6), 2′-deoxy-D-uridine (CAS No 951-78-0), telbivudine (CAS No 3424-98-4), zidovudine (AZT, CAS No 30516-87-1), trifluridine (CAS No 70-00-8), clevudine (CAS No 163252-36-6), PSI-6206 (CAS No 863329-66-2), 2′-(5)-2′-chloro-2′-deoxy-2′-fluorouridine (CAS No 1673560-41-2), ND06954 (CAS No 114248-23-6), stavudine (CAS No 3056-17-5), 5-ethynyltavudine (Festinavir, CAS No 634907-30-5), torcitabine (CAS No 40093-94-5), (−)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4 (1H,3H)-pyrimidinedione, CAS No. 127658-07-5), 2-(6-amino-purin-9-yl)-ethanol (CAS No 707-99-3), 2′-C-methylcytidine (CAS No 20724-73-6), PSI-6130 (CAS No 817204-33-4), gemcitabine (CAS No 95058-81-4), 2′-chloro-2′-deoxy-2′-fluorocytidine (CAS No 1786426-19-4), 2′,2′-dichloro-2′-deoxycytidine (CAS No 1703785-65-2), 2′-C-methylcytidine (CAS No 20724-73-6), PSI-6130 (CAS No 817204-33-4), lamivudine (3TC, CAS No 134678-17-4), emtricitabine (CAS No 143491-57-0), 2′-deoxyadenosine (CAS No 958-09-8), 2′-deoxy-β-L-adenosine (CAS No 14365-45-8), 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (CAS No 865363-93-5), didanosine (CAS No 69655-05-6), entecavir (CAS No 209216-23-9), FMCA (CAS No 1307273-70-6), dioxolane-G (DOG, CAS No 145514-01-8), β-D-2′-deoxy-2′-(R)-fluoro-2′-β-C-methylguanosine (CAS No 817204-45-8), abacavir (ABC, CAS No 136470-78-5), dioxolane-A (DOA, CAS #145514-02-9), [(2R,4R)-4-(6-cyclopropylamino-purin-9-yl)-[1,3]dioxolan-2-yl]-methanol (CAS No 1446751-04-7), amdoxovir (AMDX, CAS No 145514-04-1), (R)-1-(6-amino-purin-9-yl)-propan-2-ol (CAS No 14047-28-0), and [(2S,5R)-5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yl]-methanol.Macroheterocyclic nucleoside derivative and its analogue of the general formula 1 or general formula 2, a stereoisomer, isotope-enriched analogue, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: Ar is aryl or hetaryl; R1 and R2 are not necessarily the same substituents selected from H, F, Cl, CH3, OH; R3 is H or CH3; X is oxygen or ethanediyl-1,1 (C═CH2); Y is CH(R4)(CH2)k, CH(R4)(CH2)mC(O)O(CH2)n; R4 is H or CH3; k has a value from zero to six; m has a value from zero to two; n has a value of one to four; Q is a radical selected from Q1-Q4; wherein: R5 is the substituent selected from H, F, Cl, CH3, OH; the arrow (→) indicates the location, joined by Q1-Q4.

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。