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1. 发明申请

WO2012087182A3 SUBSTITUTED METHYL AMINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS, METHODS FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代的甲基氨基磺酸盐，丝氨酸5-HT6受体拮抗剂，其生产和使用方法
公开(公告)号：WO2012087182A3
公开(公告)日：2012-09-13
申请号：PCT/RU2011000981
申请日：2011-12-13
申请人： IVACHTCHENKO ALEXANDRE VASILIEVICH , ALLA CHEM LLC , MITKIN OLEG DMITRIEVICH , KADIEVA MADINA GEORGIEVNA
发明人： IVACHTCHENKO ALEXANDRE VASILIEVICH , MITKIN OLEG DMITRIEVICH , KADIEVA MADINA GEORGIEVNA
IPC分类号： C07C317/36 , A61K31/13 , A61K31/341 , A61K31/381 , A61K31/421 , A61K31/422 , A61K31/437 , A61K31/44 , A61K31/4706 , A61K31/4709 , A61K31/495 , A61K31/496 , A61P3/06 , A61P9/10 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/28 , C07D211/84 , C07D213/34 , C07D213/38 , C07D215/38 , C07D215/42 , C07D263/48 , C07D295/096 , C07D307/64 , C07D307/66 , C07D317/32 , C07D333/34 , C07D333/36 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , C07C317/36 , C07D213/40 , C07D215/42 , C07D295/135 , C07D413/04 , C07D413/14
摘要： The invention relates to novel substituted methyl amines, serotonin 5-HT6 receptor antagonists, active ingredients, pharmaceutical compositions and a method for preventing and treating diseases of the central nervous system, as well as to molecular instruments, wherein the novel substituted methyl amines are compounds of general formula 1 and crystalline forms, polycrystalline forms, pharmaceutically acceptable salts and/or hydrates thereof, where: W is naphthalene, indolizine or quinoline; R1 is hydrogen, fluorine, chlorine, methyl; R2 is hydrogen, fluorine, methyl, phenyl, thiophen-2-yl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 is methyl; or W is benzene, R3 has the above meaning; R1 is 3-C 1, R2 is ?-piperazin-1-yl or 3-(4-methylpiperazin-1-yl); or R1 is hydrogen, R2 is phenyl or pyridyl; or R1 is hydrogen, fluorine, chlorine, methyl; R2 is 4-piperazin-1-yl or 4-(4-methylpiperazin-1-yl); or W is oxazole, R3 is optionally substituted methyl; R1 is chlorine or fluorine, R2 is methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is piperazin-1-yl, 4-methylpiperazin-1-yl, or R1 is chlorine, fluorine or methyl; R2 is furan-2-yl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is furan-2-yl, R3 is (tetrahydrofuran-2-yl)methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is thiophen-2-yl, R3 is 2-methoxyethyl, or R1 is chlorine or fluorine, R2 is thiophen-2-yl, R3 is methyl.
摘要翻译：本发明涉及新型取代的甲胺，5-羟色胺5-HT 6受体拮抗剂，活性成分，药物组合物和预防和治疗中枢神经系统疾病的方法，以及分子仪器，其中新取代的甲胺是化合物通式1和结晶形式，多晶形式，其药学上可接受的盐和/或水合物，其中：W是萘，中氮茚或喹啉; R1是氢，氟，氯，甲基; R 2是氢，氟，甲基，苯基，噻吩-2-基，呋喃-2-基，吡啶基，哌嗪-1-基或4-甲基哌嗪-1-基; R3是甲基; 或W为苯，R3具有上述含义; R1是3-C 1，R2是α-哌嗪-1-基或3-（4-甲基哌嗪-1-基）; 或R 1为氢，R 2为苯基或吡啶基; 或R 1为氢，氟，氯，甲基; R2是4-哌嗪-1-基或4-（4-甲基哌嗪-1-基）; 或W为恶唑，R3为任选取代的甲基; R1是氯或氟，R2是甲基，或R1是氢，氟，氯，甲基; R2是哌嗪-1-基，4-甲基哌嗪-1-基，或R1是氯，氟或甲基; R2是呋喃-2-基，或R1是氢，氟，氯，甲基; R2是呋喃-2-基，R3是（四氢呋喃-2-基）甲基，或R1是氢，氟，氯，甲基; R2是噻吩-2-基，R3是2-甲氧基乙基，或R1是氯或氟，R2是噻吩-2-基，R3是甲基。

2. 发明申请

WO2012091628A3 SUBSTITUTED HYDROGENATED THIENO-PYRROLO[3,2-C]PYRIDINE, LIGANDS, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR USING THE ABOVE 审中-公开
标题翻译：取代的氢化噻吩并吡咯[3,2-C]吡啶，配体，药物组合物和使用上述方法
公开(公告)号：WO2012091628A3
公开(公告)日：2012-09-13
申请号：PCT/RU2011000980
申请日：2011-12-13
申请人： IVACHTCHENKO ALEXANDRE VASILIEVICH , ALLA CHEM LLC , MITKIN OLEG DMITRIEVICH
发明人： IVACHTCHENKO ALEXANDRE VASILIEVICH , MITKIN OLEG DMITRIEVICH
IPC分类号： C07D495/14 , A61K31/4365 , A61K31/439 , A61K31/46 , A61P25/24 , A61P25/28 , C07D451/02 , C07D495/22
CPC分类号： C07D495/14 , C07D471/04 , C07D495/22
摘要： The invention relates to novel substituted tetrahydro-4H-thieno-pyrrolo[3,2-c]pyridines of general formula 1, geometric isomers thereof, mixtures of the geometric isomers thereof, and pharmaceutically acceptable salts thereof, where Th is an annulated thiene ring; W is a single bond (in this case R3 is bonded directly to the nitrogen atom of the pyrrole ring), a methylene, 1,2-ethane, 1,2-ethylene, 1,2-acetylene, 1,3-propane or 1,3-allyl bridge optionally substituted by a hydroxyl group; R1 and R2 are hydrogen, C1-C4alkyl, halogen or -??2??; R3 is hydrogen, optionally substituted phenyl, optionally substituted azaheteroaryl; R4 is C1-C4alkyl, ??2?2?5 or ??2?(??3)3; R5, R6, R7, independently of one another, are hydrogen or C1-C4alkyl, or R5 and R6 together form an ethylene bridge and R7 is a hydrogen atom, or R5 and R7 together form an ethylene bridge and R6 is a hydrogen atom; and also to the synthesis of novel chemical substances, novel physiologically active substances, "molecular instruments", a pharmaceutical composition, methods for producing same and a method for treating and preventing the development of various diseases, including diseases of the central nervous system.
摘要翻译：本发明涉及通式1的新的取代的四氢-4H-噻吩并 - 吡咯并[3,2-c]吡啶，其几何异构体，其几何异构体的混合物及其药学上可接受的盐，其中Th是稠合的噻吩环 ; W是单键（在这种情况下R3直接键合到吡咯环的氮原子上），亚甲基，1,2-乙烷，1,2-亚乙基，1,2-乙炔，1,3-丙烷或任选被羟基取代的1,3-烯丙基桥; R 1和R 2是氢，C 1 -C 4烷基，卤素或-α2δ; R3是氢，任选取代的苯基，任选取代的氮杂杂芳基; R4是C1-C4烷基，α2→2α5或β2β（αβ3）3; R5，R6，R7彼此独立地为氢或C1-C4烷基，或R5和R6一起形成亚乙基桥，并且R7为氢原子，或R5和R7一起形成亚乙基桥，R6为氢原子; 并且还涉及新化学物质，新型生理活性物质，“分子仪器”的合成，药物组合物，其制备方法以及治疗和预防包括中枢神经系统疾病在内的各种疾病发展的方法。

3. 发明申请

WO2012074437A3 SUBSTITUTED AZOLES, ANTI-VIRAL ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代的偶氮唑，抗病毒活性成分，药物组合物，其生产方法和用途
公开(公告)号：WO2012074437A3
公开(公告)日：2012-09-13
申请号：PCT/RU2011000932
申请日：2011-11-28
申请人： IVACHTCHENKO ALEXANDRE VASILIEVICH , ALLA CHEM LLC , BICHKO VADIM VASILIEVICH , MITKIN OLEG DMITRIEVICH
发明人： IVACHTCHENKO ALEXANDRE VASILIEVICH , BICHKO VADIM VASILIEVICH , MITKIN OLEG DMITRIEVICH
IPC分类号： C07D403/04 , A61K31/12 , A61K31/4178 , A61K31/422 , A61K31/427 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/14
CPC分类号： C07D403/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel azoles, novel anti-viral active ingredients of general formula 1A and 1B, a pharmaceutical composition, an anti-viral drug and a method for preventing and treating viral diseases, particularly those caused by hepatitis C viruses (HCV). In the general formula 1A and 1B, in which the continuous lines accompanied by dotted lines (---) represent a single or double bond, X and Y assume different meanings, one being nitrogen and the other being oxygen, sulphur or an NH group; R1 and R2 are optionally identical radicals selected from 2-(R) and (S)-substituted N-acyl pyrrolidine derivatives; N-MeTmi-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl [2-(R) and (S)-substituted (((methyl)amino)-(1-oxo-butan-2-yl)-2-(11)-] and (?)-isopropyl)-carbamates. ? stands for an aliphatic ?2-?8 biradical; dioxane, cycloaliphatic, bicycloaliphatic, alkyloxyalkyl, alkyloxyalkyleneoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl biradicals and thia analogues thereof; aryl and thiophenyl, alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, alkyloxyaryl, alkenyloxyaryl, alkynyloxyaryl, alkylthiaaryl, alkenylthiaaryl, alkynylthiaaryl, cycloalkylthiophene, aryldioxane and thiophenyldioxane biradicals. ? stands for: an aliphatic ?2-?8 radical comprising 1, 2 or 3 triple ?=? bonds; aryl and thiophenyl, alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, cycloalkylbenzene, 4-cycloalkylbiphenyl, bicycloalkylbenzene, 4-bicycloalkylbiphenyl, cycloalkylthiophene, aryldioxane and thiophenyldioxane radicals.
摘要翻译：本发明涉及新的唑类，通式1A和1B的新型抗病毒活性成分，药物组合物，抗病毒药物以及预防和治疗病毒疾病，特别是由丙型肝炎病毒（HCV）引起的病毒疾病的方法，。在由虚线（---）表示单键或双键的连续线表示单键或双键的通式1A和1B中，X和Y具有不同的含义，一个是氮，另一个是氧，硫或NH基团 ; R1和R2任选地是选自2-（R）和（S） - 取代的N-酰基吡咯烷衍生物的相同的基团; N-MeTmi-N- [2-（R）和（S） - 取代的2,2-二取代乙酰胺; （2-（R）和（S） - 取代的（（（甲基）氨基） - （1-氧代 - 丁烷-2-基）-2-（11） - ]和（ - ） - 异丙基）？代表脂族α2→8双基; 环烷基，二环脂族基，烷氧基烷基，烷氧基亚烷氧基烷基，烯氧基烷基，炔氧基烷基双基和它们的硫杂类似物; 烯基噻吩和炔基噻吩，烷氧基芳基，烯氧基芳基，炔氧基芳基，烷基硫杂芳基，烯硫基芳基，炔基硫杂芳基，环烷基噻吩，芳基二氧杂环己烷和噻吩基二恶烷双基。？代表：包含1,2或3个三重α=β的脂族α2→8基团。债券; 炔基环烷基，炔基二恶烷，炔基芳基，烷基噻吩，烯基噻吩和炔基噻吩，环烷基苯，4-环烷基联苯，双环烷基苯，4-双环烷基联苯，环烷基噻吩，芳基二恶烷和噻吩基二恶烷。

4. 发明申请

WO2013058681A3 SUBSTITUTED PHENOXYACETIC ACIDS AND ESTERS AND AMIDES THEREOF, COMPRISING A 2,6-DIOXO-2,3,6,7-TETRAHYDRO-1Н-PURINE-8-YL FRAGMENT AND CONSTITUTING А2A ADENOSINE RECEPTOR ANTAGONISTS, AND THE USE THEREOF 审中-公开
标题翻译：包含2,6-二氧代-2,3,6,7-四氢-1H-嘌呤-8-yL片段并构成-2A腺苷受体拮抗剂的取代苯氧乙酸及其酯和酰胺及其用途
公开(公告)号：WO2013058681A3
公开(公告)日：2013-06-20
申请号：PCT/RU2012000830
申请日：2012-10-12
申请人： NEWVAC LLC , IVACHTCHENKO ALEXANDRE VASILIEVICH , MITKIN OLEG DMITRIEVICH , KADIEVA MADINA GEORGIEVNA , OKUN ILYA MATUSOVICH
发明人： IVACHTCHENKO ALEXANDRE VASILIEVICH , MITKIN OLEG DMITRIEVICH , KADIEVA MADINA GEORGIEVNA , OKUN ILYA MATUSOVICH
IPC分类号： C07D473/06 , A61K31/522 , A61P25/16 , A61P25/24 , A61P25/28 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02
CPC分类号： C07D473/06
摘要： The invention relates to novel compounds of general formula 1, namely substituted phenoxyacetic acids and esters and amides thereof, which comprise a 2,6-dioxo-2,3,6,7-tetrahydro-1H-purine-8-yl fragment and exhibit antagonist activity against A2A adenosine receptors, and to the use thereof as a therapeutic principle and agent (adjuvant) for pharmaceutical compositions and drugs, as well as to methods for treating diseases of the central nervous system, oncological diseases and viral and bacterial diseases, where R1, R2 and R3, not necessarily simultaneously, are hydrogen, C1-C5 alkyl, C3-C5 alkenyl or C3-C5 alkynyl; R4 is hydrogen, a halogen atom, a hydroxyl, C1-C3 alkyl, C1-C3 alkyloxy; R5 is hydrogen, C1-C3 alkyl, the group -C(O)R6; and R6 is a hydroxyl, C1-C5 alkyloxy, C3-C5 alkenyloxy, C3-C5 alkynyloxy, an optionally substituted amino group where the substitutes, not necessarily identical, are selected from hydrogen, C1-C5 alkyl optionally substituted with a mono- or dialkylamino group or an alkoxy group or a 5-6 membered saturated heterocyclyl comprising 1-2 heteroatoms selected from nitrogen and oxygen; pyridyl or phenyl optionally substituted with 1-3 methoxy groups; or an optionally substituted 6 membered saturated heterocyclyl optionally annulated with a 5 membered unsaturated heterocyclyl and comprising 2 nitrogen atoms, where the substitutes are selected from C1-C5 alkyl optionally substituted with a 5 membered heteroaryl comprising 1-3 heteroatoms selected from nitrogen and oxygen; or a 6 membered optionally saturated heterocyclyl comprising 1-2 nitrogen atoms optionally substituted with C1-C5 alkyl, oxo, optionally substituted with phenyl; and the broken line with an adjacent unbroken line represents a single, double or triple bond.
摘要翻译：本发明涉及通式1的新型化合物，即取代的苯氧基乙酸及其酯和酰胺，其包含2,6-二氧代-2,3,6,7-四氢-1H-嘌呤-8-基片段并展现对A 2A腺苷受体的拮抗剂活性，及其作为药物组合物和药物的治疗原理和药剂（佐剂）的用途，以及治疗中枢神经系统疾病，肿瘤疾病和病毒和细菌疾病的方法，其中 R 1，R 2和R 3不必同时为氢，C 1 -C 5烷基，C 3 -C 5烯基或C 3 -C 5炔基; R4是氢，卤原子，羟基，C1-C3烷基，C1-C3烷氧基; R5是氢，C1-C3烷基，基团-C（O）R6; 并且R6是羟基，C1-C5烷氧基，C3-C5烯氧基，C3-C5炔氧基，任选取代的氨基，其中取代基不一定相同，选自氢，任选被一 - 或二烷基氨基或烷氧基或包含1-2个选自氮和氧的杂原子的5-6元饱和杂环基; 吡啶基或任选被1-3个甲氧基取代的苯基; 或任选取代的6元饱和杂环基，其任选地被5元不饱和杂环基环化并且包含2个氮原子，其中所述取代基选自任选地被5元杂芳基取代的C 1 -C 5烷基，所述5元杂芳基包含1-3个选自氮和氧的杂原子; 或6个任选饱和的杂环基，其包含1-2个任选被苯基任选取代的C 1 -C 5烷基，氧代取代的氮原子; 并且具有相邻的不间断线的虚线表示单键，双键或三键。

5. 发明申请

WO2007136300A2 SUBSTITUTED INDOLES AND A METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代的吲哚及其生产和使用方法
公开(公告)号：WO2007136300A2
公开(公告)日：2007-11-29
申请号：PCT/RU2007000244
申请日：2007-05-17
申请人： ALLA CHEM LLC , IVASCHENKO ANDREY ALEXANDROVIC , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH , MITKIN OLEG DMITRIEVICH , OKUN ILYA MATUSOVICH , KYSELVEV ALEXANDR SERGEEVICH , KYSIL VOLODYMYR MIKHAILOVICH , SAVCHUK NIKOLAY FILIPPOVICH , IVASHCHENKO ALEXANDER VASILIEV
发明人： IVASCHENKO ANDREY ALEXANDROVIC , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH , MITKIN OLEG DMITRIEVICH , OKUN ILYA MATUSOVICH , KYSELVEV ALEXANDR SERGEEVICH , KYSIL VOLODYMYR MIKHAILOVICH , SAVCHUK NIKOLAY FILIPPOVICH , IVASHCHENKO ALEXANDER VASILIEV
IPC分类号： C07D209/42 , A61K31/405 , A61K31/407 , A61K31/416 , A61K31/4465 , A61K31/454 , A61K31/4709 , A61K31/506 , A61K31/5365 , A61K31/55 , A61P31/12 , A61P31/16 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D409/04 , C07D413/14 , 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 R 1 , R 1 4
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，特别是由感染性肝炎（HCV，HBV）病毒引起的病毒性疾病的药物制剂的用途，，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R 1，R 1， ⁴

6. 发明申请

WO2009082268A3 LIGANDS OF a-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF 审中-公开
标题翻译：阿托品和多巴胺，组胺，咪唑啉和丝氨酸受体的配体及其用途
公开(公告)号：WO2009082268A3
公开(公告)日：2009-08-20
申请号：PCT/RU2008000780
申请日：2008-12-19
申请人： IVASHCHENKO ANDREY ALEXANDROVI , ALLA CHEM LLC , IVASHCHENKO ALEXANDER VASILIEV , LAVROVSKY YAN VADIMOVICH , MITKIN OLEG DMITRIEVICH , SAVCHUK NIKOLAY FILIPPOVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , IVASHCHENKO ALEXANDER VASILIEV , LAVROVSKY YAN VADIMOVICH , MITKIN OLEG DMITRIEVICH , SAVCHUK NIKOLAY FILIPPOVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH
IPC分类号： C07D471/04 , A61K31/43 , A61K31/519 , A61P25/00 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to novel ligands, the broad spectrum of which simultaneously comprises alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and seratinin receptors, including 5-HT7 seratinin receptors, as compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers and also in the form of pharmaceutically acceptable salts and/or hydrates, wherein: R1 is an aminogroup substituent, optionally substituted C1-C2 alkyl, acyl, heterocyclyl, alkoxycarbonyl and substituted sulphonyl; R2 is a cyclic group substituent, including a hydrogen atom, a halogen atom, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulphonyl; Ar is optionally substituted aryl, possibly annelated with heterocyclyl, or optionally substituted heterocyclyl; W is an optionally substituted CH2-CH=CH group, an optionally substituted C=C group, an SO2 group; n=1 or 2; m=1, 2 or 3; a continuous line together with a dotted line following it (---) represent a single or a double bonds. Medicinal substances, pharmaceutical compositions containing the novel ligands in the form of medicinal substances, novel medicinal agents which are used for treating diseases and states of the central nervous system of human beings and animals, are also disclosed.
摘要翻译：本发明涉及新的配体，其广谱同时包含α-游离碱形式的通式1化合物的α-肾上腺素能受体，多巴胺受体，组胺受体，咪唑啉受体和seratinin受体，包括5-HT7丝氨酸蛋白受体，几何异构体，外消旋混合物或单独的光学异构体，还以药学上可接受的盐和/或水合物的形式，其中：R 1是氨基取代基，任选取代的C 1 -C 2烷基，酰基，杂环基，烷氧基羰基和取代的磺酰基; R2是环状基团取代基，包括氢原子，卤素原子，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; Ar是任选取代的芳基，可能与杂环基或任选取代的杂环基取代; W是任选取代的CH 2 -CH = CH基团，任选取代的C = C基团，SO 2基团; n = 1或2; m = 1,2或3; 连续线与虚线一起（---）表示单键或双键。还公开了药物，包含药物形式的新型配体的药物组合物，用于治疗人类和动物的中枢神经系统的疾病和状态的新型药物。

7. 发明申请

WO2008115098A3 SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR THE PRODUCTION AND THE USE THEREOF 审中-公开
标题翻译：取代2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚，其生产方法及其用途
公开(公告)号：WO2008115098A3
公开(公告)日：2008-11-13
申请号：PCT/RU2008000169
申请日：2008-03-21
申请人： ALLA CHEM LLC , IVASHCHENKO ANDREY ALEXANDROVICH , IVASHCHENKO ALEXANDER VASILIEVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH , MITKIN OLEG DMITRIEVICH , KRAVCHENKO DMITRI VLADIMIROVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , IVASHCHENKO ALEXANDER VASILIEVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH , MITKIN OLEG DMITRIEVICH , KRAVCHENKO DMITRI VLADIMIROVICH
IPC分类号： C07D471/04 , A61K31/437 , A61P3/14 , A61P9/10 , A61P17/00 , A61P17/02 , A61P17/06 , A61P25/08 , A61P25/14 , A61P25/28 , A61P37/08
CPC分类号： C07D471/04
摘要： The invention relates to novel substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles, to the pharmaceutically acceptable salts and/or hydrates thereof, to methods for the production and the use thereof in the form of biologically active substances, to novel pharmaceutical compositions and medicinal agents which are based thereon, exhibit antihistamine activity and contain, in the form of an active substance, substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles and the pharmaceutically acceptable salts and/or hydrates thereof and to the to methods for the production and the use thereof. The novel substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles and the pharmaceutically acceptable salts and/or hydrates thereof correspond to general formula 1.1, 1.2 or 1.3, wherein, in the compounds of 1.1, R 1 is an amino group substituent selected from hydrogen or optionally substituted C 1 -C 5 alkyl; R 2 is a hydrogen atom or C 1 -C 4 alkyl; R 3 i
摘要翻译：本发明涉及新的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚及其药学上可接受的盐和/或水合物，用于生产和使用它们的方法生物活性物质的形式，以其为基础的新型药物组合物和药剂，表现出抗组胺活性，并以活性物质的形式含有取代的2,3,4,5-四氢-1H-吡啶并[4,3 -b]吲哚及其药学上可接受的盐和/或水合物，以及其制备方法和用途。新颖的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚及其药学上可接受的盐和/或水合物对应于通式1.1,1.2或1.3，其中在 1.1，R 1是选自氢或任选取代的C 1 -C 5烷基的氨基取代基; R 2是氢原子或C 1 -C 4烷基; R 3 3 i

8. 发明申请

WO2010134846A8 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：WO2010134846A8
公开(公告)日：2012-01-05
申请号：PCT/RU2010000216
申请日：2010-04-30
申请人： IVASHCHENKO ANDREY ALEXANDROVICH , ALLA CHEM LLC , IVASHCHENKO ALEXANDER VASILIEVICH , KYSIL VOLODYMYR MIKHAILOVICH , MITKIN OLEG DMITRIEVICH , SAVCHUK NIKOLAY FILIPPOVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , IVASHCHENKO ALEXANDER VASILIEVICH , KYSIL VOLODYMYR MIKHAILOVICH , MITKIN OLEG DMITRIEVICH , SAVCHUK NIKOLAY FILIPPOVICH
IPC分类号： C07D471/04 , A61K9/08 , A61K9/48 , A61K31/437 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： A61K31/437 , A61K9/0019 , A61K9/2018 , A61K9/2059 , A61K9/4858 , A61K47/10 , C07D471/04
摘要： The invention relates to substituted 8-sulfonyl-2,3,4,5-tetrahydro-1H-?-carbolines of general formula 1 and pharmaceutically acceptable salts and ligands thereof which exhibit biological activity with respect to alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepinephrine receptors and serotonin receptors simultaneously, as well as to active ingredients and pharmaceutical compositions containing the new ligands as active ingredient and to new drugs that can be used to treat diseases and conditions of the central nervous system. In general formula 1, R1 is a substituent selected from hydrogen, optionally substituted C1-C3 alkyl or C1-C4 alkoxycarbonyl; R2 is a cyclic system substituent, inter alia a hydrogen atom, optionally substituted C1-C3 alkyl, optionally substituted C2-C3 alkenyl or substituted sulfonyl; and R3 is optionally substituted aryl or a substituted amino group.
摘要翻译：本发明涉及通式1的取代的8-磺酰基-2,3,4,5-四氢-1H--咔啉及其与α肾上腺素能受体，受体，咪唑啉受体，σ受体，去甲肾上腺素受体和5-羟色胺受体，以及含有新配体作为活性成分的活性成分和药物组合物，以及可用于治疗中枢神经系统疾病和病症的新药物。在通式1中，R 1是选自氢，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是环系取代基，特别是氢原子，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; 并且R 3是任选取代的芳基或取代的氨基。

9. 发明申请

WO2008123796A3 SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚，其生产方法及其用途
公开(公告)号：WO2008123796A3
公开(公告)日：2008-12-31
申请号：PCT/RU2008000196
申请日：2008-04-01
申请人： ALLA CHEM LLC , IVASHCHENKO ANDREY ALEXANDROVI , IVASHCHENKO ALEXANDER VASILIEV , TKACHENKO SERGEY YEVGENIEVICH , FROLOV YEVGENIY BORISOVICH , MITKIN OLEG DMITRIEVICH , KRAVCHENKO DMITRI VLADIMIROVIC , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , IVASHCHENKO ALEXANDER VASILIEVICH , TKACHENKO SERGEY YEVGENIEVICH , FROLOV YEVGENIY BORISOVICH , MITKIN OLEG DMITRIEVICH , KRAVCHENKO DMITRI VLADIMIROVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH
IPC分类号： C07D471/04 , A61K31/437 , A61P37/02 , A61P37/08
CPC分类号： A61K31/437 , A61K31/444 , C07D471/04
摘要： The invention relates to antagonists of 5-HT6 serotoninreceptors which simultaneously control the homeostasis of calcium ions in cells and is in the form of substituted 2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indoles of general formula (1), wherein R1 is an aminogroup substituent selected form optionally substituted C1-C5 alkyl; R2 i is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3 or OCF3; Ar is C1-C6 alkoxy non-substituted or substituted by halogen, C1-C6 alkyl, phenyl substituted byan aminogroup or trifluormethyl or optionally substituted aromatic 6-member heterocycle comprising 1-3 nitrogen atoms in a cycle; and W is an -CH2CH2- ethyl group, vinyl or acetenyl group. The novel compounds selected from the compounds of general formula 1, methods for the production thereof, pharmaceutical compositions and methods for the use thereof are also disclosed.
摘要翻译：本发明涉及5-HT6血清素受体的拮抗剂，其同时控制细胞中钙离子的体内平衡，并且是一般为取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚的形式式（1）其中R1是选自任选取代的C 1 -C 5烷基的氨基取代基; R2 i是一个或多个选自氢，卤素，C 1 -C 3烷基，CF 3或OCF 3的取代基; Ar是未被取代或被卤素取代的C1-C6烷氧基，C1-C6烷基，被氨基或三氟甲基取代的苯基或任选取代的芳族6-元杂环，其中一个循环包含1-3个氮原子; W是-CH 2 CH 2 - 乙基，乙烯基或乙炔基。还公开了选自通式1的化合物，其制备方法，药物组合物及其使用方法的新化合物。

10. 发明申请

WO2008123800A2 SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES 审中-公开
标题翻译：取代2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚
公开(公告)号：WO2008123800A2
公开(公告)日：2008-10-16
申请号：PCT/RU2008000213
申请日：2008-04-04
申请人： ALLA CHEM LLC , IVASHCHENKO ANDREY ALEXANDROVI , IVASHCHENKO ALEXANDER VASILIEV , TKACHENKO SERGEY YEVGENIEVICH , FROLOV YEVGENIY BORISOVICH , MITKIN OLEG DMITRIEVICH , KRAVCHENKO DMITRI VLADIMIROVIC , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVI , IVASHCHENKO ALEXANDER VASILIEVICH , TKACHENKO SERGEY YEVGENIEVICH , FROLOV YEVGENIY BORISOVICH , MITKIN OLEG DMITRIEVICH , KRAVCHENKO DMITRI VLADIMIROVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH
IPC分类号： C07D471/04 , A61K31/437 , A61P37/02 , A61P37/08
CPC分类号： C07D471/04
摘要： The invention relates to novel blockers for pharmaceutical compositions exhibiting antihistaminic activity and to a method for treating and preventing the development of different allergic diseases. The inventive blockers are in the form of substituted 2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indoles of general formula (1) and the pharmaceutically acceptable salts and/or hydrates thereof, wherein R 1 is an aminogroup substituent selected from optionally substituted C 1 -C 5 alkyl, optionally substituted C 2 -C 4 alkenyl, optionally substituted C 1 -C 5 alkinyl, carbamoyl, thiocarbamoyl and a substituted mercapto group R 2 i
摘要翻译：本发明涉及具有抗组胺活性的药物组合物的新型阻断剂，以及治疗和预防不同过敏性疾病发展的方法。本发明的阻断剂是通式（1）的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚及其药学上可接受的盐和/或水合物的形式， SUP> 1是选自任选取代的C 1 -C 5烷基，任选取代的C 2 -C 3烷基的氨基取代基，亚烷基，任选取代的C 1 -C 5炔基，氨基甲酰基，硫代氨基甲酰基和取代的巯基R 2， SUB> I

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