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    SUBSTITUTED AZOLES, ANTIVIRAL ACTIVE COMPONENT, PHARMACEUTICAL COMPOSITION, METHOD FOR PREPARATION AND USE THEREOF
    2.
    发明申请
    SUBSTITUTED AZOLES, ANTIVIRAL ACTIVE COMPONENT, PHARMACEUTICAL COMPOSITION, METHOD FOR PREPARATION AND USE THEREOF 有权
    取代的AZOLES，抗病毒活性成分，药物组合物，其制备和使用方法

    公开(公告)号：US20130253008A1

    公开(公告)日：2013-09-26

    申请号：US13990428

    申请日：2011-11-28

    申请人： Alexandre Vasilievich Ivachtchenko ,  Vadim Vasilievich Bichko ,  Oleg Dmitrievich Mitkin

    发明人： Alexandre Vasilievich Ivachtchenko ,  Vadim Vasilievich Bichko ,  Oleg Dmitrievich Mitkin

    IPC分类号： C07D403/14 ,  C07D403/04 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14

    CPC分类号： C07D403/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

    摘要： The present invention relates to novel azoles, novel antiviral active components of the general formulas 1A and 1B, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatitis C viruses (HCV). In general formulas 1A and 1B wherein: solid lines with accompanying dotted lines () represent ordinary bond or double bond, provided that one of them is an ordinary bond, the other one is double bond; X and Y accept various meanings, one of them is—nitrogen, the other—oxygen, sulfur or NH group; R1 and R2—optionally the same radicals selected from 2-(R)- and (S)-substituted N-acyl pyrrolidine derivatives; N-methyl-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl[2-(R) and (S)-substituted ((methyl)amino)-(1-oxobutan-2-yl)-2-(R)-] and (S)-iso-propyl)-carbamates. A represents aliphatic C2-C8 biradical; dioxane, cyclo- and bicycloaliphatic, alkyloxyalkyl, alkyloxyalkylenoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl biradicals and their thioanaloges; aryl and thiophene alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, alkyloxyaryl, alkenyloxyaryl, alkynyloxyaryl, alkylthioaryl, alkenylthioaryl, alkynylthioaryl, cycloalkylthiophene, aryldioxane and thiophenyldioxane biradicals. B represents: aliphatic C2-C8 radical, including 1, 2 or 3 triple C≡C bonds; aryl and thiophene, alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, cycloalkylbenzene, 4-cycloalkylbiphenyl, bicycloalkylbenzene, 4-bicycloalkylbiphenyl, cycloalkylthiophene, aryldioxane and thiophenyldioxane radicals.

    摘要翻译： 本发明涉及通式1A和1B的新型唑类，新型抗病毒活性成分，药物组合物，抗病毒药物，特别是丙型肝炎病毒（HCV）引起的病毒性疾病的预防和治疗方法。 在通式1A和1B中，其中：具有相应虚线（）的实线代表普通键或双键，条件是它们之一是普通键，另一个是双键; X和Y接受各种含义，其中之一是氮，其他氧，硫或NH基; R 1和R 2 - 任选相同的选自2-（R） - 和（S） - 取代的N-酰基吡咯烷衍生物的基团; N-甲基-N- [2-（R）和（S） - 取代的2,2-二取代的乙酰胺; 甲基[2-（R）和（S） - 取代的（（甲基）氨基） - （1-氧代丁-2-基）-2-（R） - ]和（S） - 异丙基） - 氨基甲酸酯。 A代表脂族C 2 -C 8双基; 烷基氧基烷基，烷氧基烷基，烷氧基烷基双基和它们的硫代烟碱; 芳基和噻吩炔基环烷基，炔基二恶烷，炔基芳基，烷基噻吩，烯基噻吩和炔基噻吩，烷氧基芳基，烯氧基芳基，炔氧基芳基，烷硫基芳基，烯基硫代芳基，炔硫基芳基，环烷基噻吩，芳基二恶烷和硫代苯基二恶烷双基。 B表示：脂族C 2 -C 8基团，包括1,2或3个三价C = C键; 芳基和噻吩，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，4-二环烷基联苯，环烷基噻吩，芳基二恶烷和硫代苯基二恶烷基。

    SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PREPARATION AND USE THEREOF
    3.
    发明申请
    SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PREPARATION AND USE THEREOF 审中-公开
    取代的吲哚类，抗真菌活性成分，其制备方法及用途

    公开(公告)号：US20130196991A1

    公开(公告)日：2013-08-01

    申请号：US13811669

    申请日：2011-07-19

    申请人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  Vadim Vasilievich Bichko

    发明人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  Vadim Vasilievich Bichko

    IPC分类号： C07D487/06 ,  C07D413/14 ,  C07D401/14 ,  C07D401/06

    CPC分类号： C07D487/06 ,  A61K9/0019 ,  A61K9/145 ,  A61K9/2059 ,  A61K31/404 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4985 ,  C07D209/82 ,  C07D209/88 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04

    摘要： The invention relates to novel antiviral active components of the general formula 1, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatisis C viruses (HCV). In the general formula 1 R1 represents hydrogen, optionally substituted C1-C4 alkyl, C6 cycloalkyl, aryl, ethoxycarbonyl, nitro group; R2 represents hydrogen; R3 represents N-mono- or N,N-disubstituted 1-methylene-piperidine-3-carboxamide of the general formula 1a or N-mono- or N,N-disubstituted 1-methylene-piperidine-4-carboxamide of the general formula 1b; R4 represents hydrogen, optionally substituted C1-C3 alkyl; or R2 and R3 together with the C-atoms they are attached to form substituted 2,3,4,9-tetrahydro-1H-carbazole of the general formula 1.1, or R2, R3, and R4 together with the atoms they are attached to form substituted azaheterocycles of the general formula 1.2; R5 and R6 optionally identical represent hydrogen, optionally substituted C1-C3 alkyl or C3-C6 cycloalkyl, or R5 and R6 together with the N-atom they are attached to form optionally substituted 5- or 6-membered azaheterocyclyl comprising one or two N-atoms and optionally condensed with benzene ring; R7 and R8 represent hydrogen or R7 and R8 together with the C-atom they are attached to form C═0 group; R9 represents azaheterocyclyl comprising at least one N-atom, unsubstituted formamide, or phenyl substituted with ethoxycarbonyl or nitro group; R10 represents hydrogen, optionally substituted C1-C3 alkyl, substituted acetyl; n=1 or 2; solid line accompanied by the dotted line, i.e. (), represents single or double C—C bond.

    摘要翻译： 本发明涉及通式1的新型抗病毒活性成分，药物组合物，抗病毒药物，预防和治疗病毒性疾病的方法，尤其是由丙型肝炎病毒（HCV）引起的。 在通式1中，R1表示氢，任选取代的C 1 -C 4烷基，C 6环烷基，芳基，乙氧羰基，硝基; R2表示氢; R 3表示通式1a的N-单 - 或N，N-二取代的1-亚甲基 - 哌啶-3-甲酰胺或通式为N-单 - 或N，N-二取代的1-亚甲基 - 哌啶-4-甲酰胺 1b; R4表示氢，任选取代的C 1 -C 3烷基; 或者R 2和R 3与它们所连接的C原子一起形成通式为1.1的取代的2,3,4,9-四氢-1H-咔唑，或者R2，R3和R4与它们所连接的原子一起 形成通式1.2的取代的氮杂环; R5和R6任选地相同，表示氢，任选取代的C 1 -C 3烷基或C 3 -C 6环烷基，或者R 5和R 6与它们所连接的N-原子一起形成任选取代的含有一个或两个N-烷基的5-或6-元氮杂环基， 原子并任选地与苯环稠合; R 7和R 8表示氢或R 7和R 8与它们连接的C原子一起形成C = O基团; R9表示氮杂环基，其包含至少一个N-原子，未取代的甲酰胺或被乙氧基羰基或硝基取代的苯基; R10表示氢，任选取代的C 1 -C 3烷基，取代的乙酰基; n = 1或2; 伴随着虚线的实线即（）表示单C或C C键。