SUBSTITUTED AZOLES, ANTI-VIRAL ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF
    1.
    发明公开
    SUBSTITUTED AZOLES, ANTI-VIRAL ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
    取代唑类抗病毒活性,药物组合物,其制造方法相同,它们的用途

    公开(公告)号:EP2657231A2

    公开(公告)日:2013-10-30

    申请号:EP11844522.0

    申请日:2011-11-28

    IPC分类号: C07D403/04

    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 hepatisis 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; R 1 and R 2 - 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 C 2 -C 8 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 C 2 -C 8 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: 本发明涉及新的吡咯,通式1A和图1B,药物组合物,抗病毒药物,用于预防和治疗病毒性疾病,由hepatisis肝炎病毒(HCV)引起的特别的方法的新的抗病毒活性组分。 在通式1A和1B worin:实线伴随虚线(---)表示普通键或双键,条件没有他们中的一个是一个普通的键,另外一个是双键; X和Y接受各种含义,它们中的一个是 - 氮,其他 - 氧,硫或NH基; R 1和R 2 - 任选地从2-(R)中选择的相同自由基 - 和(S) - 取代的N-酰基吡咯烷衍生物; 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)-carbamates。 甲darstellt脂族C 2 -C 8二价基团; 二恶烷,环和bicycloaliphatic,烷氧基烷基,alkyloxyalkylenoxyalkyl,链烯氧基烷基,alkynyloxyalkyl双自由基及其硫代类似物; 芳基和噻吩alkynylcycloalkyl,alkynyldioxane,炔,烷基噻吩,alkenylthiophene和alkynylthiophene,alkyloxyaryl,alkenyloxyaryl,alkynyloxyaryl,alkylthioaryl,alkenylthioaryl,alkynylthioaryl,cycloalkylthiophene,aryldioxane和thiophenyldioxane双自由基。 乙darstellt:脂肪族C 2 -C 8基团,包含1,2或3倍C‰¡C键; 芳基和噻吩,alkynylcycloalkyl,alkynyldioxane,炔,烷基噻吩,alkenylthiophene和alkynylthiophene,环烷基苯,4- cycloalkylbiphenyl,bicycloalkylbenzene,4- bicycloalkylbiphenyl,cycloalkylthiophene,aryldioxane和thiophenyldioxane自由基。

    SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PRODUCING AND USING SAME
    3.
    发明公开
    SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PRODUCING AND USING SAME 审中-公开
    替代品INDOLE,ANTIVIRALER WIRKSTOFF,HERSTELLUNGS- UND VERWENDUNGSVERFAHRENDAFÜR

    公开(公告)号:EP2597097A1

    公开(公告)日:2013-05-29

    申请号:EP11809940.7

    申请日:2011-07-19

    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 C 1 -C 4 alkyl, C 6 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 C 1 -C 3 alkyl; or R2 and R3 together with the C-atoms they are attached to form substituted ,3,4,9-tetrahydro-1 H -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 eneral formula 1.2; R5 and R6 optionally identical represent hydrogen, optionally substituted C 1 -C 3 alkyl or C 3 -C 6 cydoalkyl, 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=O 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 C 1 -C 3 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,特别是由丙型肝炎病毒(HCV)引起的。 在通式1中,R 1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; R3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; R 4表示氢,任选取代的C 1 -C 3烷基; 或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 形式的取代的氮杂杂环化合物1.2; 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多个 或两个N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; R 10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()表示单或双C-C键。