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    ANTIVIRAL 2,4-PYRIMIDINDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
    81.
    发明授权
    ANTIVIRAL 2,4-PYRIMIDINDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 失效
    抗病毒2.4嘧啶二酮衍生物和工艺及其

    公开(公告)号：EP0736015B1

    公开(公告)日：2001-03-07

    申请号：EP95903455.4

    申请日：1994-12-20

    申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

    发明人： SON, Jong, Chan ,  LEE, Ill, Young ,  BAE, Byung, Il ,  HAN, Jeong, Sik ,  CHOI, Joong, Kwon ,  CHAE, Yung, Bok

    IPC分类号： C07D239/60 ,  C07D239/54 ,  A61K31/505

    CPC分类号： C07D239/54 ,  C07D239/60

    摘要： Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by formula (I) wherein: R1 represents an unsubstituted or substituted alkyl group represented by CH¿2?CH=CR?5R6¿ or an unsubstituted or substituted propargyl group represented by CH¿2?C CR?7¿ wherein R?5, R6 and R7¿ are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C¿1-10? carbonyloxy, hydroxy, azido, cyano, optionally substituted amino, optionally substituted phosphonyl, optionally substituted phenyl, C3-10 heteroaryl, C1-3 alkoxy or benzyloxy radical; a C2-10 alkyl or alkenyl group; a cyclopropyl group; an optionally substituted phenyl group; a C3-10 heteroaryl group; a C1-10 ester group; or an optionally substituted C1-10 alkylamide group; R?2¿ represents a halogen atom, an optionally substituted C¿1-5? alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl group or a benzyl group; R?3 and R4¿ represent independently a hydrogen or halogen atom, or a hydroxy, C¿1-3? alkyl, fluoromethyl, C1-3 alkoxy, amino, C2-6 alkylester or C2-7 alkylamide group; A represents an oxygen or sulfur atom; Z represents an oxygen or sulfur atom; a carbonyl group; an amino group; or a methylene group optionally substituted with at least one selected from the group consisting of a halogen atom, and a cyano, hydroxy, azido, amino, C1-3 alkylamide, C1-4 ester, and nitro groups.

    Hydroquinone derivative and pharmaceutical use thereof
    89.
    发明公开
    Hydroquinone derivative and pharmaceutical use thereof 失效
    Hydrochinon-Derivate und deren pharmazeutische Verwendung

    公开(公告)号：EP0831092A2

    公开(公告)日：1998-03-25

    申请号：EP97250280.1

    申请日：1997-09-17

    申请人： JAPAN ENERGY CORPORATION

    发明人： Isobe, Yoshiaki ,  Goto, Yuso ,  Tobe, Masanori ,  Takahashi, Osamu

    IPC分类号： C07D405/12 ,  C07D239/54 ,  A61K31/505

    CPC分类号： C07D239/545 ,  C07D405/12

    摘要： Disclosed is a hydroquinone derivative or a pharmaceutically acceptable salt thereof, the hydroquinone derivative being represented by formula (I):
    wherein

    R 1 is a phenyl group which is unsubstituted or substituted with a substituent or substituents each independently selected from the group consisting of a halogen atom, a C1-4 alkyl group and a C1-4 alkoxy group;
    R 2 is a hydrogen atom or a C1-4 alkyl group;
    each of R 3 and R 4 is independently a hydrogen atom or a C1-4 alkyl group;
    R 5 is a hydrogen atom or a C1-4 alkyl group;
    each of R 6 , R 7 and R 8 is independently a hydrogen atom or a C1-4 alkyl group;
    P is a hydroxyl group;
    Q is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group;
    P may form together with Q an ether bond;
    R is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group, provided that when one of said Q and said R is an oxo group, the other is also an oxo group;
    X is a single bond, an -NR 10 - group or a -CH 2 -NR 10 - group in which R 10 is a hydrogen atom or a C1-4 alkyl group;
    Y is a methylene group or a carbonyl group; and
       dotted bonds in a six membered ring represent that said six membered ring has the maximum number of double bonds.

    摘要翻译： 公开了氢醌衍生物或其药学上可接受的盐，氢醌衍生物由式（I）表示：其中R 1是未取代的或被取代基取代的苯基，其各自独立地选自 由卤素原子，C 1-4烷基和C 1-4烷氧基组成的基团; R 2是氢原子或C 1-4烷基; R 3和R 4各自独立地为氢原子或C 1-4烷基; R 5是氢原子或C 1-4烷基; R 6，R 7和R 8各自独立地为氢原子或C 1-4烷基; P是羟基; Q是羟基，C 1-4烷氧基，C 1-18酰氧基或氧代基; P可与Q形成醚键; R是羟基，C 1-4烷氧基，C 1-18酰氧基或氧代基，条件是当所述Q和所述R中的一个是氧代基时，另一个也是氧代基; X是单键，-NR 10 - 或-CH 2 -NR 10 - 基，其中R 10是氢原子或C 1-4烷基; Y是亚甲基或羰基; 并且六元环中的点状键表示所述六元环具有最大数目的双键。

    6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof
    90.
    发明公开
    6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
    6-取代基Acylopyrimidin-Nucleoside-Derivate und diese als wirksamen Stoff enthaltende Antivirusmittel

    公开(公告)号：EP0829476A2

    公开(公告)日：1998-03-18

    申请号：EP97110658.8

    申请日：1990-09-28

    申请人： Mitsubishi Chemical Corporation

    发明人： Miyasaka, Tadashi ,  Tanaka, Hiromichi ,  De Clercq, Erik Desire Alice ,  Masanori, Baba ,  Walker, Richard Thomas ,  Ubasawa, Masaru

    IPC分类号： C07D239/46 ,  C07D239/54 ,  C07D239/56 ,  C07D239/58 ,  C07D239/60 ,  A61K31/505

    CPC分类号： C07D239/47 ,  C07D239/54 ,  C07D239/545 ,  C07D239/56 ,  C07D239/58 ,  C07D239/60

    摘要： A 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I';


    wherein R 1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group;
    R 2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a halogen atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups;
    R 3 represents a hydrogen atom, methyl, branched alkyl or -CH 2 -Z-(CH 2 ) n -R 5 group where R 5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R 5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5,
    R 4 represents a hydrogen atom, alkyl or aralkyl group,
    X represents an oxygen or sulfur atom,
    Y represents an oxygen or sulfur atom,
    provided that when R 4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R 5 does not represent a hydroxyl group,
    or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient.

    摘要翻译： 由以下通式I或I'表示的6-取代的环磷酰嘧啶核苷衍生物; 其中R 1表示氢原子，卤素原子，烷基，环烷基，烯基，炔基，烷基羰基，芳基羰基，芳基羰基烷基，芳硫基或芳烷基。 R 2表示芳硫基，烷硫基，环烷基硫基，芳基亚磺酰基，烷基亚磺酰基，环烷基亚磺酰基，烯基，炔基，芳烷基，芳基羰基，芳基羰基烷基或芳氧基，这些基团任选被一个或多个选自卤素原子， 烷基，烷氧基，羟基，硝基，氨基，氰基和酰基; R 3表示氢原子，甲基，支链烷基或-CH 2 -Z-（CH 2）n R 5基团，其中R 5表示氢原子，卤素原子，羟基，杂环羰氧基，甲酰氧基，烷基羰基氧基，环烷基羰基氧基 ，芳烷基羰基氧基，芳基羰基氧基，叠氮基，烷氧基羰基氧基，N-烷基氨基甲酰氧基，N-芳基氨基甲酰氧基，N-烷基硫代氨基甲酰氧基，N-芳硫基氨基甲酰氧基，烷氧基，芳烷氧基，支链烷基，环烷基或芳基，上述作为R 5烷氧基羰基氧基至芳基 被一个或多个选自卤素原子，芳基，烷基，烷氧基和卤代烷基的取代基取代，Z表示氧，硫原子或亚甲基，n表示0或1〜5的整数，R 4表示 氢原子，烷基或芳烷基，X表示氧或硫原子，Y表示氧或硫原子，条件是当R 4和Z分别代表式IR 5中的氢原子和氧原子时， 不代表水电 甲基或其药学上可接受的盐，以及含有其衍生物或其盐作为活性成分的抗病毒剂。