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    LEUKOTRIENE B4 DERIVATIVES, METHODS OF PREPARING THEM AND THEIR USE AS DRUGS
    9.
    发明申请
    LEUKOTRIENE B4 DERIVATIVES, METHODS OF PREPARING THEM AND THEIR USE AS DRUGS 审中-公开
    新白三烯B4衍生物，用于生产及其作为药物

    公开(公告)号：WO1995020564A1

    公开(公告)日：1995-08-03

    申请号：PCT/EP1994000216

    申请日：1994-01-27

    申请人： SCHERING AKTIENGESELLSCHAFT ,  SKUBALLA, Werner ,  BUCHMANN, Bernd ,  HEINDL, Josef ,  FRÖHLICH, Wolfgang ,  EKERDT, Roland ,  GIESEN, Claudia

    发明人： SCHERING AKTIENGESELLSCHAFT

    IPC分类号： C07C59/62

    CPC分类号： C07C59/72 ,  C07C59/62 ,  C07C69/708 ,  C07C235/08 ,  C07C2601/14

    摘要： Described are pharmacologically active leukotriene B4 derivatives of general formula (I) in which R1 is CH2OH, CH3, CF3, COOR4 or CONR5R6, R2 is H or an organic-acid group with 1 to 15 C-atoms, R3 is H, a C1-C14 alkyl group, optionally with one or more substituents, a C3-C10 cycloalkyl group, a C6-C10 aryl group optionally substituted, independently of each other, with one or more halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy groups or R3 is a 5- to 6-membered aromatic heterocyclic ring with at least one hetero atom, R4 is H, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl group optionally substituted with 1 to 3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy groups or R4 is CH2-CO-(C6-C10) aryl or a 5- to 6-membered ring with at least one hetero atom, A is a trans, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B is a straight-chain or branched-chain C1-C10 alkylene group, which may be substituted with fluorine, or the group (a), D is a direct bond, oxygen, sulphur, -CC- or -CH=CR7 or, together with B, may also form a direct bond, R5 and R6 which may be the same or different, are H or C1-C4 alkyl, or R6 is H and R5 is C1-C15 alkanoyl or R8SO2-, R5 and R6 being optionally substituted with OH, R7 is H, C1-C5 alkyl, chlorine or bromine, R8 is defined in the same way as R3, n is 2 to 5 plus, when R4 is hydrogen, salts of these compounds with physiologically tolerated bases, as well as their cyclo-dextrin clathrates.

    摘要翻译： 药理学上通式（I）的活性白三烯B4衍生物被描述，其中R 1是CH 2 OH，CH 3，CF 3，COOR 4，CONR 5 R 6，或R 2是H或有机残基与1-15个碳原子，R 3是H，任选地单 或多取代的C1-C14烷基，C3-C10环烷基任选独立地单独使用，或者乘以卤素，苯基，C1-C4烷基，C1-C4烷氧基，氟甲基，氯甲基，三氟甲基，羰基，羧基或羟基取代的 C6-C10芳基基团或具有至少1个杂原子象征着的5-6元芳族杂环，R 4是氢，C1-C10烷基，C3-C10环烷基，任选地被1-3个卤素，苯基，C1-C4烷基，C1取代的 C4烷氧基，氟甲基，氯甲基，三氟甲基，羧基或羟基取代的C 6 -C 10 - 芳基，CH 2 -CO-（C6-C10）芳基或具有至少1个杂原子的5-6元环，是反式，反式 - CH = CH-CH = CH，-CH 2 CH 2一个-CH = CH-或一个Tetramethylengrup PE，B是直链或支链的，一个C 1个-C 10亚烷基，其可任选被氟取代，或（a）象征团，D是一个直接键，氧，硫， - CC-，-CH = CR7，或连同乙 也可以代表一个直接键，R 5和R 6相同或不同并且是H或C1-C4烷基或R 6是H和R 5的C1-C15烷酰基或R8SO2-，任选地被OH取代的，R 7是H，C1-C5烷基 ，氯，溴，R8的含义同R 3，n为2-5，并且当R 4是氢，其与生理学上可接受的碱及其环糊精笼形物的盐。