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24 条记录 (耗时 0.014 秒)

    Leukotriene antagonists
    22.
    发明公开
    Leukotriene antagonists 失效
    白三烯，Antagonisten。

    公开(公告)号：EP0296731A1

    公开(公告)日：1988-12-28

    申请号：EP88305185.6

    申请日：1988-06-07

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： Gleason, John Gerald ,  Hall, Ralph Floyd ,  Uzinskas, Irene Nijole

    IPC分类号： C07D257/04 ,  C07D277/36 ,  C07D277/56 ,  A61K31/41

    CPC分类号： C07D257/04 ,  C07D277/56 ,  C07D285/125 ,  C07D307/68

    摘要： Compounds of formula:
    in which, inter alia q is 0 to 2, R₁ is (L) a -(CH₂) b -(T) c -B wherein a and c are 0 or 1, b is 3 to 14, L and T are independently O, S or CH₂; B is C₁₋₄ alkyl, ethynyl, CF₃, isopropenyl, furanyl, thienyl, furanyl, cyclohexyl or optionally substituted phenyl; R₂ and A are H, CF₃, C₁₋₄ alkyl, C₁₋₄ alkoxy, halogen, OH, NO₂ or NH₂ or R₁ and A are H and R₂ is (L) a -(CH₂) b -(T) c as above; y is COR₃ or (CHX) n (CH₂) p Z wherein R₃ is OH, NH₂, aryloxy or alkoxy, n is 0 or 1, p is 0, 1 and 2; X is H, OH, alkyl, alkoxy or F, Z is COR₃ or tetrazolyl; R is (CR₄R₅) m W, m is 0 to 6, R₄ and R₅ are alkyl and W is an optionally substituted heteroaryl group; intermediates and processes for their preparation and their use in therapy as leukotriene antagonists.

    摘要翻译： 其中特别是q为0至2，R 1为（L）a-（CH 2）b - （T）c B的化合物：其中a和c为0或1，b为3至14，L 和T独立地为O，S或CH 2; B是C 1-4烷基，乙炔基，CF 3，异丙烯基，呋喃基，噻吩基，呋喃基，环己基或任选取代的苯基; R2和A是H，CF3，C1-4烷基，C1-4烷氧基，卤素，OH，NO2或NH2，R1和A是H，R2是（L）a-（CH2）b-（T） ; y是COR 3或（CHX）n（CH 2）p Z，其中R 3是OH，NH 2，芳氧基或烷氧基，n是0或1，p是0,1和2; X是H，OH，烷基，烷氧基或F，Z是COR 3或四唑基; R为（CR 4 R 5）m W，m为0至6，R 4和R 5为烷基，W为任选取代的杂芳基; 中间体及其制备方法及其在治疗中的用途，作为白细胞三烯拮抗剂。

    Leukotriene antagonists
    24.
    发明公开
    Leukotriene antagonists 失效
    白三烯拮抗剂

    公开(公告)号：EP0202759A2

    公开(公告)日：1986-11-26

    申请号：EP86302752.0

    申请日：1986-04-14

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： Gleason, John Gerald ,  Wen-Fu Ku, Thomas ,  Hall, Ralph Floyd ,  Perchonock, Carl David

    IPC分类号： C07C321/12 ,  C07C323/19 ,  C07D233/84 ,  C07D233/90 ,  C07D257/04 ,  C07D307/40 ,  A61K31/19

    CPC分类号： C07D257/04 ,  A61K31/19 ,  C07C45/298 ,  C07C45/44 ,  C07C45/56 ,  C07C45/62 ,  C07C45/673 ,  C07C45/68 ,  C07C45/71 ,  C07C47/542 ,  C07C47/546 ,  C07C47/548 ,  C07C47/55 ,  C07C47/575 ,  C07C323/56 ,  C07C323/60 ,  C07C323/66 ,  C07C323/67 ,  C07C2601/14 ,  C07D233/84 ,  C07D233/90 ,  C07D303/40 ,  C07D303/48 ,  C07D307/38 ,  C07D307/54 ,  C07D309/30 ,  Y02P20/55

    摘要： Compounds of formula (I)
    in which R, is C a to C 13 alkyl, C 7 to C 12 alkoxy, C 7 to C 12 thioalkyl, C 10 to C 12 1-alkynyl, 10-undecynyloxy, 11-dodecynyl, phenyl-C 4 to C 10 alkyl, phenyl-C 3 to C 9 alkoxy, phenylthio-C 3 to C 9 alkyl with the phenyl optionally mono substituted; R 2 is hydrogen, bromo, chloro, methyl, trifluoromethyl, hydroxy, methoxy or nitro; or R, is hydrogen and R 2 is C 8 to C 13 alkyl, C7 to C 12 alkoxy, C7 to C,2 thioalkyl, C 10 to C 12 1-alkynyl, 10-undecynyloxy, 11-dodecynyl, phenyl-C 4 O to C 10 alkyl, phenyl-C 3 to C 9 alkoxy, phenylthio-C 3 to C 9 alkyl with the phenyl optionally mono substituted; Y is COR 3 ,
    or {CH 2 ) 0-1 -C-tetrazolyl;

    R 3 is hydroxy or amino; R 4 is hydrogen, methyl, methoxy, fluoro or hydroxy; m is 0, 1 or 2;
    R is
    CH(CO 2 H)CH 2 CO 2 H, CH 2 CH 2 Z or
    n is 0, 1 or 2; R 5 is hydrogen, amino or NHCOCH 2 CH 2 CH(NH 2 )CO 2 H; R 6 is hydroxy, amino or NHCH 2 CO 2 H; Z is SO 3 H, SO 2 NH 2 or CN; R 7 is hydrogen, C, to C 4 alkyl or C 3 to C 4 alkenyl; R 8 is hydrogen, C, to C alkyl, carboxyl or carboxamido, or (CH 2 ) P CO 2 H, in which p is 1 or 2, when R 7 and R 9 are hydrogen or C, to C 4 alkyl; and R 9 is hydrogen, C, to C 4 alkyl or CH 2 CO 2 H; compositions containing then and their use in therapy as leukotriene antagonists, for example in the treatment of asthma.

    摘要翻译： 其中R1是C10-C13烷基，C7-C12烷氧基，C7-C12硫代烷基，C10-C12-炔基，10-十一炔基氧基，11-十二炔基，苯基-C4-C10烷基，苯基-C3- C9烷氧基，苯硫基-C3至C9烷基，苯基任选单取代; R2是氢，溴，氯，甲基，三氟甲基，羟基，甲氧基或硝基; 或R 1是氢并且R 2是C 8 -C 13烷基，C 7 -C 12烷氧基，C 7 -C 12硫代烷基，C 10 -C 12炔基，10-十一烷基氧基，11-十二炔基，苯基-C 40 -C 10烷基， C9烷氧基，苯硫基-C3至C9烷基，苯基任选单取代; Y是COR3，或者是{CH2）0-1-C-四唑基; R3是羟基或氨基; R4是氢，甲基，甲氧基，氟或羟基; m是0,1或2; R是CH（CO 2 H）CH 2 CO 2 H，CH 2 CH 2 Z或n是0,1或2; R5是氢，氨基或NHCOCH2CH2CH（NH2）CO2H; R6是羟基，氨基或NHCH2CO2H; Z是SO3H，SO2NH2或CN; R7是氢，C1-C4烷基或C3-C4链烯基; 当R 7和R 9是氢或C 1至C 4烷基时，R 8是氢，C 1至C 8烷基，羧基或甲酰氨基或（CH 2）PCO 2 H，其中p是1或2; 和R9是氢，C1-C4烷基或CH2CO2H; 含有它们的组合物以及它们作为白三烯拮抗剂在治疗中的用途，例如用于治疗哮喘。