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    Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds
    3.
    发明授权
    Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds 失效
    吲哚，苯并呋喃，苯并噻吩含脂氧合酶抑制化合物

    公开(公告)号：US4873259A

    公开(公告)日：1989-10-10

    申请号：US138073

    申请日：1988-01-11

    申请人： James B. Summers, Jr. ,  Bruce P. Gunn ,  Dee W. Brooks

    发明人： James B. Summers, Jr. ,  Bruce P. Gunn ,  Dee W. Brooks

    IPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58

    CPC分类号： C07D333/58 ,  C07D209/14 ,  C07D307/81

    摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.sub.12 arylalkoxy, (17) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (18) aryl, (19) aryloxy, (20) aroyl, (21) C.sub.1 to C.sub.12 arylalkyl, (22) C.sub.2 to C.sub.12 arylalkenyl, (23) C.sub.1 to C.sub.12 arylalkoxy, or (24) C.sub.1 to C.sub.12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C.sub.1 to C.sub.12 alkyl, alkoxy, and halosubstituted alkyl;Z is oxygen or sulfur;and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes.Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase activity.

    摘要翻译： 其中R 1是（1）氢，（2）C 1至C 4烷基，（3）C 2至C 4链烯基或（4）NR 2 R 3，其中R 2和R 3独立地选自（1）氢 ，（2）C1至C4烷基和（3）羟基，但R2和R3不同时为羟基; 其中X是氧，硫，SO 2或NR 4，其中R 4是（1）氢，（2）C 1至C 6烷基，（3）C 1至C 6烷酰基，（4）芳酰基或（5）烷基磺酰基; A选自C1至C6亚烷基和C2至C6亚烯基; n为1-5; 在（1）氢，（2）卤素，（3）羟基，（4）氰基，（5）卤代烷基，（6）C1至C12烷基，（7）C2至C12烯基， （8）C1至C12烷氧基，（9）C3至C8环烷基，（10）C1-C8硫代烷基，（11）芳基，（12）芳氧基，（13）芳酰基，（14）C1至C12芳烷基，（15） （18）芳基，（19）芳氧基，（20）芳酰基，（21）C1〜C12芳基烷基，（22）C1〜C12芳基烷氧基，（17）C1〜C12芳基烷氧基，（17） ）C 2至C 12芳基烯基，（23）C 1至C 12芳基烷氧基或（24）C 1至C 12芳硫基烷氧基，其中取代基选自卤素，硝基，氰基，C 1至C 12烷基，烷氧基和卤代烷基; Z是氧或硫; 和M是氢，可药用阳离子，芳酰基或C 1至C 12烷酰基，是5-和/或12-脂氧合酶的有效抑制剂。 还公开了脂氧合酶抑制组合物和抑制脂氧合酶活性的方法。