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32 条记录 (耗时 0.018 秒)

    Lipoxygenase inhibiting compounds
    4.
    发明授权
    Lipoxygenase inhibiting compounds 失效
    脂氧合酶抑制化合物

    公开(公告)号：US5026729A

    公开(公告)日：1991-06-25

    申请号：US430841

    申请日：1989-11-02

    申请人： Dee W. Brooks ,  James B. Summers ,  James H. Holms

    发明人： Dee W. Brooks ,  James B. Summers ,  James H. Holms

    IPC分类号： C07C275/64

    CPC分类号： C07C275/64

    摘要： Compounds having 5- and 12-lipoxygenase inhibitory activity have the structure ##STR1## where A is straight or branched divalent alkylene of from one to four carbon atoms, R.sub.1 is methyl, amino, or alkylamino of from one to six carbon atoms and the substituent group R.sub.2 is C.sub.1 -C.sub.2 alkyl.The group R.sub.3 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, halogen, cyano, and trihalomethyl, and R.sub.4 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, hydroxy, halogen, cyano, and trihalomethyl, with the proviso that when R.sub.1 is amino and A is >CHCH.sub.3, R.sub.3 and R.sub.4 may not both be hydrogen.The group designated M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group. Pharmaceutical compositions and a method of inhibiting 5- and 12-lipoxygenase activity are also disclosed.

    摘要翻译： 具有5-和12-脂氧合酶抑制活性的化合物具有结构，其中A是1-4个碳原子的直链或支链二价亚烷基，R1是甲基，氨基或1-6个碳原子的烷基氨基， 基团R2是C1-C2烷基。 基团R3是一个或多个选自氢，一至六个碳原子的烷基，一个至六个碳原子的烷氧基，一个至六个碳原子的硫代烷氧基，卤素，氰基和三卤甲基的取代基，R4是一个 或更多取代基选自氢，一至六个碳原子的烷基，一至六个碳原子的烷氧基，一至六个碳原子的硫代烷氧基，羟基，卤素，氰基和三卤代甲基，条件是当R1为 氨基和A是> CHCH 3，R 3和R 4可以不都是氢。 指定为M的基团是氢，可药用阳离子或代谢可裂解基团。 还公开了药物组合物和抑制5-和12-脂肪氧合酶活性的方法。

    Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds
    6.
    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。

    Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
    9.
    发明授权
    Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds 失效
    含吲哚，苯并呋喃和苯并噻吩的脂氧合酶抑制化合物

    公开(公告)号：US5250565A

    公开(公告)日：1993-10-05

    申请号：US823411

    申请日：1992-01-21

    申请人： Dee W. Brooks ,  James B. Summers

    发明人： Dee W. Brooks ,  James B. Summers

    IPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58 ,  A61K31/38 ,  A61K31/34 ,  C07D209/04 ,  C07D333/52

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

    摘要： Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R.sup.1 is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R.sup.1 must bear a metabolically cleavable leaving group.

    摘要翻译： 有效的5-脂氧合酶抑制化合物的前药包括其中A为亚烷基或亚烯基的式（IMAGE）化合物，X为氧，硫，亚砜基或取代的氮，Y为包括取代或未取代的基团 碳环或取代或未取代的杂环芳基。 R 1是烷基，烯基，氨基，烷基氨基，二烷基氨基或羟基氨基或具有代谢可切割离去基团的胺基。 M是氢，药学上可接受的阳离子或代谢可切割的离去基团，条件是M或R 1必须承载代谢可切割的离去基团。