N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds
having lipoxygenase inhibitory activity
    4.
    发明授权
    N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
    N-取代呋喃基异羟肟酸和具有脂氧合酶抑制活性的N-羟基脲化合物

    公开(公告)号:US5169854A

    公开(公告)日:1992-12-08

    申请号:US841968

    申请日:1992-02-26

    摘要: Compounds useful in inhibiting the biosynthesis of leukotrienes have the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group, R.sup.4 is alkyl, cycloalkyl or --NR.sup.5 R.sup.6, where R.sup.5 and R.sup.6 are hydrogen, alkyl, cycloalkyl or alkanoyl, where A is a valence bond or is a straight or branched divalent alkylene group of from one to twelve carbon atoms, R.sup.2 and R.sup.3 are independently selected from hydrogen, straight or branched alkyl of from one to twelve carbon atoms, halogen, or trifluoroalkyl, and R.sup.1 is selected from phenoxy, phenylthio, 2-, 3-, or 4-pyridyloxy, 1 or 2-naphthyloxy, or 2,4,5, or 8-quinolyloxy, all optionally substituted with alkyl, haloalkyl, alkoxy, hydroxy or halogen.

    摘要翻译: 可用于抑制白细胞三烯生物合成的化合物具有其中M是氢,药学上可接受的阳离子或代谢可裂解基团的结构,R 4是烷基,环烷基或-NR 5 R 6,其中R 5和R 6是氢,烷基,环烷基或 烷酰基,其中A是价键或是具有1至12个碳原子的直链或支链二价亚烷基,R 2和R 3独立地选自氢,具有1至12个碳原子的直链或支链烷基,卤素或三氟烷基 ,R1选自苯氧基,苯硫基,2-,3-或4-吡啶氧基,1或2-萘氧基或2,4,5或8-喹啉氧基,全部任选被烷基,卤代烷基,烷氧基,羟基 或卤素。

    O-substituted N-hydroxyurea derivatives
    6.
    发明授权
    O-substituted N-hydroxyurea derivatives 失效
    O-取代的N-羟基脲衍生物

    公开(公告)号:US5292900A

    公开(公告)日:1994-03-08

    申请号:US992389

    申请日:1992-12-18

    摘要: The present invention provides compounds useful as intermediates for the preparation of 5-lipoxygenase inhibiting compounds. The intermediates of this invention have the structure ##STR1## wherein R.sup.1 is an O-protecting group selected from the group consisting of ##STR2## In the above, X is oxygen or sulfur.

    摘要翻译: 本发明提供了可用作制备5-脂氧合酶抑制化合物的中间体的化合物。 本发明的中间体具有结构(*化学结构*),其中R1是选自(*化学结构*)(*化学结构*)的O-保护基。在上述中,X是氧或硫。

    Pyrimido-pyrimidine lipoxygenase inhibiting compounds
    7.
    发明授权
    Pyrimido-pyrimidine lipoxygenase inhibiting compounds 失效
    嘧啶 - 嘧啶脂氧合酶抑制化合物

    公开(公告)号:US4963541A

    公开(公告)日:1990-10-16

    申请号:US314008

    申请日:1989-02-22

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: Compounds of the formula: ##STR1## wherein A is selected from NR.sub.1 R.sub.2 and N(OR.sub.6)R.sub.2 ; and B and C are chloro when A is N(OR.sub.6)R.sub.2 or are independently selected from NHR.sub.3 and NR.sub.4 R.sub.5 where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of alkyl, cycloalkyl and alkylaryl each of which may be unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxy, OR, NRR, OCOR, OCONRR, NRCOR and NRCONRR where R is selected from the group consisting of hydrogen, alkyl, aryl, alkylaryl, alkoxy and hydroxy or R.sub.1 and R.sub.2 or R.sub.4 and R.sub.5 together can form a heteroaryl group and R.sub.6 is a member selected from the group consisting of hydrogen, alkyl, alkylaryl and trialkylsilyl; and the pharmaceutically acceptable salts thereof.These compounds are useful as inhibitors of lipoxygenase enzymes.

    摘要翻译: 下式的化合物:其中A选自NR1R2和N(OR6)R2; 当A为N(OR 6)R 2时,B和C为氯,或独立地选自NHR 3和NR 4 R 5,其中R 1,R 2,R 3,R 4和R 5独立地选自烷基,环烷基和烷芳基,其各自可以是 未取代或被一个或多个选自羟基,OR,NRR,OCOR,OCONRR,NRCOR和NRCONRR的取代基取代,其中R选自氢,烷基,芳基,烷基芳基,烷氧基和羟基或R 1和 R2或R4和R5一起可以形成杂芳基,R6是选自氢,烷基,烷基芳基和三烷基甲硅烷基的成员; 及其药学上可接受的盐。 这些化合物可用作脂氧合酶的抑制剂。

    Thiopyrano(2,3,4-c,d) indolyloxime ether alkylcarboxylates
    9.
    发明授权
    Thiopyrano(2,3,4-c,d) indolyloxime ether alkylcarboxylates 失效
    噻哆醇(2,3,4-c,d)吲哚肟醚烷基羧酸盐

    公开(公告)号:US5420282A

    公开(公告)日:1995-05-30

    申请号:US197422

    申请日:1994-02-15

    CPC分类号: C07D495/06

    摘要: Compounds of the structure ##STR1## wherein R.sup.1 is selected from the group consisting of ##STR2## are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    摘要翻译: 结构的化合物,其中R1选自是脂氧合酶的有效抑制剂,从而抑制白细胞三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。