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    LIPOXYGENASE AND CYCLOOXYGENASE INHIBITING COMPOUNDS
    12.
    发明申请
    LIPOXYGENASE AND CYCLOOXYGENASE INHIBITING COMPOUNDS 审中-公开
    LIPOXYGENASE和CYCLOOXYGENASE抑制化合物

    公开(公告)号：WO1996032377A1

    公开(公告)日：1996-10-17

    申请号：PCT/US1996003907

    申请日：1996-03-22

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  BROOKS, Clint, D., W. ,  STEWART, Andrew, O. ,  BASHA, Anwer ,  BELL, Randy, L.

    IPC: C07C275/64

    CPC classification number: C07D409/12 ,  C07C275/64 ,  C07D307/52 ,  C07D333/20 ,  C07D333/58

    Abstract: Compounds having the structure of general formula (I) or a pharmaceutically acceptable salt thereof have activity as inhibitors of cyclooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B4, C4, D4, and E4 and cyclooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optionally susbtituted carbocyclic aryl, (b) optionally substituted furyl, (c) optionally substituted benzo[b]furyl, (d) optionally substituted thienyl, (e) optionally substituted pyridyloxy, (f) optionally substituted pyridylalkyl, (g) optionally substituted benzo[b]thienyl, (h) optionally substituted pyridyl, (i) optionally substituted quinolyl, and (j) optionally substituted indolyl; X is selected from (a) optionally susbtituted alkyl, (b) optionally substituted alkenyl, and (c) optionally substituted alkynyl; R and R are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z-COOH.

    Abstract translation: 具有通式（I）结构的化合物或其药学上可接受的盐具有作为环加氧酶和5-脂氧合酶抑制剂的活性，降低了白三烯B4，C4，D4和E4以及环氧合酶产物如前列腺素和血栓素的生物合成， 可用于治疗炎症和过敏性疾病状态。 化合物具有上述结构，其中A选自（a）任选取代的碳环芳基，（b）任选取代的呋喃基，（c）任选取代的苯并[b]呋喃基，（d）任选取代的噻吩基，（e） 吡啶基氧基，（f）任选取代的吡啶基烷基，（g）任选取代的苯并[b]噻吩基，（h）任选取代的吡啶基，（i）任选取代的喹啉基，和（j）任选取代的吲哚基; X选自（a）任选的取代的烷基，（b）任选取代的烯基，和（c）任选取代的炔基; R 1和R 2独立地选自氢，羟基和烷基; Z为通式Z-COOH的非甾体抗炎药物的残基。

    IMINOXYCARBOXYLATES AND DERIVATIVES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
    15.
    发明申请
    IMINOXYCARBOXYLATES AND DERIVATIVES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 审中-公开
    作为紫苏酮生物合成酶抑制剂的甲氧基羧酸酯和衍生物

    公开(公告)号：WO1996002507A1

    公开(公告)日：1996-02-01

    申请号：PCT/US1995008367

    申请日：1995-06-28

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  BROOKS, Dee, W. ,  BHATIA, Pramila ,  KOLASA, Teodozyj ,  STEWART, Andrew, O.

    IPC: C07D215/14

    CPC classification number: C07D213/30 ,  C07D215/14 ,  C07D215/227 ,  C07D215/36 ,  C07D235/12 ,  C07D239/26 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D513/04

    Abstract: The present invention relates to a compound of the formula: W-X-Q-Y-CH(R )-O-N=C(R )-A-COM, or a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or heteroaryl; X is a valence bond, or methylene, divalent alkylene, alkenylene, alkynylene or alkyloxy; Q is a valence bond, or -O-, -S-, > NR or > NCOR ; Y is optionally substituted phenyl, biphenyl, naphthyl, tetrahydronaphthyl, indolyl, pyridyl, or benzo[b]thienyl, thienyl, thiazolyl, or thiazolylphenyl; R is alkyl, cycloalkyl, alkoxyalkyl, aryl or arylalkyl, heteroaryl or heteroarylalkyl; R is hydrogen, alkyl or hydroxyalkyl; A is a valence bond or is selected from alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, pyridylene, thienylene and furylene; and M is a pharmaceutically acceptable, metabolically cleavable group, -OR , -NR R , -NH-tetrazoyl, -NH-2-, 3-, or 4-pyridyl, and -NH-2-, 4-, or 5-thiazolyl which inhibit leukotriene biosynthesis and are useful in the treatment of inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting lipoxygenase activity and leukotriene biosynthesis.

    Abstract translation: 本发明涉及下式化合物：W-X-Q-Y-CH（R 1）-O-N = C（R 2）-A-COM或其药学上可接受的盐，其中W为任选取代的芳基或杂芳基; X是价键，或亚甲基，二价亚烷基，亚烯基，亚炔基或烷氧基; Q是价键，或-O - ， - S-，> NR 4或NCOR 5。 Y是任选取代的苯基，联苯基，萘基，四氢萘基，吲哚基，吡啶基或苯并[b]噻吩基，噻吩基，噻唑基或噻唑基苯基; R 1是烷基，环烷基，烷氧基烷基，芳基或芳基烷基，杂芳基或杂芳基烷基; R 2是氢，烷基或羟烷基; A是价键或选自亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚吡啶基，亚噻吩基和亚芳基; 并且M是药学上可接受的代谢可裂解基团-OR 6，-NR 6 R 7，-NH-三唑基，-NH-2-，3-或4-吡啶基和-NH- 抑制白细胞三烯生物合成的2-，4-或5-噻唑基并且可用于治疗炎性疾病状态。 还公开了白三烯生物合成抑制组合物和抑制脂氧合酶活性和白三烯生物合成的方法。

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