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    SYMMETRICAL bis-HETEROARYLMETHOXYPHENYLALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
    1.
    发明申请
    SYMMETRICAL bis-HETEROARYLMETHOXYPHENYLALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 审中-公开
    作为紫苏酮生物合成酶抑制剂的对称双 - 二叔丁氧基苯甲醛羧酸酯

    公开(公告)号：WO1997012867A1

    公开(公告)日：1997-04-10

    申请号：PCT/US1996015345

    申请日：1996-09-25

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  BROOKS, Clint, D., W. ,  BHATIA, Pramila ,  KOLASA, Theodozyj ,  STEWART, Andrew, O. ,  GUNN, David, E. ,  CRAIG, Richard, A.

    IPC: C07D215/14

    CPC classification number: C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D241/42 ,  C07D277/64

    Abstract: Compounds having formula (I), wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R and R are independently selected from hydrogen, alkyl, haloalkyl, alkoxy, halogen; R is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH=N-O-A-COM, (c) CH2-O-N=A-COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) -OR , (c) -NR R , (d) -NR SO2R , (e) -NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.

    Abstract translation: 具有式（I）的化合物，其中W在每次出现时相同，并且选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基， 噻唑基; R 1和R 2独立地选自氢，烷基，卤代烷基，烷氧基，卤素; R 3是价键或选自氢和烷基; X是价键或选自亚烷基，烯基和亚炔基; 并且Z选自（a）COM，（b）CH = NOA-COM，（c）CH2-ON = A-COM其中A选自亚烷基和亚环烷基，M选自（a）药学上可接受的代谢 可裂解基团，（b）-OR 6，（c）-NR 7 R 8，（d）-NR 6 SO 2 R 9，（e）-NH-四唑基和（f） 甘氨酰抑制白三烯生物合成，可用于治疗过敏性和炎性疾病状态。 还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。

    ARYLALKYLETHER AND ARYLALKYLTHIOETHER INHIBITORS OF LIPOXYGENASE ENZYME ACTIVITY
    5.
    发明申请
    ARYLALKYLETHER AND ARYLALKYLTHIOETHER INHIBITORS OF LIPOXYGENASE ENZYME ACTIVITY 审中-公开
    LYYXYGENASE酶活性的ARYLALKYLETHER和ARYLALKYLTHIOETHER抑制剂

    公开(公告)号：WO1993003719A1

    公开(公告)日：1993-03-04

    申请号：PCT/US1992006567

    申请日：1992-08-06

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  BROOKS, Dee, W. ,  STEWART, Andrew, O. ,  MARTIN, Jonathan, G.

    IPC: A61K31/34

    CPC classification number: C07D307/42 ,  C07D307/38 ,  C07D333/16 ,  C07D333/34 ,  C07D333/56 ,  C07D495/04

    Abstract: The present invention provides compounds having the structure Y-Het-[Q1]-X-[Q2]-Z which inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B4, C4, D4, and E4. In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl. Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl, alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: -CRROR, -NRC(O)R, -NRC(O)OR, and -C(O)NRR. The group Q1 is absent or is divalent alkylene of from one to six carbon atoms, and Q2 is divalent alkylene from two to ten carbon atoms. The group Z is N(OR1)COR2 where R1 is selected from hydrogen or a pharmaceutically suitable salt. R2 is selected from hydrogen; alkyl; cycloalkyl; amino; alkylamino, optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; dialkylamino in which the alkyl groups are independently optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; cycloalkylamino; 2-hydroxyethylamino; N-morpholino; N-thiomorpholino; N-piperazino; N'-alkyl-N-piperazino and cyclopropylmethylamino.

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