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    Cycloalkyl N-hydroxy derivatives having lipoxygenase inhibitory activity
    2.
    发明授权
    Cycloalkyl N-hydroxy derivatives having lipoxygenase inhibitory activity 失效
    具有脂氧合酶抑制活性的环烷基N-羟基衍生物

    公开(公告)号：US5326787A

    公开(公告)日：1994-07-05

    申请号：US111764

    申请日：1993-08-25

    申请人： Dee W. Brooks ,  Jimmie L. Moore ,  Karen E. Rodriques

    发明人： Dee W. Brooks ,  Jimmie L. Moore ,  Karen E. Rodriques

    IPC分类号： C07C275/64 ,  A01N55/02

    CPC分类号： C07C275/64

    摘要： Compounds of the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation or metabolically cleavable group, R is alkyl, cycloalkyl, or NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl alkonyl, or carbocyclic aryl, Y is alkylene, alkenylene, or cyclopropyl, and A is optionally substituted cycloalkyl or cycloalkylene 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M是氢，药学上可接受的阳离子或代谢可裂解基团，R是烷基，环烷基或NR 1 R 2，其中R 1和R 2是氢，烷基，环烷基烷基或碳环芳基，Y是亚烷基， 亚烯基或环丙基，A是任选取代的环烷基或环亚烷基是脂氧合酶的有效抑制剂，因此抑制白三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。

    Indole carboxylate derivatives which inhibit leukotriene biosynthesis
    3.
    发明授权
    Indole carboxylate derivatives which inhibit leukotriene biosynthesis 失效
    抑制白细胞三烯生物合成的吲哚羧酸衍生物

    公开(公告)号：US5288743A

    公开(公告)日：1994-02-22

    申请号：US979138

    申请日：1992-11-20

    申请人： Dee W. Brooks ,  Keith W. Woods ,  Karen E. Rodriques

    发明人： Dee W. Brooks ,  Keith W. Woods ,  Karen E. Rodriques

    IPC分类号： C07D209/30 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/405 ,  C07D277/04

    CPC分类号： C07D401/12 ,  C07D209/30 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

    摘要： Compounds of the structure ##STR1## where A is straight or branched divalent alkylene or divalent cycloalkylene, R.sub.1 is selected from hydrogen; alkylthio; optionally substituted phenylthio; optionally substituted phenylalkylthio; optionally substituted 2-, 3-, and 4-pyridyl; optionally substituted 2-, and 3-thienylthio; and optionally substituted 2-thiazolythio, R.sub.2 is selected from --COOB; --COOalkyl; --COOalkyl(carbocyclic aryl); --CONR.sub.5 R.sub.6 ; --COR.sub.6 ; and --OH, R.sub.3 is selected from phenylalkyl and heteroarylalkyl, and R.sub.4 is selected from optionally substituted alkoxy(carbocyclic aryl); optionally substituted carbocyclic aryloxy; optionally substituted heteroarylalkoxy; and optionally substituted heteroaryloxy are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    摘要翻译： 其中A是直链或支链二价亚烷基或二价亚环烷基的结构化合物，其中A选自氢; 烷硫基 任选取代的苯硫基; 任选取代的苯基烷硫基; 任选取代的2-，3-和4-吡啶基; 任选取代的2-和3-噻吩基硫基; 和任选取代的2-噻唑硫基，R2选自-COOB; -COO烷基; -COO烷基（碳环芳基）; -CONR5R6; -COR6; 和-OH，R 3选自苯基烷基和杂芳基烷基，并且R 4选自任选取代的烷氧基（碳环芳基）; 任选取代的碳环芳氧基; 任选取代的杂芳基烷氧基; 和任选取代的杂芳氧基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。

    Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors
    10.
    发明授权
    Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors 失效

    公开(公告)号：US4992464A

    公开(公告)日：1991-02-12

    申请号：US430710

    申请日：1989-11-01

    申请人： Dee W. Brooks ,  James B. Summers ,  Karen E. Rodriques ,  Robert G. Maki ,  Joseph F. Dellaria ,  James H. Holms ,  Jimmie L. Moore

    发明人： Dee W. Brooks ,  James B. Summers ,  Karen E. Rodriques ,  Robert G. Maki ,  Joseph F. Dellaria ,  James H. Holms ,  Jimmie L. Moore

    IPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58 ,  A61K31/38 ,  C07D333/56

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

    摘要： Compounds, compositions a method of inhibiting lipoxygenase and treating related disorders are disclosed. The compounds are of the formula:Ar-A(R.sub.2).sub.n -N(OM)-CZ-R.sub.1whereinAr is ##STR1## where X is O, S, SO.sub.2 or NR.sub.3 ;R.sub.3 is hydrogen, alkyl, alkylaryl, alkoyl, alkylakoyl, aroyl or alkylaroyl;Y is hydrogen, halogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH).sub.2, --SO.sub.2 R, --SO.sub.2 N(R).sub.2, --O(CH.sub.2).sub.p OR, --CN, --NO.sub.2, --O(CH).sub.p O(CH.sub.2).sub.p OR or --CF.sub.3 ;R is hydrogen, hydroxyl, alkyl, alkylaryl or aryl;m is 0 to 5;p is 1 to 4;A is C.sub.1 -C.sub.12 alkylene or C.sub.2 -C.sub.14 alkenylene;R.sub.2 is --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH.sub.2).sub.y CON(R).sub.2, --O(CH.sub.2).sup.y OR, --CN, --NO.sub.2, 1-tetrazolo, C.sub.4 -C.sub.8 cyclic amido, imidazolo, --O(CH.sub.2).sub.y O(CH.sub.2).sub.y OR, --CF.sub.3, --N(R) COCHR--NH(R), CONHCH(R)CO.sub.2 R, --OCOCHR-NH(R), --CR(NHR)CONR, --CR(NHR)COR, morpholino, --NH(CH.sub.2).sub.y OH, --N[(CH.sub.2).sub.y OH].sub.2, --N.sub.3, --SO.sub.2 N(R).sub.2, --N(R)COR, --N(R)COOR, --N(R)CON(R).sub.2, --C(.dbd.NOH)NHOH or --C(.dbd.NOH)NH.sub.2 where R is as defined above, y is 1 to 4 and --N(R).sub.2 can form a heterocyclic ring of 5-8 atoms;M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable group;Z is oxygen or sulfur; andR.sub.1 us hydrogen, alkyl, alkenyl, --NR.sub.4 R.sub.5, --NCOR.sub.6 or --Q--(R.sub.2).sub.2 where R.sub.4 and R.sub.5 independently selected from the group consisting of hydrogen, hydroxyl, alkyl, substituted alkyl with 1-3 substituents selected from the group consisting of R.sub.2 as defined above, acyl, aryl and CON(R).sub.2 is as defined above, R.sub.6 is hydrogen alkyl, alkylaryl, aryl or NR.sub.4 R.sub.5 where R.sub.4 and R.sub.5 are as defined above and where NR.sub.4 R.sub.5 can form a heterocyclic ring of a 5-8 atoms, Q is alkyl, alkenyl or aryl and z is 0 to 3; provided when n is O, R.sub.1 is not hydrogen, alkyl, alkenyl, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as defined above; and the pharmaceutically acceptable salts thereof.