利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

14 条记录 (耗时 0.029 秒)

    Ether-containing inhibitors of 5-lipoxygenase
    3.
    发明授权
    Ether-containing inhibitors of 5-lipoxygenase 失效
    含醚的5-脂氧合酶抑制剂

    公开(公告)号：US5350765A

    公开(公告)日：1994-09-27

    申请号：US113942

    申请日：1993-08-30

    申请人： Joseph F. Dellaria ,  Jimmie L. Moore ,  Dee W. Brooks

    发明人： Joseph F. Dellaria ,  Jimmie L. Moore ,  Dee W. Brooks

    IPC分类号： C07D309/10 ,  C07D405/12 ,  A61K31/35 ,  C07D309/02

    CPC分类号： C07D405/12 ,  C07D309/10

    摘要： Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl 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： 其中Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物 并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基或苯并[b]噻吩基，A1是丙炔基，亚甲基或与X的直接连接，X是氧基，硫代，磺酰基， 或NR4，A2选自 ，其中Y是氢，卤素或腈; Z是氢，R1是烷基，R2是氢或烷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
    4.
    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.

    Cycloalkyl N-hydroxy derivatives having lipoxygenase inhibitory activity
    5.
    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。

    Ether-containing inhibitors of 5-lipoxygenase
    6.
    发明授权
    Ether-containing inhibitors of 5-lipoxygenase 失效
    含醚的5-脂氧合酶抑制剂

    公开(公告)号：US5268379A

    公开(公告)日：1993-12-07

    申请号：US935079

    申请日：1992-08-24

    申请人： Joseph F. Dellaria ,  Jimmie L. Moore ,  Dee W. Brooks

    发明人： Joseph F. Dellaria ,  Jimmie L. Moore ,  Dee W. Brooks

    IPC分类号： C07D309/10 ,  C07D405/12 ,  A61K31/47

    CPC分类号： C07D405/12 ,  C07D309/10

    摘要： Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl 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： 其中Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物 并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基或苯并[b]噻吩基，A1是丙炔基，亚甲基或与X的直接连接，X是氧基，硫代，磺酰基， 或NR4，A2选自 ，其中Y是氢，卤素或腈; Z是氢，R1是烷基，R2是氢或烷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。