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    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    2.
    发明授权
    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
    取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂

    公开(公告)号：US07351730B2

    公开(公告)日：2008-04-01

    申请号：US11158881

    申请日：2005-06-22

    申请人： Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah ,  David LeRoy Crandall

    发明人： Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah ,  David LeRoy Crandall

    IPC分类号： A61K31/404 ,  C07D209/04 ,  C07D403/02

    CPC分类号： C07D403/12 ,  C07D209/12

    摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

    摘要翻译： 本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选被R 8取代的芳基，烷酰基，任选被R 8取代的芳酰基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    3.
    发明授权
    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
    取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂

    公开(公告)号：US06800654B2

    公开(公告)日：2004-10-05

    申请号：US10171041

    申请日：2002-06-13

    申请人： Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah ,  David LeRoy Crandall

    发明人： Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah ,  David LeRoy Crandall

    IPC分类号： C07D20904

    CPC分类号： C07D403/12 ,  C07D209/12

    摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

    摘要翻译： 本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4各自为H，烷基，烷酰基，卤素，OH，任选被R 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基， 全氟烷氧基 R5是H，烷基，全氟烷基，任选被R 8取代的芳基，烷酰基，任选被R 8取代的芳酰基; R6是H，烷基，烷芳基，任选被R8，烷酰基取代的苄基，任选被R8取代的芳酰基; R7是H，烷基，烷芳基，任选被R8取代的芳基; n为0-6; A是COOH，或酸性模拟物如四唑，SO 3 H，PO 3 H 2，四氢萘等; R8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    4.
    发明授权
    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
    取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂

    公开(公告)号：US07629377B2

    公开(公告)日：2009-12-08

    申请号：US12026272

    申请日：2008-02-05

    申请人： David LeRoy Crandall ,  Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah

    发明人： David LeRoy Crandall ,  Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah

    IPC分类号： A61K31/404 ,  C07D209/04

    CPC分类号： C07D403/12 ,  C07D209/12

    摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

    摘要翻译： 本发明提供了PAI-1抑制式I化合物：其中：R1，R2，R3和R4分别为H，烷基，烷酰基，卤素，OH，任选被R8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基， 全氟烷氧基 R5是H，烷基，全氟烷基，任选被R 5取代的芳基，烷酰基，任选被R 8取代的芳酰基; R6是H，烷基，烷芳基，任选被R8，烷酰基取代的苄基，任选被R8取代的芳酰基; R7是H，烷基，烷芳基，任选被R8取代的芳基; n为0-6; A是COOH，或酸性模拟物如四唑，SO 3 H，PO 3 H 2，四氢萘等; R8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

    SUBSTITUTED NAPHTHYL INDOLE DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1)
    7.
    发明申请
    SUBSTITUTED NAPHTHYL INDOLE DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1) 失效
    作为PLASMINOGEN激活剂抑制剂类型1（PAI-1）的抑制剂的取代的萘基吲哚衍生物

    公开(公告)号：US20080182883A1

    公开(公告)日：2008-07-31

    申请号：US12026272

    申请日：2008-02-05

    申请人： David LeRoy Crandall ,  Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah

    发明人： David LeRoy Crandall ,  Scott Christian Mayer ,  Eric Gould Gundersen ,  Hassan Mahmoud Elokdah

    IPC分类号： A61K31/41 ,  C07D403/02 ,  A61P7/00 ,  A61P11/00 ,  A61P25/28 ,  A61P35/00

    CPC分类号： C07D403/12 ,  C07D209/12

    摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, , alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, pertluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

    摘要翻译： 本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选地被R 5， - 烷酰基，任选被R 8取代的芳酰基的芳基取代的芳基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。