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14 条记录 (耗时 0.029 秒)

    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    2.
    发明申请
    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：US20060014725A1

    公开(公告)日：2006-01-19

    申请号：US11158881

    申请日：2005-06-22

    申请人： Scott Mayer ,  Eric Gundersen ,  Hassan Elokdah ,  David Crandall

    发明人： Scott Mayer ,  Eric Gundersen ,  Hassan Elokdah ,  David Crandall

    IPC分类号： A61K31/415 ,  A61K31/404 ,  C07D403/02 ,  C07D209/12

    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 dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
    3.
    发明申请
    Substituted dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
    取代的二氢吡喃并吲哚-3,4-二酮衍生物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂

    公开(公告)号：US20060270728A1

    公开(公告)日：2006-11-30

    申请号：US11446838

    申请日：2006-06-05

    申请人： Hassan Elokdah ,  David Li

    发明人： Hassan Elokdah ,  David Li

    IPC分类号： A61K31/407 ,  A61K31/4439 ,  A61K31/405 ,  C07D491/02 ,  C07D403/02

    CPC分类号： C07D491/04 ,  C07D209/22

    摘要： Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

    摘要翻译： 提供式（I）和II）的化合物，其中：X是碱金属或碱性胺部分; R 1是烷基，环烷基，-CH 2 - 环烷基，吡啶基，-CH 2 - 吡啶基，苯基或苄基，这些环 基团任选被取代; R 2是H，卤素，烷基，全氟烷基，烷氧基，环烷基，-CH 2 2-环烷基，-NH 2 - 或-NO 2 - SUB> 2 R 3是苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，这些基团的环任选被取代; 或其药学上可接受的盐或酯形式，以及使用这些化合物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂的药物组合物和方法，以及用于治疗由纤维蛋白溶解性疾病如深静脉血栓形成和 冠心病和肺纤维化。

    Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor (PAI-1)
    4.
    发明申请
    Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor (PAI-1) 失效

    公开(公告)号：US20060122254A1

    公开(公告)日：2006-06-08

    申请号：US11335233

    申请日：2006-01-19

    申请人： Hassan Elokdah ,  Geraldine McFarlane ,  David Li

    发明人： Hassan Elokdah ,  Geraldine McFarlane ,  David Li

    IPC分类号： A61K31/405 ,  C07D209/18

    CPC分类号： C07D403/06 ,  C07D209/22

    摘要： This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure: wherein: R1 is alkyl or optionally substituted cycloalkyl, —CH2-cycloalkyl, pyridinyl, CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(═O)CH2—, H2NC(═O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(═NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptable salt or ester form thereof.