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    Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
    3.
    发明授权
    Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效

    公开(公告)号：US07056943B2

    公开(公告)日：2006-06-06

    申请号：US10731074

    申请日：2003-12-09

    申请人： Hassan Mahmoud Elokdah ,  Geraldine Ruth McFarlane ,  David Zenan Li

    发明人： Hassan Mahmoud Elokdah ,  Geraldine Ruth McFarlane ,  David Zenan Li

    IPC分类号： A61K43/38 ,  C07D209/90

    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.

    SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1)
    5.
    发明申请
    SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 审中-公开
    作为PLASMINOGEN ACTIVATOR INHIBITOR-1（PAI-1）的抑制剂的取代的吲哚酸衍生物

    公开(公告)号：US20080214647A1

    公开(公告)日：2008-09-04

    申请号：US12098916

    申请日：2008-04-07

    申请人： Hassan Mahmoud Elokdah ,  Geraldine Ruth McFarlane ,  David Zenan Li ,  Lee D. Jennings ,  David LeRoy Crandall

    发明人： Hassan Mahmoud Elokdah ,  Geraldine Ruth McFarlane ,  David Zenan Li ,  Lee D. Jennings ,  David LeRoy Crandall

    IPC分类号： A61K31/403 ,  A61P7/04

    CPC分类号： C07D209/12

    摘要： This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2— cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the 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： 本发明提供下式的化合物：其中：X为化学键，-CH 2 - 或-C（O） - ; 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; R 2是H，烷基，环烷基，-CH 2 - 环烷基或全氟烷基; R 3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 3， SUB> 2 R 4是任选取代的苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，或其盐或酯形式，以及使用该化合物的方法 作为纤维蛋白溶酶原激活物抑制剂-1（PAI-1）的抑制剂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引起的病症和肺纤维化的治疗组合物。

    Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
    7.
    发明申请
    Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
    取代的吲哚酸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：US20060167059A1

    公开(公告)日：2006-07-27

    申请号：US11391893

    申请日：2006-03-29

    申请人： Hassan Mahmoud Elokdah ,  Geraldine Ruth McFarlane ,  David Zenan Li ,  Lee Jennings ,  David LeRoy Crandall

    发明人： Hassan Mahmoud Elokdah ,  Geraldine Ruth McFarlane ,  David Zenan Li ,  Lee Jennings ,  David LeRoy Crandall

    IPC分类号： A61K31/4439 ,  A61K31/405 ,  C07D403/02 ,  C07D209/18

    CPC分类号： C07D209/12

    摘要： This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the 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： 本发明提供下式的化合物：其中：X为化学键，-CH 2 - 或-C（O） - ; 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; R 2是H，烷基，环烷基，-CH 2 - 环烷基或全氟烷基; R 3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 3， SUB> 2 R 4是任选取代的苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，或其盐或酯形式，以及使用该化合物的方法 作为纤维蛋白溶酶原激活物抑制剂-1（PAI-1）的抑制剂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引起的病症和肺纤维化的治疗组合物。