embedded imagewherein: 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."/> Substituted dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
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Substituted dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)

机译:取代的二氢吡喃基吲哚-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

摘要

Compounds of formula (I) and II) are provided embedded imagewherein: 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.
机译:提供了式(I)和II)的化合物 <图像alt =“嵌入式图像” file =“ US20050113436A1-20050526-C00001.GIF” he =“ 62.57mm” imgContent =“ chem” imgFormat =“ GIF” wi =“ 57.40mm“ /> 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,它们的环任选被取代的基团; R 2 是H,卤素,烷基,全氟烷基,烷氧基,环烷基,-CH 2 -环烷基,-NH 2 或-NO < Sub> 2 ; R 3 是苯基,苄基,苄氧基,吡啶基或-CH 2 -吡啶基,这些基团的环是任选取代的;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)的抑制剂以及作为治疗由纤溶障碍引起的疾病(例如深静脉血栓形成和冠心病和肺纤维化。

著录项

  • 公开/公告号US2005113436A1

    专利类型

  • 公开/公告日2005-05-26

    原文格式PDF

  • 申请/专利权人 HASSAN M. ELOKDAH;DAVID ZENAN LI;

    申请/专利号US20030731290

  • 发明设计人 HASSAN M. ELOKDAH;DAVID ZENAN LI;

    申请日2003-12-09

  • 分类号A61K31/4439;A61K31/407;A61K31/405;C07D491/02;C07D43/02;

  • 国家 US

  • 入库时间 2022-08-21 22:24:37

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