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    Substituted indoles and their use as integrin antagonists
    1.
    发明申请
    Substituted indoles and their use as integrin antagonists 有权
    取代的吲哚及其作为整联蛋白拮抗剂的用途

    公开(公告)号：US20020169200A1

    公开(公告)日：2002-11-14

    申请号：US10058215

    申请日：2002-01-29

    申请人： 3-Dimensional Pharmaceuticals, Inc.

    发明人： Tianbao Lu ,  Louis V. LaFrance ,  Thomas P. Markotan ,  Juan Jose Marugan ,  Victor J. Marder ,  David C. U'Prichard ,  Beth M. Anaclerio ,  Zihong Guo ,  Wenxi Pan ,  Kristi A. Leonard

    IPC分类号： A61K031/405 ,  C07D209/04

    CPC分类号： C07D213/74 ,  C07D209/08 ,  C07D401/12 ,  C07D401/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/14

    摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (nullv) integrins, for example nullvnull3 and nullvnull5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by nullvnull3 and nullvnull5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: 1 where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.

    摘要翻译： 本发明涉及作为αV（alphav）整联蛋白的拮抗剂的新型取代的吲哚化合物，例如阿尔法博3和阿尔法肽5整联蛋白，其药学上可接受的盐及其药物组合物。 这些化合物可以用于治疗由α1和α2融合蛋白介导的病理状态，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。 化合物具有以下通式：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，D，X，W，a，m，n， j，k和v在本文中定义。

    Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
    2.
    发明申请
    Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists 有权
    取代的苯并呋喃和苯并噻吩，其制备方法和用作整联蛋白拮抗剂的方法

    公开(公告)号：US20030018064A1

    公开(公告)日：2003-01-23

    申请号：US10132706

    申请日：2002-04-26

    申请人： 3-Dimensional Pharmaceuticals, Inc.

    发明人： Beth M. Anaclerio ,  Juan Jose Marugan Sanchez ,  Victor J. Marder ,  David C. U'Prichard

    IPC分类号： C07D333/52 ,  A61K031/44 ,  C07D307/87

    CPC分类号： C07D405/12 ,  C07D409/12

    摘要： The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (nullv) integrins, for example nullvnull3 and nullvnull5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by nullvnull3 and nullvnull5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: 1 where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.

    摘要翻译： 本发明涉及作为αV（alphav）整联蛋白的拮抗剂的新型取代的苯并呋喃和苯并噻吩类化合物，例如阿尔法博3和阿夫泊亭5整联蛋白，其药学上可接受的盐及其药物组合物。 这些化合物可以用于治疗由α1和α2融合蛋白介导的病理状态，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。 化合物具有通式I：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，m，n，i，j和k在本文中定义。