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    Cyclopeptide derivatives with anti-integrin activity
    7.
    发明申请
    Cyclopeptide derivatives with anti-integrin activity 审中-公开
    具有抗整联蛋白活性的环肽衍生物

    公开(公告)号：US20070178045A1

    公开(公告)日：2007-08-02

    申请号：US11596190

    申请日：2005-05-04

    申请人： Claudio Pisano ,  Giuseppe Giannini ,  Maria Omelia Tinti ,  Loredana Vesci ,  Sergio Penco ,  Alma Dal Pozzo ,  Ni Minghong

    发明人： Claudio Pisano ,  Giuseppe Giannini ,  Maria Omelia Tinti ,  Loredana Vesci ,  Sergio Penco ,  Alma Dal Pozzo ,  Ni Minghong

    IPC分类号： A61K38/12 ,  A61K103/32 ,  A61K51/08

    CPC分类号： C07K5/12 ,  A61K38/00 ,  C07K7/64

    摘要： Formula (I) compounds are described c(R1-Arg-Gly-Asp-R2) where the meanings of the various groups are as described here below, which are integrin inhibitors, and particularly inhibitors of integrins of the α,β3 and α,β5 family, and therefore are useful as medicaments, particularly for the treatment of the diseases underlying abnormal angiogenesis, such as retinopathy, acute renal failure, osteoporosis and metastases. The compounds described herein, when suitably labelled, are also useful as diagnostic agents, especially for the detection of small tumour masses and arterial occlusion events, and as targeted drug vectors.

    摘要翻译： 式（I）化合物描述为其中各种基团的含义如下所述的c（R 1 -Arg-Gly-Asp-R 2） 整合素抑制剂，特别是α，β3和α，β5家族的整联蛋白的抑制剂，因此可用作药物，特别是用于治疗潜在的疾病 异常血管发生，如视网膜病变，急性肾衰竭，骨质疏松症和转移。 本文所述的化合物在适当标记时也可用作诊断剂，特别是用于检测小肿瘤块和动脉闭塞事件以及作为靶向药物载体。

    Fluoro-alkyl-cyclopeptide derivatives having anti-integrin activity
    8.
    发明申请
    Fluoro-alkyl-cyclopeptide derivatives having anti-integrin activity 审中-公开
    具有抗整联蛋白活性的氟 - 烷基 - 环肽衍生物

    公开(公告)号：US20060205637A1

    公开(公告)日：2006-09-14

    申请号：US10522268

    申请日：2003-07-18

    申请人： Alma Dal Pozzo ,  Giuseppe Giannini ,  Claudio Pisano

    发明人： Alma Dal Pozzo ,  Giuseppe Giannini ,  Claudio Pisano

    IPC分类号： A61K38/12 ,  C07K5/12

    CPC分类号： C07K7/54 ,  A61K38/00 ,  C07K7/64

    摘要： Compounds of formula (I) cyclo [NX1-R1-CO—NX2-R2-CO—NX3-R3-CO—NX4-CO—NX5-R5-CO], wherein at least one x-fluoroalkylated amino acid is present, are inhibitors of integrins, particularly those belonging to the alphavbeta3 and alphavbeta5 family, and thus are useful as medicaments, particularly for the treatment of the underlying diseases responsible for abnormal angiogenesis, such as retinopathy, acute kidney failure, osteoporosis and metastases. The compounds described herein are also useful as diagnostic agents, when appropriately labelled, especially for the detection and location of small tumour masses and arterial occlusion events.

    摘要翻译： 式（I）环[NX1-R1-CO-NX2-R2-CO-NX3-R3-CO-NX4-CO-NX5-R5-CO]的化合物，其中存在至少一个x-氟烷基化氨基酸 整合素的抑制剂，特别是属于alphavbeta3和alphavbeta5家族的那些，因此可用作药物，特别是用于治疗负责异常血管生成的潜在疾病，例如视网膜病变，急性肾功能衰竭，骨质疏松症和转移。 当适当标记时，本文所述的化合物还可用作诊断剂，特别是用于小肿瘤块和动脉闭塞事件的检测和定位。