Cyclopeptide derivatives with anti-integrin activity
    13.
    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

    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。

    7-imino derivatives of camptothecin having antitumor activity
    16.
    发明授权
    7-imino derivatives of camptothecin having antitumor activity 有权
    具有抗肿瘤活性的喜树碱的7-亚氨基衍生物

    公开(公告)号:US07351714B2

    公开(公告)日:2008-04-01

    申请号:US10546211

    申请日:2004-03-10

    IPC分类号: A61K31/4745 C07D491/22

    CPC分类号: C07D491/22

    摘要: Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index.Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.

    摘要翻译: 公开了式(I)的喜树碱喜树碱衍生物,其中基团R 1,R 2和R 3 3如说明书中所定义。 式(I)化合物具有抗肿瘤活性,显示出良好的治疗指标。 还公开了制备式(I)化合物及其在制备用于治疗肿瘤,病毒感染和恶性疟原虫药物中的用途的方法。

    7-Imino derivatives of camptothecin having antitumor activity
    17.
    发明申请
    7-Imino derivatives of camptothecin having antitumor activity 有权
    具有抗肿瘤活性的喜树碱的7-亚氨基衍生物

    公开(公告)号:US20060167033A1

    公开(公告)日:2006-07-27

    申请号:US10546211

    申请日:2004-03-10

    IPC分类号: A61K31/4745 C07D519/04

    CPC分类号: C07D491/22

    摘要: Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.

    摘要翻译: 公开了式(I)的喜树碱喜树碱衍生物,其中基团R 1,R 2和R 3 3如说明书中所定义。 式(I)化合物具有抗肿瘤活性,显示出良好的治疗指标。 还公开了制备式(I)化合物及其在制备用于治疗肿瘤,病毒感染和恶性疟原虫药物中的用途的方法。