公开(公告)号：US20080021088A1

公开(公告)日：2008-01-24

申请号：US11765737

申请日：2007-06-20

申请人： Sabrina Dallavalle ,  Lucio Merlini ,  Claudio Pisano ,  Loredana Vesci ,  Giuseppe Giannini ,  Sergio Penco

发明人： Sabrina Dallavalle ,  Lucio Merlini ,  Claudio Pisano ,  Loredana Vesci ,  Giuseppe Giannini ,  Sergio Penco

IPC分类号： A61K31/40 ,  A61K31/19 ,  A61P35/04 ,  C07D205/00 ,  C07D307/00 ,  C07C63/00 ,  A61K31/36

CPC分类号： C07D209/48 ,  C07C59/54 ,  C07C59/72 ,  C07C62/32 ,  C07C69/732 ,  C07C69/734 ,  C07C229/34 ,  C07C2601/14 ,  C07C2603/74 ,  C07D317/50 ,  C07F7/1804

摘要： Described and claimed are compounds of Formula (I) in which R, R′, R″, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterized by altered angiogenesis and as antitumorals.

摘要翻译： 描述和要求保护的是式（I）的化合物，其中R，R'，R“，A和D具有本文中所述的含义，作为治疗以血管生成改变为特征的病态的有用试剂和抗肿瘤剂。

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。