公开(公告)号：US20070213353A1

公开(公告)日：2007-09-13

申请号：US11783495

申请日：2007-04-10

申请人： Mauro Marzi ,  Domenico Alloatti ,  Claudio Pisano ,  Maria Tinti ,  Loredana Vesci ,  Franco Zunino

发明人： Mauro Marzi ,  Domenico Alloatti ,  Claudio Pisano ,  Maria Tinti ,  Loredana Vesci ,  Franco Zunino

IPC分类号： A61K31/4745 ,  C07D491/14

CPC分类号： C07D491/22

摘要： Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.

摘要翻译： 描述了式（I）化合物：其中基团如下文所述的定义，外消旋混合物，其各自的对映异构体，其各自的非对映异构体，它们的混合物及其药学上可接受的盐。 所述化合物是拓扑异构酶I抑制剂。

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。