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1. 发明申请

WO2006020979A2 FACTOR VII CONJUGATES FOR SELECTIVELY TREATING NEOVASCULARIZATION DISORDERS 审中-公开
标题翻译：因子VII共轭选择性治疗新生血管性疾病
公开(公告)号：WO2006020979A2
公开(公告)日：2006-02-23
申请号：PCT/US2005/029017
申请日：2005-08-15
申请人： YALE UNIVERSITY , GAREN, Alan , ADELMAN, Ron, A. , HU, Zhiwei
发明人： GAREN, Alan , ADELMAN, Ron, A. , HU, Zhiwei
IPC分类号： A61K41/00 , A61P19/08 , A61P29/00 , A61P35/00 , A61P27/00
CPC分类号： A61K38/41 , A61K41/0071 , A61K47/64
摘要： Methods and compositions are provided for the treatment of diseases such as exudative macular degeneration, diabetic retinopathy, retinopathy of prematurity, choroidal neovascularization, retinal neovascularization, iris neovascularization, corneal neovascularization, ocular tumors, and other disorders of the eye, cancer, and inflammatory disorders. The method involves administering a conjugate, referred to as fVIIPD, containing a photosensitizer and a targeting molecule such as factor VII ("fVII"), fVIIa, or modified fVII, which binds with high affinity and specificity to tissue factor (TF). TF is more highly expressed, abnormally expressed or specifically expressed on endothelial cells lining the luminal surface of pathological neovasculature, than on normal vasculature, thus providing a specific and accessible therapeutic target. Following administration of fVIIPD, the compound specifically binds to the pathological neovasculature of the eye by interaction of the targeting molecule with TF expressed by endothelial cells within abnormal blood vessels. The photosensitizer may then be activated with a non-thermal laser light for selective destruction of abnormal vasculature.
摘要翻译：提供了用于治疗诸如渗出性黄斑变性，糖尿病性视网膜病，早产儿视网膜病，脉络膜新血管生成，视网膜新血管生成，虹膜新血管生成，角膜新血管生成，眼部肿瘤和其他病症的方法和组合物，眼睛，癌症和炎症性疾病。该方法包括施用含有光敏剂和靶向分子（例如因子VII（“fVII”），fVIIa或修饰的fVII）的结合物（称为fVIIPD），其以高亲和力和特异性与组织因子（TF）结合。 TF在病理性新血管系统的管腔表面上的内皮细胞上比在正常脉管系统中更高度表达，异常表达或特异性表达，从而提供特异性和可接近的治疗靶标。施用fVIIPD后，化合物通过靶向分子与异常血管内的内皮细胞表达的TF的相互作用特异性结合眼睛的病理性新血管系统。然后可以用非热激光激活光敏剂以选择性破坏异常脉管系统。

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