Heparanases and Splice Variants Thereof, Ponucleotides Encoding Them and Uses Thereof
    22.
    发明申请
    Heparanases and Splice Variants Thereof, Ponucleotides Encoding Them and Uses Thereof 有权
    肝素酶和接头变体,编码它们的用途及其用途

    公开(公告)号:US20080248020A1

    公开(公告)日:2008-10-09

    申请号:US12067498

    申请日:2006-09-20

    摘要: The invention relates to novel heparanases, heparanase splice variants, and to polynucleotides encoding them. Particularly, the invention relates to Spalax heparanases, and to Spalax and human heparanase splice variants. Heparanase splice variants can be used, for example, to modulate the activity of heparanase in diseases disorders or conditions caused by or associated with the enzymatic activity of heparanase. For instance, a splice variant capable of down regulating the activity of heparanase can be used to treat primary tumors and/or to prevent or treat metastasis.

    摘要翻译: 本发明涉及新型肝素酶,乙酰肝素酶剪接变体和编码它们的多核苷酸。 特别地,本发明涉及Spalax肝素酶,以及Spalax和人肝素酶剪接变体。 肝素酶剪接变体可用于例如调节乙酰肝素酶在由乙酰肝素酶的酶活性引起或与之相关的疾病疾病或病症中的活性。 例如,能够下调肝素酶活性的剪接变体可用于治疗原发性肿瘤和/或预防或治疗转移。

    Inhibition of pathogenic processes related to tissue trauma
    23.
    发明申请
    Inhibition of pathogenic processes related to tissue trauma 审中-公开
    抑制与组织创伤相关的致病过程

    公开(公告)号:US20070010538A1

    公开(公告)日:2007-01-11

    申请号:US11402638

    申请日:2006-04-11

    IPC分类号: A61K31/517

    CPC分类号: A61K31/517

    摘要: According to the present invention compositions and methods are provided to prevent the pathogenic aspects of tissue trauma while preserving normal tissue repair mechanisms, based on the fact that these molecules abrogate the cascade of damage initiated by tissue trauma, while maintaining this the requisite healthy extracellular matrix economy. The composition for regulating the extracellular matrix economy, comprise a pharmaceutically effective amount of an effector in combination with a pharmaceutically acceptable carrier. Preferably, the effector is a quinazolinone derivative. More preferably, the quinazolinone derivative is a member of a group having formula (I), wherein R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, and R3 is a member of the group consisting of hydrogen and lower alkenoxy; and pharmaceutically acceptable salts thereof; and n is either 1 or 2. Most preferably, the effector is Halofuginone and pharmaceutically acceptable salts thereof.

    摘要翻译: 根据本发明,提供了组合物和方法,以防止组织创伤的病态方面,同时保持正常组织修复机制,这是基于这些分子消除由组织创伤引起的损伤级联的事实,同时保持必需的健康细胞外基质 经济。 用于调节细胞外基质经济性的组合物包含与药学上可接受的载体组合的药学有效量的效应物。 优选地,效应子是喹唑啉酮衍生物。 更优选地,喹唑啉酮衍生物是具有式(I)的基团的成员,其中R 1是由氢,卤素,硝基,苯并,低级烷基,苯基和 低级烷氧基 R 2是由羟基,乙酰氧基和低级烷氧基组成的组中的成员,R 3 3是氢和低级链烯氧基的成员; 及其药学上可接受的盐; 并且n为1或2.最优选地,效应物是卤代酮及其药学上可接受的盐。

    Angiogenic factor and use thereof in treating cardiovascular disease
    24.
    发明申请
    Angiogenic factor and use thereof in treating cardiovascular disease 审中-公开
    血管生成因子及其在治疗心血管疾病中的应用

    公开(公告)号:US20060084622A1

    公开(公告)日:2006-04-20

    申请号:US11254675

    申请日:2005-10-21

    IPC分类号: A61K48/00

    摘要: The present invention relates to a novel VEGF protein product, and nucleic acid encoding the novel protein product, comprising exons 1-6 and 8 of the VEGF gene, and its use thereof in treating the cardiovascular system and its diseases through effects on anatomy, conduit function, and permeability. VEGF145 has been found to be an active mitogen for vascular endothelial cells and to function as an angiogenic factor in-vivo. VEGF145 has novel properties compared with previously characterized VEGF species with respect to cellular distribution, susceptibility to oxidative damage, and extra-cellular matrix (ECM) binding ability. The present invention provides methods of treating the cardiovascular system, enhancing endothelialization of diseased vessels, and enhancing drug permeation by providing the novel VEGF protein product. The invention also provides expression vectors, compositions, and kits for use in the methods of the invention.

    摘要翻译: 本发明涉及一种新型的VEGF蛋白产物,以及编码新型蛋白质产物的核酸,其包含VEGF基因的外显子1-6和8及其在治疗心血管系统及其疾病中的用途,通过对解剖结构,导管 功能和渗透性。 已经发现VEGF 145是血管内皮细胞的活性丝裂原,并且在体内作为血管生成因子起作用。 相对于细胞分布,对氧化损伤的敏感性和细胞外基质(ECM)结合能力,VEGF 145具有新的特性。 本发明提供了治疗心血管系统,增强患病血管的内皮化,并通过提供新的VEGF蛋白产物增强药物渗透的方法。 本发明还提供用于本发明方法的表达载体,组合物和试剂盒。

    Angiogenic factors and use thereof in treating cardiovascular disease
    27.
    发明授权
    Angiogenic factors and use thereof in treating cardiovascular disease 失效
    血管生成因子及其在治疗心血管疾病中的应用

    公开(公告)号:US06583276B1

    公开(公告)日:2003-06-24

    申请号:US09037983

    申请日:1998-03-11

    IPC分类号: C07H2104

    摘要: The present invention relates to novel VEGF protein products, and nucleic acids encoding these novel protein products, comprising exons 1-6 and 8 of the VEGF gene, and derivatives thereof, and these uses in treating the cardiovascular system and its diseases through effects on anatomy, conduit function, and permeability. VEGF145 and its derivatives have been found to be active mitogens for vascular endothelial cells and to function as angiogenic factors in-vivo. VEGF145 and its derivatives have novel properties compared with previously characterized VEGF species with respect to cellular distribution, susceptibility to oxidative damage, and extra-cellular matrix (ECM) binding ability. The present invention also relates to derivatives of VEGF145 which have altered properties in that they have altered biological activity and altered heparin-binding activity when compared to VEGF145. The present invention provides methods of treating the cardiovascular system, enhancing endothelialization of diseased vessels, and enhancing drug permeation by providing the novel VEGF protein products. The invention also provides expression vectors, compositions, and kits for use in the methods of the invention.

    摘要翻译: 本发明涉及新型VEGF蛋白产物和编码这些新蛋白产物的核酸,其包含VEGF基因的外显子1-6和8及其衍生物,以及这些用于通过解剖学影响治疗心血管系统及其疾病的用途 ,管道功能和渗透性。 已经发现VEGF145及其衍生物是血管内皮细胞的活性丝裂原,并且在体内用作血管生成因子。 VEGF145及其衍生物与先前表征的VEGF物质相比具有新的特性,其相对于细胞分布,对氧化损伤的敏感性和细胞外基质(ECM)结合能力。 本发明还涉及VEGF145的衍生物,其具有改变的性质,因为它们与VEGF145相比具有改变的生物活性和改变的肝素结合活性。 本发明提供了治疗心血管系统,增强患病血管的内皮化,并通过提供新的VEGF蛋白产物增强药物渗透的方法。 本发明还提供用于本发明方法的表达载体,组合物和试剂盒。

    Heparanase specific molecular probes and their use in research and medical applications
    28.
    发明授权
    Heparanase specific molecular probes and their use in research and medical applications 有权
    肝素酶特异性分子探针及其在研究和医学应用中的应用

    公开(公告)号:US06531129B2

    公开(公告)日:2003-03-11

    申请号:US09322977

    申请日:1999-06-01

    IPC分类号: A61K39395

    摘要: A variety of heparanase specific molecular probes which can be used for research and medical applications including diagnosis and therapy are disclosed. Specific applications include the use of a heparanase specific molecular probe for detection of the presence, absence or level of heparanase expression; the use of a heparanase specific molecular probe for therapy of a condition associated with expression of heparanase; the use of a heparanase specific molecular probe for quantification of heparanase in a body fluid; the use of a heparanase specific molecular probe for targeted drug delivery; and, the use of a heparanase specific molecular probe as a therapeutic agent.

    摘要翻译: 公开了可用于包括诊断和治疗在内的研究和医学应用的各种肝素酶特异性分子探针。 具体应用包括使用乙酰肝素酶特异性分子探针来检测乙酰肝素酶表达的存在,不存在或水平; 使用乙酰肝素酶特异性分子探针治疗与肝素酶表达相关的病症; 使用肝素酶特异性分子探针来定量体液中的乙酰肝素酶; 使用乙酰肝素酶特异性分子探针进行靶向药物递送; 以及使用乙酰肝素酶特异性分子探针作为治疗剂。

    Heparanase specific molecular probes and their use in research and medical applications
    29.
    发明授权
    Heparanase specific molecular probes and their use in research and medical applications 失效
    肝素酶特异性分子探针及其在研究和医学应用中的应用

    公开(公告)号:US06177545B1

    公开(公告)日:2001-01-23

    申请号:US09071739

    申请日:1998-05-01

    IPC分类号: C12P2108

    摘要: A variety of heparanase specific molecular probes which can be used for research and medical applications including diagnosis and therapy. Specific applications include the use of a heparanase specific molecular probe for detection of the presence, absence or level of heparanase expression; the use of a heparanase specific molecular probe for therapy of a condition associated with expression of heparanase; the use of a heparanase specific molecular probe for quantification of heparanase in a body fluid; the use of a heparanase specific molecular probe for targeted drug delivery; and the use of a heparanase specific molecular probe as a therapeutic agent.

    摘要翻译: 各种乙酰肝素酶特异性分子探针,可用于研究和医疗应用,包括诊断和治疗。 具体应用包括使用乙酰肝素酶特异性分子探针来检测乙酰肝素酶表达的存在,不存在或水平; 使用乙酰肝素酶特异性分子探针治疗与肝素酶表达相关的病症; 使用肝素酶特异性分子探针来定量体液中的乙酰肝素酶; 使用乙酰肝素酶特异性分子探针进行靶向药物递送; 以及使用乙酰肝素酶特异性分子探针作为治疗剂。