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    • 1. 发明申请
    • Novel curcuminoid-factor VIIa constructs as suppressors of tumor growth and angiogenesis
    • 新型姜黄素因子VIIa构建成肿瘤生长和血管生成抑制因子
    • US20060229239A9
    • 2006-10-12
    • US10383898
    • 2003-03-07
    • Mamoru ShojiJames SnyderDennis LiottaAiming Sun
    • Mamoru ShojiJames SnyderDennis LiottaAiming Sun
    • A61K38/17
    • C12Y304/21021A61K47/64A61K47/6425C07D213/63C12N9/6437
    • The fluorinated curcuminoid (3,5-bis-(2-fluorobenzylidene)-piperidin-4-one-acetate is about ten times more effective at arresting the growth of tumor cells than cisplatin. The present invention provides methods to deliver a cytotoxic compound, such as a curcuminoid, specifically to cancer cells and to the vascular endothelial cells that nourish solid tumors. The method involves tethering the drug to a protein such as in factor VIIa that retains high affinity for the surface protein tissue factor. Upon complexation, the resulting heterodimer is endocytosed and the drug is subsequently liberated inside the target cell via proteolytic cleavage. The present invention further provides for the synthesis of novel curcuminoid-tether-linker-factor VIIa compositions and for methods of delivery of effective doses of the novel compositions to target tumor or endothelial cells in a patient
    • 氟化姜黄素(3,5-双 - (2-氟亚苄基) - 哌啶-4-酮乙酸酯在阻止肿瘤细胞生长方面比顺铂高约十倍。本发明提供递送细胞毒性化合物的方法, 例如姜黄素,特别是癌细胞和滋养实体瘤的血管内皮细胞,该方法涉及将药物系在蛋白质上,例如对表面蛋白组织因子保持高亲和力的因子VIIa,在复合后,产生 异二聚体被内吞,并且药物随后通过蛋白水解切割在靶细胞内释放。本发明还提供了新型姜黄素 - 连接子 - 连接因子VIIa组合物的合成和用于将有效剂量的新组合物递送至靶 肿瘤或内皮细胞
    • 3. 发明申请
    • Cytotoxic compound-protein conjugates as suppressors of tumor growth and angiogenesis
    • 细胞毒性复合物 - 蛋​​白质缀合物作为肿瘤生长和血管发生的抑制剂
    • US20050069551A1
    • 2005-03-31
    • US10900490
    • 2004-07-28
    • Mamoru ShojiJames SnyderDennis LiottaAiming Sun
    • Mamoru ShojiJames SnyderDennis LiottaAiming Sun
    • A61K47/48C07D213/63C12N9/64A61K39/395C07K16/46
    • C12N9/6437A61K47/64A61K47/642A61K47/6849C07D213/63C12Y304/21021
    • Compositions and methods are provided for delivering cytotoxic compounds, such as natural curcumoids and synthetic curcumin analogs, specifically to cancer cells and to blood vessels that nourish solid tumors. The compositions include a cytotoxic drug tethered to a protein, such as factor VIIa, which can bind with high affinity to a receptor, such as tissue factor, expressed on the surface of cancer cells and vascular endothelial cells within the tumor microenvironment. Upon binding, the drug-protein-receptor complex is endocytosed and the drug is subsequently liberated inside the target cell via proteolytic cleavage. The compositions and methods may increase the efficacy of the cytotoxic agets and decrease their side effects by delivering the agents to specific target cells, such as cancer cells, vascular endothelial cells in a tumor, and metastatic foci anywhere in the body, providing the target cells express surface bound tissue factor. Additionally, methods of synthesis of cytotoxic compound-protein conjugates are provided, for example, curcuminoid-tether-linker-factor VIIa composition, as well as pharmaceutically acceptable compositions and methods for delivering a therapeutically-effective amount of a cytotoxic compound-protein conjugate together with one or more pharmaceutically acceptable carriers (additives) and/or diluents to an animal or human patient.
    • 提供组合物和方法用于递送细胞毒性化合物,例如天然的姜黄素和合成的姜黄素类似物,特别是癌细胞和滋养实体瘤的血管。 组合物包括与诸如因子VIIa结合的蛋白质的细胞毒性药物,其可以高度亲和力结合到在肿瘤微环境中在癌细胞表面和血管内皮细胞表面上的受体,例如组织因子。 结合后,药物 - 蛋​​白 - 受体复合物被内吞,并且药物随后通过蛋白水解切割在靶细胞内释放。 组合物和方法可以通过将药物递送到特定靶细胞,例如肿瘤中的癌细胞,血管内皮细胞和体内任何地方的转移灶,来增加细胞毒性作用的功效并降低其副作用,提供靶细胞 表达结合组织因子。 此外,提供了合成细胞毒性化合物 - 蛋​​白质缀合物的方法,例如,姜黄素 - 链 - 连接体 - 因子VIIa组合物,以及用于将治疗有效量的细胞毒性化合物 - 蛋​​白质缀合物一起递送的药学上可接受的组合物和方法 与动物或人类患者的一种或多种药学上可接受的载体(添加剂)和/或稀释剂。
    • 10. 发明授权
    • Single solvent process for preparing 2-methallyloxy-phenol from catechol
    • 用于从儿茶酚制备2-甲基烯丙氧基 - 苯酚的单一溶剂法
    • US4851587A
    • 1989-07-25
    • US200336
    • 1988-05-31
    • Borivoj Franko-FilipasicJames Snyder
    • Borivoj Franko-FilipasicJames Snyder
    • C07C41/16
    • C07C41/16
    • 2-Methallyloxyphenol precursor to 2,3-dihydro-2,2-dimethyl-7-hydroxybenzofuran is prepared selectively and in good yield in the etherification of an alkali metal catecholate by methallyl chloride in an improved process using the same solvent medium for both the precursor and the hydroxybenzofuran, the process characterized by a solvent medium comprising an aromatic hydrocarbon solvent, the medium also containing an amine selected from alkylamines and N-heterocyclic amines. The amine forms a quaternary salt with the methallyl chloride in situ to catalyze the etherification and the aromatic solvent permits rearrangement of the product and Claisen closure to a benzofuran intermediate without solvent exchange.
    • 对于2,3-二氢-2,2-二甲基-7-羟基苯并呋喃的2-甲基丙烯酰氧基苯酚前体是通过甲基烯丙基氯在碱金属儿茶酚酸的醚化中以良好的收率制备的,使用相同的溶剂介质, 前体和羟基苯并呋喃,该方法的特征在于包含芳族烃溶剂的溶剂介质,该介质还含有选自烷基胺和N-杂环胺的胺。 胺与甲代烯丙基氯原位形成季盐以催化醚化,并且芳族溶剂允许将产物重新排列并将Claisen封闭物重整至苯并呋喃中间体而无需溶剂交换。