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    • 5. 发明申请
    • METHOD OF PRODUCING FULLY CARBAMYLATED ERYTHROPOIETIN
    • 生产完全氨基甲酰化红细胞生成素的方法
    • WO2006014349A3
    • 2006-07-20
    • PCT/US2005023505
    • 2005-07-01
    • KENNETH S WARREN INST INCCERAMI ANTHONYHAND CARLA CERAMIXIE QIAO WENBRINES MICHAEL
    • BRINES MICHAEL
    • A61K38/00
    • C07K14/505A61K38/00
    • The present invention relates to a method of carbamylating an erythropoietin such that the resulting carbamylated erythropoietin has less that about 10% free primary amines on the lysines and the N-terminal amino acids, is not digested when exposed to Lys-C proteolysis, exhibits no erythropoietic activity in a TF-1 or UT-7/EPOR cell viability assay at a concentration of 1 µg/ml, and demonstrates a static sciatic index of less than about .65 within a Sciatic Nerve Assay. Additionally, the invention is related to pharmaceutical compositions containing carbamylated erythropoietins of the invention and the use of the pharmaceutical compositions for the treatment of conditions and diseases of excitable tissues.
    • 本发明涉及使促红细胞生成素氨基甲酰化的方法,使得所得的氨基甲酰化促红细胞生成素具有少于赖氨酸上约10%的游离伯胺和N端氨基酸,当暴露于Lys-C蛋白水解时不被消化, 在浓度为1μg/ ml的TF-1或UT-7 / EPOR细胞活力测定中的促红细胞生成活性,并且在坐骨神经分析中显示小于约.65的静态坐骨指数。 此外,本发明涉及含有本发明的氨基甲酰化促红细胞生成素的药物组合物以及该药物组合物用于治疗可兴奋组织的病症和疾病的用途。