首页> 外国专利> MOLECULE interferon-β-1a HUMAN pegylated with antiviral, immunomodulatory and antiproliferative activity, with improved stability, reduce immunogenicity, improved pharmacokinetic and pharmacodynamic parameters are suitable for medical use, and immunobiological BEING BASED ON HER

MOLECULE interferon-β-1a HUMAN pegylated with antiviral, immunomodulatory and antiproliferative activity, with improved stability, reduce immunogenicity, improved pharmacokinetic and pharmacodynamic parameters are suitable for medical use, and immunobiological BEING BASED ON HER

机译:具有抗病毒,免疫调节和抗增殖活性的聚乙二醇化的分子干扰素-β-1a人类,具有改善的稳定性,降低的免疫原性,改善的药代动力学和药效学参数,适用于医疗用途,并且免疫生物学基于HER

摘要

1. Stable conjugate of PEGylated interferon-β-1a Human of formula (I), representing one positional isomer: where n - integral values ​​from 454 to 909; m - integer ≥4; NH-IFN - interferon-β-1a.2 . The conjugate according to Claim. 1, wherein m is an integer equal to 4.3. The conjugate according to Claim. 1, wherein the interferon-β-1a is a natural or recombinant interferon-β-1a cheloveka.4. The conjugate according to Claim. 1, wherein η is an integer from 454 to 909.5. The conjugate according to Claim. 1, wherein the N-terminal group is represented by methionine residue (Met) .6. The conjugate according to Claim. 1, wherein the N-terminal group is represented by serine (Ser) .7. Pharmaceutical composition having antiviral, antiproliferative and immunomodulating activity, containing conjugate of general formula (I) in an effective amount and a pharmaceutically acceptable auxiliary komponenty.8. A pharmaceutical composition according to claim. 7 for use as a medicament for the treatment of autoimmune, viral and oncologic diseases and diseases associated with primary or secondary immunodeficiency sostoyaniyami.9. A pharmaceutical composition according to claim. 8, wherein the autoimmune disease is diffused skleroz.10. A pharmaceutical composition according to claim. 8, where viral disease is hepatitis C or hepatitis B.11. A pharmaceutical composition according to claim. 8, wherein the viral disease is genital kondilomy.12. A pharmaceutical composition according to claim. 8, where oncologic disease is a melanomu.13. A medicament comprising a conjugate of formula (I), having antiviral, antiproliferative and immunomodulatory aktivnostyu.14. A medicament according to claim. 13, further comprising b
机译:1.聚乙二醇化干扰素-β-1a人的稳定缀合物,代表式(I)的一个位置异构体:其中n-整数值为454至909; m-整数≥4; NH-IFN-干扰素-β-1a.2。根据权利要求1的缀合物。 1,其中m是等于4.3的整数。根据权利要求1的缀合物。 1,其中干扰素-β-1a是天然或重组干扰素-β-1acheloveka。4。根据权利要求1的缀合物。 1,其中η是454至909.5的整数。根据权利要求1的缀合物。 1,N末端基团由甲硫氨酸残基(Met).6表示。根据权利要求1的缀合物。 1,其中N端基团由丝氨酸(Ser).7表示。具有抗病毒,抗增殖和免疫调节活性的药物组合物,包含有效量的通式(I)的缀合物和药学上可接受的辅助成分。8。根据权利要求1的药物组合物。 7用作治疗自身免疫,病毒和肿瘤疾病以及与原发性或继发性免疫缺陷sostoyaniyami.9相关的疾病的药物。9。根据权利要求1的药物组合物。 8,其中自身免疫疾病是弥散性skleroz.10。根据权利要求1的药物组合物。 8,病毒性疾病是丙型肝炎或乙型肝炎。11。根据权利要求1的药物组合物。 8,其中病毒性疾病是生殖器官kondilomy 12。根据权利要求1的药物组合物。 8,其中的肿瘤是黑色素瘤。13。包含式(I)的缀合物的药物,其具有抗病毒,抗增殖和免疫调节的aktivnostyu。14。根据权利要求1的药物。 13,进一步包括b

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