发明名称 PH-SENSITIVE POLYMERIC CONJUGATES OF AN ANTHRACYCLINE CANCEROSTATIC DRUG FOR TARGETED THERAPY
摘要 Conjugates consisting of a polymeric carrier constituted by 30 to 3,000 monomer units linked to form a polymeric chain, composed of a. 60 to 99 % of N -(2-hydroxypropyl)methacrylamide units b. 1 to 25 % of units of methacryloylated hydrazones of ±-amino acids, µ-amino acids, aromatic amino acids, or oligopeptides terminated with a molecule of an anthracycline cancerostatic c. 0.5 to 15 % of units ofmethacryloylated ±-amino acids, µ-amino acids, aromatic amino acids or oligopeptides or their sodium salts, and optionally d. 0.5 to 10 % of units of methacryloylated hydrazides of ±-amino acids, µ-amino acids, aromatic amino acids or oligopeptides e. 0.5 to 5 % of methacryloylated ±-amino acids, µ-amino acids or oligopeptides terminated by a molecule of immunoglobulin or of a specific monoclonal or polyclonal antibody, of the below given general formula, the individual structural units being disposed in a random manner in the chain and where x ranges from 20 to 3,000, a is from 1 to 750, b and c are each from 1 to 450, d ranges from 1 to 150, X is a residue of an amino acid or oligopeptide chosen from the following series: Gly, Ala, Leu, GlyGly, GlyLeuGly, GlyPheGly, GlyPheLeuGly, ²-alanine, ³-amino butyric acid, µ-amino caproic acid (AKap), p-amino benzoic acid (AB), and S is an antibody selected from the following series: ³-globulin for i.v. administrations, autologous antibodies, antibodies anti-17-1A, anti-CA 15-3 and the like, linked to the polymeric chain by the marked structure.
申请公布号 PL216518(B1) 申请公布日期 2014.04.30
申请号 PL20020370719 申请日期 2002.12.20
申请人 ZENTIVA, A.S. 发明人 ULBRICH KAREL;ETRYCH TOMÁ&Scaron,;&Rcaron,ÍHOVÁ BLANKA;JELÍNKOVÁ MARKÉTA;KOVÁ&Rcaron, MAREK
分类号 A61K47/48;A61K31/78;A61K39/395;A61P35/00;C07K5/083;C07K5/103;C07K7/06;C07K16/00 主分类号 A61K47/48
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