发明公开
EP1782833A2 pH-sensitive polymeric conjugates of an anthracycline cancerostatic drug for targeted therapy
审中-公开
pH敏感聚合物 - 魔芋螨蒽环类药物Kanzerostatikumsfürgezielte Therapie
- 专利标题： pH-sensitive polymeric conjugates of an anthracycline cancerostatic drug for targeted therapy
- 专利标题（中）： pH敏感聚合物 - 魔芋螨蒽环类药物Kanzerostatikumsfürgezielte Therapie
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申请号： EP06025316.8申请日： 2002-12-20
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公开(公告)号： EP1782833A2公开(公告)日： 2007-05-09
- 发明人: Ulbrich, Karel , Etrych, Thomás , Rihova, Blanka, , Jelinkova, Markéta , Kovar, Marek
- 申请人： Zentiva, a.s.
- 申请人地址： Dolni Mecholupy 130 102 37 Praha 10 CZ
- 专利权人： Zentiva, a.s.
- 当前专利权人： Zentiva, a.s.
- 当前专利权人地址： Dolni Mecholupy 130 102 37 Praha 10 CZ
- 代理机构： Jirotkova, Ivana
- 优先权： CZ20014653 20011220
- 主分类号： A61K47/48
- IPC分类号： A61K47/48
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 α-amino acids, ε-amino acids, aromatic amino acids, or oligopeptides terminated with a molecule of an anthracycline cancerostatic
c. 0.5 to 15 % of units ofmethacryloylated α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides or their sodium salts, and optionally
d. 0.5 to 10 % of units of methacryloylated hydrazides of α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides
e. 0.5 to 5 % of methacryloylated α-amino acids, ε-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, β-alanine, γ-amino butyric acid, ε-amino caproic acid (AKap), p-amino benzoic acid (AB), and S is an antibody selected from the following series: γ-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.
a. 60 to 99 % of N -(2-hydroxypropyl)methacrylamide units
b. 1 to 25 % of units of methacryloylated hydrazones of α-amino acids, ε-amino acids, aromatic amino acids, or oligopeptides terminated with a molecule of an anthracycline cancerostatic
c. 0.5 to 15 % of units ofmethacryloylated α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides or their sodium salts, and optionally
d. 0.5 to 10 % of units of methacryloylated hydrazides of α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides
e. 0.5 to 5 % of methacryloylated α-amino acids, ε-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, β-alanine, γ-amino butyric acid, ε-amino caproic acid (AKap), p-amino benzoic acid (AB), and S is an antibody selected from the following series: γ-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.
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