申请人:Ceskoslovenska akademie ved
公开号:EP0187547A2
公开(公告)日:1986-07-16
A polymeric drug comprising an inert synthetic polymeric carrier combined through aminoacid or peptide spacers with a bioactive molecule, a targeting moiety, and an optional cross-linkage, comprises:
(a) 5.0 to 99.7 mol % of units derived from N-(2-hydroxypropyl) methacrylamide,
(b) 0.2 to 20.0 mol % of units derived from an N-methacryloylated peptide, the peptide groups being bound to a bioactive moiety,
(c) 0.1 to 94.8 mol % of units derived from N-methacrylamide, N-methacrylic acid or an N-meth- ecryloylated aminoacid or peptide, to which are bound a determinant capable of interacting with specific receptors on cell surfaces,
(d) optionally, 0 to 5 mol % of units derived from an N-methacryloylated peptide, the peptide groups being bound to a linking group which is similarly attached to a similar peptide group attached to another polymer chain, and
(e) optionally, as a bioassay label, Q to 2 mol % of units derived from N-methacryloylated tyrosinamide.
一种聚合药物,由惰性合成聚合载体通过氨基酸或肽间隔与生物活性分子、靶向分子和可选的交联剂结合而成,包括
(a) 5.0 至 99.7 摩尔%由 N-(2-羟丙基)甲基丙烯酰胺衍生的单元、
(b) 0.2 至 20.0 摩尔%由 N-甲基丙烯酰化肽衍生的单元,肽基与生物活性分子结合、
(c) 0.1 至 94.8 摩尔%的单元来自 N-甲基丙烯酰胺、N-甲基丙烯酸或 N-甲基丙烯酰化的氨基酸或肽,其上结合了能与细胞表面特定受体相互作用的决定因子、
(d) 可选地,0-5 摩尔%的单元来自 N-甲基丙烯酰化肽,这些肽基团与一个连接基 团结合,该连接基团与连接到另一个聚合物链上的类似肽基团相类似,以及 (e) 可选地,作为 N-甲基丙烯酰化肽的单元,这些肽基团与一个连接基团结合, 该连接基团与连接到另一个聚合物链上的类似肽基团相类似。
(e) 作为生物测定标签,可选 Q 至 2 摩尔%的衍生自 N-甲基丙烯酰化酪氨酰胺的单元。