公开(公告)号：US5401742A

公开(公告)日：1995-03-28

申请号：US214467

申请日：1994-03-18

申请人： Takashi Hirano ,  Takeshi Todoroki ,  Shinichi Ohashi ,  Tomokuni Kokubu ,  Hideaki Tanaka

发明人： Takashi Hirano ,  Takeshi Todoroki ,  Shinichi Ohashi ,  Tomokuni Kokubu ,  Hideaki Tanaka

IPC分类号： A61K31/505 ,  A61K47/48 ,  A61P35/00 ,  C08F281/00 ,  C08L33/06

CPC分类号： A61K47/48192

摘要： Methotrexate, which is a known anticancer agent, can be converted into a polymeric conjugate with a pyran copolymer, which in itself has a certain anticancer effect, by a method in which an alkylene diamine is reacted with the carboxyl group of the methotrexate molecule to give an amidation product having a free amino group in a molecule, which is then reacted with the carboxyl group of the pyran copolymer, of which at least 10% of the repeating units have been modified with the methotrexate residue. The polymeric conjugate has sustained releasability of the methotrexate compound in blood serum so that an excellent therapeutic effect can be obtained by the administration thereof against cancers with little problems due to the side effects caused by an unduly high concentration of the drug in blood unavoidable when methotrexate as such is administrated.

摘要翻译： 通过使亚烷基二胺与甲氨蝶呤分子的羧基反应而得到的方法，可以将已知抗癌剂的甲氨蝶呤与吡喃共聚物转化为本身具有一定抗癌作用的聚合物， 分子中具有游离氨基的酰胺化产物，然后与吡喃共聚物的羧基反应，其中至少10％的重复单元已被甲氨蝶呤残基修饰。 聚合物缀合物具有甲氨蝶呤化合物在血清中具有持续的释放性，因此，由于由于甲氨蝶呤中不可避免的血液中药物浓度过高而引起的副作用，因此通过对癌症给药而获得优异的治疗效果 因此被管理。