发明授权
US5401742A Polymeric conjugate of methotrexate compound and pyran copolymer and
method for the preparation thereof
失效
甲氨蝶呤化合物和吡喃共聚物的聚合物缀合物及其制备方法
- 专利标题: Polymeric conjugate of methotrexate compound and pyran copolymer and method for the preparation thereof
- 专利标题(中): 甲氨蝶呤化合物和吡喃共聚物的聚合物缀合物及其制备方法
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申请号: US214467申请日: 1994-03-18
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公开(公告)号: US5401742A公开(公告)日: 1995-03-28
- 发明人: Takashi Hirano , Takeshi Todoroki , Shinichi Ohashi , Tomokuni Kokubu , Hideaki Tanaka
- 申请人: Takashi Hirano , Takeshi Todoroki , Shinichi Ohashi , Tomokuni Kokubu , Hideaki Tanaka
- 申请人地址: JPX Tokyo
- 专利权人: Japan, as represented by Director General of Agency of Industrial Science and Technology
- 当前专利权人: Japan, as represented by Director General of Agency of Industrial Science and Technology
- 当前专利权人地址: JPX Tokyo
- 优先权: JPX5-132873 19930511
- 主分类号: A61K31/505
- IPC分类号: A61K31/505 ; A61K47/48 ; A61P35/00 ; C08F281/00 ; C08L33/06
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.
公开/授权文献
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