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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

Polymeric conjugate of methotrexate compound and pyran copolymer and
method for the preparation thereof
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.
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